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Investigating the Effects of Dorema hyrcanum Root Extracts on Selective Induction of Programmed Cell Death in Glioblastoma, Ovarian Cancer and Breast Cancer Cell Lines Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-03-14 Mahsa Hatami, Shamim Sahranavard, Fereshteh Bagheri, Zahra Shahsavari, Siamak Salami
Background: Despite remarkable advances, cancer has remained the second cause of death, which shows that more potent novel compounds should be found. Ethnobotanical compounds have a long history of treating diseases, and several approved chemotherapeutic compounds were isolated from plants. background: Despite remarkable advances, cancer has remained the second cause of death which shows that more
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Tabersonine Induces the Apoptosis of Human Hepatocellular Carcinoma In vitro and In vivo Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-03-11 Xuan Li, Xudan Li, Lianghua Chen, Yuan Deng, Zhizhong Zheng, Yanlin Ming
Background: Tabersonine, a natural indole alkaloid derived from Apocynaceae plants, exhibits antiinflammatory and acetylcholinesterase inhibitory activities, among other pharmacological effects. However, its anti-tumor properties and the underlying molecular mechanisms remain underexplored. background: Natural indole alkaloid Tabersonine is derived from Apocynaceae plants. It possesses good anti-inflammatory
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Ginsenoside Rb1 Inhibits the Proliferation of Lung Cancer Cells by Inducing the Mitochondrial-mediated Apoptosis Pathway Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-03-11 Lin Feng, Xinze Liu, Kaijing Sun, Ying Sun, Wei Wu, Changbao Chen, Xin Jin, Xilin Wan
Background: Lung cancer is one of the more common malignant tumors posing a great threat to human life, and it is very urgent to find safe and effective therapeutic drugs. The antitumor effect of ginsenosides has been reported to be a treatment with a strong effect and a high safety profile. Objective: This paper aimed to investigate the inhibitory effect of ginsenoside Rb1 on 95D and NCI-H460 lung
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Hyperoxic-hypoxic Paradox: Breast Cancer Microenvironment and an Innovative Treatment Strategy Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-03-01 Suman Kumar Ray, Sukhes Mukherjee
: A small therapeutic range of oxygen is required for effective metabolism. As a result, hypoxia (low oxygen concentration) is one of the most potent inducers of gene expression, metabolic alterations, and regenerative processes, such as angiogenesis, stem cell proliferation, migration, and differentiation. The cellular response is controlled by sensing the increased oxygen levels (hyperoxia) or hypoxia
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Phytol and α-Bisabolol Synergy Induces Autophagy and Apoptosis in A549 Cells and Additional Molecular Insights through Comprehensive Proteome Analysis via Nano LC-MS/MS Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-28 Chandramohan Kiruthiga, Kambati Niharika, Kasi Pandima Devi
Background: Non-Small Cell Lung Cancer (NSCLC) is a malignancy with a significant prevalence and aggressive nature, posing a considerable challenge in terms of therapeutic interventions. Autophagy and apoptosis, two intricate cellular processes, are integral to NSCLC pathophysiology, each affecting the other through shared signaling pathways. Phytol (Phy) and α -bisabolol (Bis) have shown promise as
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Recent Advances in Chemistry, Mechanism, and Applications of Quantum Dots in Photodynamic and Photothermal Therapy Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-27 Faride Ranjbari, Farzaneh Fathi
: Semiconductor quantum dots (QD) are a kind of nanoparticle with unique optical properties that have attracted a lot of attention in recent years. In this paper, the characteristics of these nanoparticles and their applications in nanophototherapy have been reviewed. Phototherapy, including photodynamic therapy (PDT) and photothermal therapy (PTT), has gained special importance because of its high
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Anticancer Activity of Sargassum fluitans Extracts in Different Cancer Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-22 José Arnold González-Garrido, Javier Alejandro Gómez-García, Oswaldo Ignacio Hernández-Abreu, Ivonne María Olivares-Corichi, Fernando Pereyra-Vergara, José Rubén García-Sánchez
Background:: The arrival of large quantities of Sargassum in the Mexican Caribbean Sea has generated major environmental, health and economic problems. Although Sargassum has been used in the generation of some commercial products, few studies have described its possible applications as a source of compounds with anticancer activity. Objective:: This study aimed to evaluate the antiproliferative effects
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Ivermectin Inhibits Bladder Cancer Cell Growth and Induces Oxidative Stress and DNA Damage Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-20 Ning Fan, Lixiu Zhang, Zhiping Wang, Hui Ding, Zhongjin Yue
Background: Bladder cancer is the most common malignant tumor of the urinary system. Nevertheless, current therapies do not provide satisfactory results. It is imperative that novel strategies should be developed for treating bladder cancer. Objective: To evaluate the effect of a broad-spectrum anti-parasitic agent, Ivermectin, on bladder cancer cells in vitro and in vivo. Method: CCK-8 and EdU incorporation
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Corrigendum to: Investigation of the Apoptosis Inducing and β-catenin Silencing by Tetradentate Schiff Base Zinc(II) Complex on the T-47D Breast Cancer Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-20 Mostafa Heidari Majd, Xiangyu Guo
A typographical error appeared in the author affiliation titled “Investigation of the Apoptosis Inducing and β-catenin Silencing by Tetradentate Schiff Base Zinc(II) Complex on the T-47D Breast Cancer Cells”, published in Anti-Cancer Agents in Medicinal Chemistry, 2023, 23(15) [1]. Details of the error and a correction are provided here. Original: Author Affiliation: 2Department of Breast Medicine
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Drug Repositioning for Ovarian Cancer Treatment: An Update Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-16 Maria Maddalena Cavalluzzi, Maurizio Viale, Natalie Paola Rotondo, Valeria Ferraro, Giovanni Lentini
: Ovarian cancer (OC) is one of the most prevalent malignancies in female reproductive organs, and its 5-year survival is below 45%. Despite the advances in surgical and chemotherapeutic options, OC treatment is still a challenge, and new anticancer agents are urgently needed. Drug repositioning has gained significant attention in drug discovery, representing a smart way to identify new clinical applications
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1,3-Diaryl Triazenes Incorporating Disulfonamides Show Both Antiproliferative Activity and Effective Inhibition of Tumor-associated Carbonic Anhydrases IX and XII Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-16 Nebih Lolak, Suleyman Akocak, Andrea Petreni, Yakup Budak, Esra Bozgeyik, Meliha Burcu Gurdere, Mustafa Ceylan, Claudiu T. Supuran
Aim: The aim of this study was to synthesize a library of novel di-sulfa drugs containing 1,3- diaryltriazene derivatives TS (1-13) by conjugation of diazonium salts of primary sulfonamides with sulfa drugs to investigate the cytotoxic effect of these new compounds in different cancer types and to determine their inhibitory activity against tumor-associated carbonic anhydrases IX and XII. Materials
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Indirubin, an Active Component of Indigo Naturalis, Exhibits Inhibitory Effects on Leukemia Cells via Targeting HSP90AA1 and PI3K/Akt Pathway Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-12 Yuanzhi Yao, Xiaoying Li, Xiaoqin Yang, Hai Mou, Lin Wei
Background: This research intended to predict the active ingredients and key target genes of Indigo Naturalis in treating human chronic myeloid leukemia (CML) using network pharmacology and conduct the invitro verification. Methods: The active components of Indigo Naturalis and the corresponding targets and leukemia-associated genes were gathered through public databases. The core targets and pathways
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Antheraea proylei J. Sericin Induces Apoptosis in a Caspase-dependent Manner in A549 and HeLa Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-12 Potsangbam Jolly Devi, Asem Robinson Singh, Naorem Tarundas Singh, Laishram Rupachandra Singh, Sanjenbam Kunjeshwori Devi, Lisam Shanjukumar Singh
Background: In spite of much progress in cancer, the global cancer burden is still significant and increasing. Sericin, an adhesive protein of silk cocoons, has been shown to be a potential protein in various biomedical applications, including cancer therapeutics. The present study evaluates the anticancer property of sericin from cocoons of Antheraea proylei J (SAP) against human lung cancer (A549)
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Anti-proliferative, Morphological and Molecular Docking Studies of New Thiophene Derivatives and their Strategy in Ionic Liquids Immobilized Reactions Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-06 Rafat M. Mohareb, Sayeed Mukhtar, Humaira Parveen, Mahmoud A. Abdelaziz, Ensaf S. Alwan
Background: A number of research were conducted on the pyran and thiophene derivatives, which were attributed to have a wide range of biological activities, including anti-plasmodial, as well as acting as caspase, hepatitis C and cancer inhibitors. Objective: The multicomponent reactions of the 5-acetyl-2-amino-4-(phenylamino)-thiophene-3-carbonitrile produced biologically active target molecules like
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Cordyceps militaris: A Comprehensive Study on Laboratory Cultivation and Anticancer Potential in Dalton's Ascites Lymphoma Tumor Model Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-02 Diksha Dutta, Namram Sushindrajit Singh, Rohit Aggarwal, Akalesh Kumar Verma
Background: Cancer, a predominant cause of mortality, poses a formidable challenge in our pursuit of elevating life expectancy. Throughout history, individuals have sought natural remedies with minimal side effects as an appealing substitute for chemotherapeutic drugs. One such remedy is Cordyceps militaris, a renowned medicinal mushroom deeply entrenched in Asian ethnomedicine. Revered for its rejuvenating
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Synthesis of a Novel Gold(I) Complex and Evaluation of Its Anticancer Properties in Breast Cancer Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-02 Haseeb A. Khan, Anvarhusein A. Isab, Abdullah S. Alhomida, Mansour K. Gatasheh, Ali Al-Hoshani, Bashayr A. Aldhafeeri, N Rajendra Prasad
Background: Platinum complexes are commonly used for cancer chemotherapy; however, they are not only highly-priced but also have various side effects. It is, therefore, important to design affordable anticancer drugs with minimal side effects. background: Platinum complexes are commonly used for cancer chemotherapy however they are not only highly priced but also have various side effects. It is therefore
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Targeting Breast Cancer with N-Acetyl-D-Glucosamine: Integrating Machine Learning and Cellular Assays for Promising Results Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-02 Ömür Baysal, Deniz Genç, Ragıp Soner Silme, Kevser Kübra Kırboğa, Dilek Çoban, Naeem Abdul Ghafoor, Leyla Tekin, Osman Bulut
Background: Breast cancer is a common cancer with high mortality rates. Early diagnosis is crucial for reducing the prognosis and mortality rates. Therefore, the development of alternative treatment options is necessary. Objective: This study aimed to investigate the inhibitory effect of N-acetyl-D-glucosamine (D-GlcNAc) on breast cancer using a machine learning method. The findings were further confirmed
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Thiosemicarbazone-benzene Sulfonamide Derivatives as Human Carbonic Anhydrases Inhibitors: Synthesis, Characterization, and In silico Studies Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-02-01 Muhammed Trawally, Kübra Demir-Yazıcı, Andrea Angeli, Kerem Kaya, Atilla Akdemir, Claudiu T. Supuran, Özlen Güzel-Akdemir
Introduction: Carbonic anhydrases (CAs) are widespread metalloenzymes with the core function of catalyzing the interconversion of CO2 and HCO3-. Targeting these enzymes using selective inhibitors has emerged as a promising approach for the development of novel therapeutic agents against multiple diseases. Methods: A series of novel thiosemicarbazone-containing derivatives were synthesized, characterized
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Cervical Cancer Therapeutics: An In-depth Significance of Herbal and Chemical Approaches of Nanoparticles Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-31 Istuti Saraswat, Anjana Goel
Cervical cancer emerges as a prominent health issue, demanding attention on a global level for women's well-being, which frequently calls for more specialized and efficient treatment alternatives. Traditional therapies may have limited tumour targeting and adverse side effects. Recent breakthroughs have induced a transformative shift in the strategies employed against cervical cancer. biocompatible
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Novel N-(3-ethynyl Phenyl)-6,7-bis(2-methoxyethoxy)Quinazoline-4-amine Derivatives: Synthesis, Characterization, Anti-cancer Activity, In-silico and DFT Studies Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-29 Amitananda Dash, Guruswamy Vaddamanu, Raja Karreddula, Surya Surendra Babu Manubolu, Pavana Kumari G., Naveen Mulakayala
Background: Cancer is one of the most common reasons for mortality in the world. A continuous effort to develop effective anti-cancer drugs with minimum side effects has become necessary. The use of small-molecule drugs has revolutionized cancer research by inhibiting cancer cell survival and proliferation. Quinazolines are a class of bioactive heterocyclic compounds with active pharmacophores in several
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An Expedition on Synthetic Methodology of FDA-approved Anticancer Drugs (2018-2021) Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-29 S. Vishakha, N. Navneesh, Balak Das Kurmi, Ghanshyam Das Gupta, Sant Kumar Verma, Ankit Jain, Preeti Patel
New drugs being established in the market every year produce specified structures for selective biological targeting. With medicinal insights into molecular recognition, these begot molecules open new rooms for designing potential new drug molecules. In this review, we report the compilation and analysis of a total of 56 drugs including 33 organic small molecules (Mobocertinib, Infigratinib, Sotorasib
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An Insight into the Effect of Schiff Base and their d and f Block Metal Complexes on Various Cancer Cell Lines as Anticancer Agents: A Review Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-25 Presenjit, Shubhra Chaturvedi, Akanksha Singh, Divya Gautam, Kaman Singh, Anil kumar Mishra
Over the last few decades, an alarming rise in the percentage of individuals with cancer and those with multi-resistant illnesses has forced researchers to explore possibilities for novel therapeutic approaches. Numerous medications currently exist to treat various disorders, and the development of small molecules as anticancer agents has considerable potential. However, the widespread prevalence of
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Nanotechnology Utilizing Ferroptosis Inducers in Cancer Treatment Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-24 Soghra Farzipour, Fatemeh Jalali Zefrei, Saeed Bahadorikhalili, Maryam Alvandi, Arsalan Salari, Zahra Shaghaghi
Current cancer treatment options have presented numerous challenges in terms of reaching high efficacy. As a result, an immediate step must be taken to create novel therapies that can achieve more than satisfying outcomes in the fight against tumors. Ferroptosis, an emerging form of regulated cell death (RCD) that is reliant on iron and reactive oxygen species, has garnered significant attention in
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Design, Synthesis, In vitro and In vivo Evaluation of New Imidazo[1,2-a]pyridine Derivatives as Cyclooxygenase-2 Inhibitors Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-24 Nahid Ahmadi, Mona Khoramjouy, Mahsa Azami Movahed, Salimeh Amidi, Mehrdad Faizi, Afshin Zarghi
Background: Cyclooxygenase-2 (COX-2), the key enzyme in the arachidonic acid conversion to prostaglandins, is one of the enzymes associated with different pathophysiological conditions, such as inflammation, cancers, Alzheimer's, and Parkinson's disease. Therefore, COX-2 inhibitors have emerged as potential therapeutic agents in these diseases. Objective: The objective of this study was to design and
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A Contemporary Review on the Critical Role of Nonsteroidal Anti-inflammatory Agents in Colorectal Cancer Therapy Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-23 Parisa Zia Sarabi, Mohammad Moradi, Malihe Bagheri, Mohammad Reza Khalili, Shahrzad Moradifard, Tannaz Jamialahmadi, Faezeh Ghasemi, Amirhossein Sahebkar
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) are widely recognized as effective pain relievers and function by inhibiting the cyclooxygenase enzyme (COXs). Moreover, they have been found to participate in various cellular processes through different signaling pathways, such as WNT, MAPK, NF-KB, and PI3K/AKT/mTOR. This makes them potential candidates for chemoprevention of several malignancies, particularly
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Potential of Nanomedicines as an Alternative for the Treatment of Colorectal Cancer - A Review Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-23 Kammila Martins Nicolau Costa, Larissa Alves Barros, Ingrid Larissa da Silva Soares, João Augusto Oshiro-Junior
Colorectal cancer is the third most common cancer and the second in cases of cancer-related death. Polytherapy generates many adverse effects, leading the patient to give up. Nanotechnology has been studied in recent years to circumvent limitations. Groups composed of polymeric, lipid, and inorganic nanoparticles are the most purpose. Thus, the objective of this work is to bring information on how
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Preparation, Characterization, and Anticancer Activity Assessment of Chitosan/TPP Nanoparticles Loaded with Echis carinatus Venom Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-18 Maral Mahboubi Kancha, Mohsen Mehrabi, Fatemeh Sadat Bitaraf, Hamid Vahedi, Morteza Alizadeh, Andreas Bernkop-Schnürch
Aims and Background: Echis carinatus venom is a toxic substance naturally produced by special glands in this snake species. Alongside various toxic properties, this venom has been used for its therapeutic effects, which are applicable in treating various cancers (liver, breast, etc.). Objective: Nanotechnology-based drug delivery systems are suitable for protecting Echis carinatus venom against destruction
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Hyperoside Inhibits RNF8-mediated Nuclear Translocation of β-catenin to Repress PD-L1 Expression and Prostate Cancer Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-16 Jie Chen, Yi Zhao, Xiaoli Wang, Long Zang, Dengke Yin, Song Tan
Background: Hyperoside is a flavonol glycoside isolated from Hypericum perforatum L. that has inhibitory effects on cancer cells; however, its effects on prostate cancer (PCa) remain unclear. Therefore, we studied the anti-PCa effects of hyperoside and its underlying mechanisms in vitro and in vivo. Aim: This study aimed to explore the mechanism of hyperoside in anti-PCa. Methods: 3-(4,5-Dimethyl-2-Thiazolyl)-2
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Turmeric Extract-loaded Selenium Nanoparticles Counter Doxorubicin-induced Hepatotoxicity in Mice via Repressing Oxidative Stress, Inflammatory Cytokines, and Cell Apoptosis Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-09 Barakat M. ALRashdi, Mohamed M. Hussein, Rawan M. Mohammed, Nada W. Abdelhamed, Maran E. Asaad, Mubarak Alruwaili, Saad M. Alrashidi, Ola A. Habotta, Ahmed E. Abdel Moneim, Shimaa S. Ramadan
Background: Doxorubicin (DOX) is an antitumor anthracycline used to treat a variety of malignancies; however, its clinical use is associated with noticeable hepatotoxicity. Therefore, the current study was designed to delineate if biosynthesized SeNPs with turmeric extract (Tur-SeNPs) could alleviate DOX-induced hepatic adverse effects. Methods: Mice were orally post-treated with Tur extract, Tur-SeNPs
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Design and Synthesis of Aspirin-chalcone Mimic Conjugates as Potential Anticancer Agents Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-09 Reham A. Mohamed-Ezzat, Aladdin M. Srour
Background: Extensive research has been conducted on aspirin, a widely recognized NSAID medication, regarding its potential as an anticancer agent. Studies have revealed its ability to trigger cell death in different types of cancer cells. Methods: A set of aspirin-chalcone mimic conjugates 5a-k and 6a-d utilizing the freshly prepared acid chloride of aspirin moiety has been designed and synthesized
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Design, Synthesis, and In vitro Anti-cervical Cancer Activity of a Novel MDM2-p53 Inhibitor Based on a Chalcone Scaffold Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-09 Yusupuwajimu Alimujiang, Aikebaier Maimaiti, Mourboul Ablise, Zheng Yang, Zhengye Liu, Yu Wang, Zuohelaguli Mutalipu, Tong Yan
Objective: Several novel fluorinated chalcone derivatives were synthesized, and their in vitro anticervical cancer activity and mechanism of action were investigated using the parent nucleus of licorice chalcone as the lead compound backbone and MDM2-p53 as the target. Methods: In this study, 16 novel chalcone derivatives (3a–3r) were designed and synthesized by molecular docking technology based on
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Design, Synthesis and Anti-cancer Evaluation of Nitrogen-containing Derivatives of 30-Carboxyl of Gambogic Acid Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-09 Hong Li, Huiping Lin, Jiajun Li, Kaixin Chen, Zanhong Chen, Jianye Zhang, Yan Huang, Xin Zhao, Huihui Ti, Yiwen Tao
Background: Gambogic acid (GA) is a natural product from the resin of the Garcinia species, which showed significant activity in the induction of apoptosis. It can be one promising lead compound for the design and synthesis of new anticancer drugs. Objective: The objective of the current study is to design novel nitrogen-contained GA derivatives with better anti-cancer activities and study the effect
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Combination of Ethacrynic Acid and ATRA Triggers Differentiation and/or Apoptosis of Acute Myeloid Leukemia Cells through ROS Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-09 Lu Li, Hui-Min Xi, Hao Lu, Xun Cai
Background and objective: All-trans retinoic acid (ATRA), an effective differentiation inducer, has been applied clinically to treat acute promyelocytic leukemia (APL). Unfortunately, it is not as potent in other kinds of acute myeloid leukemia (AML). Ethacrynic acid (EA), a classical powerful diuretic, can increase reactive oxygen species (ROS) contents, which can assist ATRA in inducing differentiation
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Dexamethasone Suppresses IL-33-exacerbated Malignant Phenotype of U87MG Glioblastoma Cells via NF-κB and MAPK Signaling Pathways Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-09 Jie Ai, Yinhua Weng, Liyan Jiang, Chao Liu, Hongbo Liu, Huoying Chen
Background: Interleukin (IL)-33 is highly expressed in glioblastoma (GBM) and promotes tumor progression. Targeting IL-33 may be an effective strategy for the treatment of GBM. Dexamethasone (DEX) is a controversial drug routinely used clinically in GBM therapy. Whether DEX has an effect on IL-33 is unknown. This study aimed to investigate the effect of DEX on IL-33 and the molecular mechanisms involved
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JHD205, A Novel Abemaciclib Derivative, Exerts Antitumor Effects on Breast Cancer by CDK4/6 Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-08 Jing Ji, Jingting Qin, Xiaoshuo Wang, Mingxiao Lv, Xiao Hou, Aixin Jing, Jiaojiao Zhou, Lingyi Zuo, Wenwen Liu, Jing Feng, Qilan Qian, Yuanyuan Liu, Xiujun Wang, Bin Liu
Background: Efficient targeted molecular therapeutics are needed for the treatment of triple-negative breast cancer (TNBC), a highly invasive and difficult-to-treat form of breast cancer associated with a poor prognosis. Objectives: This study aims to evaluate the potential of selective CDK4/6 inhibitors as a therapeutic option for TNBC by impairing the cell cycle G1 phase through the inhibition of
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Cryptolepine Analog Exhibits Antitumor Activity against Ehrlich Ascites Carcinoma Cells in Mice via Targeting Cell Growth, Oxidative Stress, and PTEN/Akt/mTOR Signaling Pathway Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-04 Bishoy El-Aarag, Eman S. Shalaan, Abdullah A.S. Ahmed, Ibrahim El Tantawy El Sayed, Wafaa M. Ibrahim
Background: The efficacy of chemotherapy continues to be limited due to associated toxicity and chemoresistance. Thus, synthesizing and investigating novel agents for cancer treatment that could potentially eliminate such limitations is imperative. Objective: The current study aims to explore the anticancer potency of cryptolepine (CPE) analog on Ehrlich ascites carcinoma cells (EACs) in mice. Methods:
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Identification of Novel EGFR Inhibitors for the Targeted Therapy of Colorectal Cancer Using Pharmacophore Modelling, Docking, Molecular Dynamic Simulation and Biological Activity Predictionn Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2024-01-03 Amrutha Krishnan K, Sudha George Valavi, Amitha Joy
Background: Colorectal cancer (CRC) is considered the second deadliest cancer in the world. One of the reasons for the occurrence of this cancer is the deregulation of the Epidermal Growth Factor Receptor (EGFR), which plays a critical role in regulating cell division, persistence, differentiation, and migration. The overexpression of the EGFR protein leads to its dysregulation and causes CRC. Objective:
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Modulation of Caco-2 Colon Cancer Cell Viability and CYP2W1 Gene Expression by Hesperidin-treated Lacticaseibacillus rhamnosus GG (LGG) Cell-free Supernatants Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-12-07 Merve Akkulak, Emre Evin, Ozlem Durukan, Hasan Ufuk Celebioglu, Orhan Adali
Background and Objective: Ensuring colon homeostasis is of significant influence on colon cancer and delicate balance is maintained by a healthy human gut microbiota. Probiotics can modulate the diversity of the gut microbiome and prevent colon cancer. Metabolites/byproducts generated by microbial metabolism significantly impact the healthy colonic environment. Hesperidin is a polyphenolic plant compound
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Antitumor Activity of a Lectin Purified from Punica granatum Pulps against Ehrlich Ascites Carcinoma (EAC) Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-30 Md Nurujjaman, Tanjila Mashhoor, Tasfik Ul Haque Pronoy, Abdul Auwal, Md Robiul Hasan, Shaikh Shohidul Islam, Imtiaj Hasan, A.K.M. Asaduzzaman, Md Belal Uddin, Syed Rashel Kabir, Farhadul Islam
Background: Lectins are carbohydrate-binding proteins with various pharmacological activities, such as antimicrobial, antidiabetic, antioxidant, and anticancer. Punica granatum fruit extract has traditional uses, however, the anti-cancer activity of purified lectin isolated from P. granatum pulp is yet to be reported. Objective: The goals of this study are purification, characterization of the lectin
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Bunium persicum Seeds Extract in Combination with Vincristine Mediates Apoptosis in MCF-7 Cells through Regulation of Involved Genes and Proteins Expression Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-30 Mohammad Rasoul Samandari-Bahraseman, Ahmad Ismaili, Saeed Esmaeili-Mahani, Esmaeil Ebrahimie, Evelin Loit
Background: Bunium persicum seeds, a member of the Apiaceae family, have historically been consumed as part of the Iranian diet. Objective: While many of this herb's biological properties have been fully investigated, there is currently no reliable information about its anticancer/cytotoxic properties. Methods: Herein, we first determined the major bioactive compounds of B. persicum seed extract (BPSE)
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An Active Compound from the Pyrazine Family Induces Apoptosis by Targeting the Bax/Bcl2 and Survivin Expression in Chronic Myeloid Leukemia K562 Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-30 Saeedeh Rostampour, Farhad Eslami, Esmaeil Babaei, Hossein Mostafavi, Majid Mahdavi
Background: It has been established that pyrazine derivatives, which have widespread bioactivities, can effectively treat cancer. Objectives: In this study, we investigated the effects of 2-methoxy-5-(oxiran-2-ylmethyl) phenyl pyrazine-2- carboxylate (2-mOPP), a new pyrazine derivative, on proliferation, viability, and apoptosis induction in human leukemia K562 cells. Methods: For this purpose, the
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Overview of the New Bioactive Heterocycles as Targeting Topoisomerase Inhibitors Useful Against Colon Cancer Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-30 Mirelly Barbosa Santos, Misael de Azevedo Teotônio Cavalcanti, Yvnni Maria Sales de Medeiros e Silva, Igor José dos Santos Nascimento, Ricardo Olimpio de Moura
Colorectal cancer (CRC) is the third most common cancer globally, with high mortality. Metastatic CRC is incurable in most cases, and multiple drug therapy can increase patients' life expectancy by 2 to 3 years. Efforts are being made to understand the relationship between topoisomerase enzymes and colorectal cancer. Some studies have shown that higher expression of these enzymes is correlated to a
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A Comprehensive Review on Nanoparticles as a Targeted Delivery System for the Treatment of Lung Cancer Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-27 Twinkle Gupta, Avinash Varanwal, Priyanshu Nema, Sakshi Soni, Arun Kumar Iyer, Ratnesh Das, Vandana Soni, Sushil Kumar Kashaw
The second most common type of cancer is lung cancer, impacting the human population. Lung cancer is treated with a number of surgical and non-surgical therapies, including radiation, chemotherapy, and photodynamic treatment. However, the bulk of these procedures are costly, difficult, and hostile to patients. Chemotherapy is distinguished by inadequate tumour targeting, low drug solubility, and insufficient
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Anticancer Potential of a synthetic quinoline, 9IV-c, by Inducing Apoptosis in A549 Cell and In vivo BALB/c Mice Models Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-24 Salimeh Mirzaei, Farhad Eisvand, Mojgan Nejabat, Razieh Ghodsi, Farzin Hadizadeh
Background: In a previous work from the author of this study, the compound of 9IV-c, ((E)-2-(3,4- dimethoxystyryl)-6,7,8-trimethoxy-N-(3,4,5-trimethoxyphenyl)quinoline-4-amine) was synthesized, and the effects of potent activity on the multiple human tumor cell lines were evaluated considering the spindle formation together with the microtubule network. Methods: Accordingly, cytotoxic activity, apoptotic
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Novel Anti-tumor Strategy for Breast Cancer: Synergistic Role of Oleuropein with Paclitaxel Therapeutic in MCF-7 Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-22 Gamze Yılmaz, Filiz Özdemir
Background: The side effects of conventional therapeutics pose a problem for cancer treatment. Recently, combination treatments with natural compounds have attracted attention regarding limiting the side effects of treatment. Oleuropein is a natural polyphenol in olives that has antioxidant and anticancer effects. Objectives: This study aimed to investigate the oxidative stress effect of a combination
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CRD-BP as a Tumor Marker of Colorectal Cancer Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-21 Fen-Xu, Liang-Hong Jiang, Chen-Fu, Wei-Wei Feng, Chang-Jiang Zhou
The National Cancer Center published a comparative report on cancer data between China and the United States in the Chinese Medical Journal, which shows that colorectal cancer (CRC) ranks second in China and fourth in the United States. It is worth noting that since 2000, the case fatality rate of CRC in China has skyrocketed, while the United States has gradually declined. Finding tumor markers with
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Matrix Metalloproteinases in Oral Cancer Pathogenesis and their Use in Therapy Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-20 Stuti Maurya, Divya Prasad, Sayali Mukherjee
Matrix metalloproteinases (MMPs) are proteolytic enzymes that aid in extracellular matrix (ECM) remodeling. MMPs destroy the extracellular matrix, causing tumor growth and metastasis. MMPs are involved in the spread and metastasis of oral cancer. High levels of MMPs and oral squamous cell carcinoma have been linked to cancer prognosis. Modern medicine aims to prevent the illness from spreading through
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An Outlook of the Structure Activity Relationship (SAR) of Naphthalimide Derivatives as Anticancer Agents Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-16 Aeyaz Ahmad Bhat
The efficacy of drugs against cancer in clinical settings may be limited due to pharmacokinetic issues, side effects and the emergence of drug resistance. However, a class of anticancer drugs known as naphthalimides have proven to be very effective. These derivatives have demonstrated to be effective in treating different types of cancers and exhibit strong DNA binding affinity. The anticancer properties
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Anti-lung Cancer Activity of Synthesized Substituted 1,4-Benzothiazines: An Insight from Molecular Docking and Experimental Studies Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-14 Andleeb Amin, Zubaid-Ul Khazir, Arfa Ji, Basharat Bhat, Dar Murtaza, Aaqib A. Hurrah, Imtiyaz A Bhat, Shaheena Parveen, Syed Nisar, Praveen Kumar Sharma
Background:: Thiazine, a 6-membered distinctive heterocyclic motif with sulfur and nitrogen atoms, is one of the heterocyclic compounds that functions as a core scaffold in a number of medicinally significant molecules. Small thiazine-based compounds may operate simultaneously on numerous therapeutic targets and by employing a variety of methods to halt the development, proliferation, and vasculature
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Chalcones as Potential Cyclooxygenase-2 Inhibitors: A Review Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-13 Mohammad Mahboubi-Rabbani, Rosa Zarei, Mehdi Baradaran, Maryam Bayanati, Afshin Zarghi
Cyclooxygenases (COXs) play a pivotal role in inflammation, a complex phenomenon required in human defense, but also involved in the emergence of insidious human disorders. Currently-used COX-1 inhibitors (Non-Steroidal Anti-Inflammatory Drugs-NSAIDs), as the most frequent choices for the treatment of chronic inflammatory diseases, have been identified to be associated with a variety of adverse drug
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Exploring the Synergistic Effect of Sildenafil and Green Tea Polyphenols on Breast Cancer Stem Cell-like Cells and their Parental Cells: A Potential Novel Therapeutic Approach Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-10 Marzie Salari Sharif, Habibeh Sadat Mohseni, Mahnaz Khanavi, Shima Ghadami, Emad Jafarzadeh, Shohreh Tavajohi, Shima Aliebrahimi, Seyed Nasser Ostad
Background: Many cancer studies have intensely focused on the role of diet, among other factors involved in cancer establishment. The positive effect of green tea polyphenols (GTP) on controlling breast cancer cells has been reported in several studies. Cancer stem cell-like cells (CSC-LCs) possessing self-renewal, metastatic, and drug-resistant capacities are considered prominent therapeutic targets
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Anticancer Potential of Novel Cinnamoyl Derivatives against U87MG and SHSY-5Y Cell Lines Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-10 Niki Gouleni, Annalisa Di Rienzo, Sena Oner, Ceren Karagöz, Mehmet Enes Arslan, Adil Mardinoglu, Hasan Turkez, Antonio Di Stefano, Stamatia Vassiliou, Ivana Cacciatore
Background: Glioblastoma multiforme (GBM) is probably the most malignant and aggressive brain tumor belonging to the class of astrocytomas. The considerable aggressiveness and high malignancy of GBM make it a tumor that is difficult to treat. Here, we report the synthesis and biological evaluation of eighteen novel cinnamoyl derivatives (3a-i and 4a-i) to obtain more effective antitumor agents against
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Tumor-associated Macrophages Mediate Gefitinib Resistance in Lung Cancer through HGF/c-met Signaling Pathway Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-08 Xiali Tang, Yu Chen, Demin Jiao, Xiang Liu, Jun Chen, Yongyang Liu, Chunyan Jiang, Qingyong Chen
Background: The biological behavior of cells changes after they develop drug resistance, and the degree of resistance will be affected by the tumor microenvironment. In this study, we aimed to study the effects of M2 macrophages on gefitinib resistance. Method: We polarized THP-1 cells into M0 and M2 macrophages, and conducted various experiments to investigate the effects of M2 macrophages on gefitinib
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Preparation of Lycium barbarum Active Glycopeptide and Investigation of Its Apoptotic Effects on Melanoma Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-08 Jinghua Qi, Xingli Qi, Hongyuan chen, Wen Rui
Introduction: The increasing number of studies have shown that Lycium barbarum polysaccharides possess anti-tumor effects. However, the determination of the active ingredients and their mechanism against melanoma inhibition are still unknown. Method: In this study, we aimed to investigate the mechanisms of action of Lycium barbarum active glycopeptide (LBAG) on melanoma. LBAG was extracted and isolated
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Curcumin Suppresses M2 Macrophage-derived Paclitaxel Chemoresistance through Inhibition of PI3K-AKT/STAT3 Signaling Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-08 Bhawna Deswal, Urmi Bagchi, Sonia Kapoor
Background: Breast cancer is the leading cancer in women worldwide. The development of chemoresistance that leads to recurrence and mortality remains a major concern. M2-type tumor-associated macrophages (TAMs), present in the breast tumor microenvironment, secrete various cytokines and growth factors that induce chemoresistance. Curcumin, isolated from Curcuma longa, is known to sensitize cancer cells
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Osmundacetone Inhibits Angiogenesis of Infantile Hemangiomas through Inducing Caspases and Reducing VEGFR2/MMP9 Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-08 Chen Ke, Changhan Chen, Ming Yang, Hao Chen, Liqun Li, Youhui Ke
Aim: This study aims to explore the potential of Osmundacetone (OSC) as a new treatment for infantile hemangiomas (IH), the most common benign tumors in infancy. Currently, propranolol serves as the primary treatment for IH, but its effectiveness is limited, and it poses challenges of drug resistance and side effects. Therefore, there is a pressing need to identify alternative therapies for IH. Methods:
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Antitumoral Potential of Artepillin C, a Compound Derived from Brazilian Propolis, against Breast Cancer Cell Lines Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-08 Lyvia Eloiza de Freitas Meirelles, Analine Rosa Barquez de Assis Carvalho, Gabrielle Marconi Zago Ferreira Damke, Raquel Pantarotto Souza, Edilson Damke, Patrícia de Souza Bonfim-Mendonça, Djaceli Sampaio de Oliveira Dembogurski, Denise Brentan da Silva, Marcia Edilaine Lopes Consolaro, Vania Ramos Sela da Silva
Background: Breast cancer is the most commonly diagnosed cancer among women worldwide with limited treatment options. Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) is one of the main constituents of Brazilian propolis presenting different activities, including antitumoral effects against various types of cancer. Objective: We evaluated the antitumoral potential and mechanisms of action of artepillin
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Karanjin, A Promising Bioactive Compound Possessing Anti-cancer Activity against Experimental Model of Non-small Cell Lung Cancer Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-08 Gourav Kumar, Dev Mani Pandey, Manik Ghosh, Stefano Dall'Acqua, Rashmi Gupta, Nishi Prakash Tiwari, Usman Mohd Siddique, Leena Vishwakarma, Sunil Kant Guleri, Uma Ranjan Lal, Supriya Dubey
Aims:: The aim of this study is to isolate the Millettia pinnata (Karanj) leaf extract for pure compound with anticancer properties and to study the molecular target of the isolates in non-small cell lung cancer cell lines. background: In our earlier research Millettia pinnata leaf extract has demonstrated potential anticancer activities. Thus, in pursuit of the bioactive compound most potential active
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Coumarin-derived Hydroxamic Acids as Histone Deacetylase Inhibitors: A Review of Anti-cancer Activities Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-07 Nguyen Quang Khai, Tran Khac Vu
Since coumarin and hydroxamic acid compounds are well-known in medicinal chemistry, a variety of their derivatives have been highlighted due to their potential uses for plentiful treatments. Different compounds of their derivatives acting through diverse activities, such as anti-tumor, anti-cancer, anti-inflammation, and histone deacetylase inhibition, have been comprehensively investigated by many
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Research on the Inhibitory Effect of Doxorubicin-loaded Liposomes Targeting GFAP for Glioma Cells Anti Cancer Agents Med. Chem. (IF 2.8) Pub Date : 2023-11-02 Qifeng Li, Jiaming Xu
Background: Glioma is the most common and devastating brain tumor. In recent years, doxorubicin (DOX) is one of the drugs used in the treatment of gliomas, but it has side effects and poor clinical outcomes. Therefore, the delivery of drugs to the tumor site by targeted transport is a new approach to tumor treatment. Objective: This study focuses on the anti-tumor effects of GFAP-modified drug-carrying