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Pentacyclic triterpene acid conjugated with mitochondria-targeting cation F16: Synthesis and evaluation of cytotoxic activities Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-25 Anna Yu. Spivak, Darya A. Nedopekina, Rinat R. Gubaidullin, Eldar V. Davletshin, Adis A. Tukhbatullin, Vladimir A. D’yakonov, Milyausha M. Yunusbaeva, Lilya U. Dzhemileva, Usein M. Dzhemilev
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Adenosine receptors as promising targets for the management of ocular diseases Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-25 Eleonora Spinozzi, Cecilia Baldassarri, Laura Acquaticci, Fabio Del Bello, Mario Grifantini, Loredana Cappellacci, Petrelli Riccardo
The ocular drug discovery arena has undergone a significant improvement in the last few years culminating in the FDA approvals of 8 new drugs. However, despite a large number of drugs, generics, and combination products available, it remains an urgent need to find breakthrough strategies and therapies for tackling ocular diseases. Targeting the adenosinergic system may represent an innovative strategy
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Synthesis and in vitro evaluation of triphenylphosphonium derivatives of acetylsalicylic and salicylic acids: structure-dependent interactions with cancer cells, bacteria, and mitochondria Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-21 Olga V. Tsepaeva, Taliya I. Salikhova, Leysan R. Grigor’eva, Denis V. Ponomaryov, Trinh Dang, Rezeda A. Ishkaeva, Timur I. Abdullin, Andrey V. Nemtarev, Vladimir F. Mironov
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Divalent tranylcypromine derivative as lysine-specific demethylase 1 inhibitor Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-20 Yin Sun, Na Li, Mingbo Su, Xiaowen Wang, Dongmei Zhao, Bing Xiong, Yubo Zhou, Tongchao Liu, Yue-Lei Chen
Tranylcypromine (TCP) is a useful pharmacophore for lysine-specific demethylase 1 (LSD1) inhibitors. Based on the mode of action (MOA) of TCP and structure of LSD1, divalent TCP derivatives with aliphatic and benzylic linkers were designed, synthesized, and evaluated for their LSD1 inhibitory activity, MV4-11 antiproliferative activity, and CD86 mRNA expression enhancement. All ten new compounds showed
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Tuberculosis: current scenario, drug targets, and future prospects Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-20 Priyanka Bose, Amit K. Harit, Ratnesh Das, Samaresh Sau, Arun K. Iyer, Sushil K. Kashaw
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Novel 1-methoxyindole- and 2-alkoxyindole-based chalcones: design, synthesis, characterization, antiproliferative activity and DNA, BSA binding interactions Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-16 Zuzana Kudličková, Peter Takáč, Danica Sabolová, Mária Vilková, Matej Baláž, Tibor Béres, Ján Mojžiš
Indole-based chalcones have been identified as interesting compounds with anticancer properties. In the present study, we report the synthesis and evaluation of new 1-methoxyindole and 2-alkoxyindole chalcone hybrids as antiproliferative agents active against colorectal carcinoma cell line. Among the 19 investigated molecules, four inhibit the proliferation of colorectal cancer cells HCT-116 with IC50
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γ- and δ-lactones as fumarate esters analogues and their neuroprotective effects Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-16 Francesca Cateni, Patrizia Nitti, Sara Drioli, Giuseppe Procida, Renzo Menegazzi, Maurizio Romano
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Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-15 Seyedeh Roya Alizadeh, Seyedeh Mahdieh Hashemi
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Sulfur-containing therapeutics in the treatment of Alzheimer’s disease Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-15 Haizhou Zhu, Venkateshwara Dronamraju, Wei Xie, Swati S. More
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Anti-inflammatory scalarane-type sesterterpenes, erectascalaranes A–B, from the marine sponge Hyrtios erectus attenuate pro-inflammatory cyclooxygenase-2 and 5-lipoxygenase Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-15 Prima Francis, Kajal Chakraborty
Chemical investigation of demosponge Hyrtios erectus (family Thorectidae) resulted in the identification of two scalarane-type sesterterpenes, erectascalaranes A–B, which were characterized as 3-((but-35-enyloxy)methyl)-icosahydro-11-hydroxy-4,4,8,10,13-pentamethyl-20-oxochryseno[2,1-c]furan-12-yl acetate (erectascalarane A) and 3-((but-35-enyloxy)methyl)-hexadecahydro-11-hydroxy-4,4,8,10,13-pentamethylchryseno[2
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Design and synthesis of newer N-benzimidazol-2yl benzamide analogues as allosteric activators of human glucokinase Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-13 Sukhbir Singh, Sandeep Arora, Ervon Dhalio, Neelam Sharma, Kunal Arora, Ajmer Singh Grewal
Allosteric activators of human glucokinase (GK) had revealed significant hypoglycemic effects for therapy of type-2 diabetes (T2D) in animal as well as human models. Some newer N-benzimidazol-2yl substituted benzamide analogues were prepared and assessed for activation of GK accompanied by molecular docking investigations for predicting the bonding interactions of these derivatives with the residues
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8-cyanobenzothiazinone analogs with potent antitubercular activity Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-13 Gang Zhang, Li Sheng, Pooja Hegde, Yan Li, Courtney C. Aldrich
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Benzopyrylium salts as new anticancer, antibacterial, and antioxidant agents Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-13 Swayamsiddha Kar, Abdul Akhir, Sidharth Chopra, Shinya Ohki, Balasubramanyam Karanam, Nageswara Rao Golakoti
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Structural insights of sulfonamide-based NLRP3 inflammasome inhibitors: design, synthesis, and biological characterization Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-13 Yiming Xu, Matteo Scipioni, Hallie Blevins, Shijun Zhang
NLRP3 inflammasome has recently attracted much attention as a potentially druggable target to develop potential therapeutics for inflammatory and neurodegenerative disorders. In our continuing studies, structure–activity relationship studies were conducted based on a newly identified NLRP3 inhibitor, YQ-II-128, from our laboratory to understand the structural features and improve aqueous solubility
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N -(2,3,4,6-tetra- O -acetyl-β- d -glucopyranosyl)thiosemicarbazones of 6-alkoxy-2-oxo-2 H -chromene-4-carbaldehydes: synthesis, evaluation of their antibacterial, anti-MRSA, antifungal activity, and docking study Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-13 Vu Ngoc Toan, Nguyen Dinh Thanh, Vu Hong Khuyen, Luu Thi Cam Tu, Nguyen Minh Tri, Nguyen Thi Thu Huong
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Design, synthesis, docking study and urease inhibitory activity evaluation of novel 2-((5-amino-1,3,4-thiadiazol-2-yl)thio)- N -arylacetamide derivatives Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-12 Mohammad Nazari Montazer, Mehdi Asadi, Saeed Bahadorikhalili, Faezeh Sadat Hosseini, Arash Amanlou, Mahmood Biglar, Massoud Amanlou
In this paper, novel 2-((5-amino-1,3,4-thiadiazol-2-yl)thio)-N-arylacetamide derivatives (7a–l) are designed, synthesized, and evaluated in vitro for their urease inhibitor activities. The compounds are synthesized efficiently in three steps in high isolated yields from amines, 2-chloroacetyl chloride, hydrazinecarbothioamide, and carbon disulfide. The molecular docking simulation were performed using
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Development of structure-based pharmacophore to target the β-catenin-TCF protein–protein interaction Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-12 Piyusha P. Pagare, Andrew Morris, Jiong Li, Yan Zhang
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Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-12 Yanzhao Xu, Na Qi, Hui Wen, Gang Zhang, Yuchen Wang, Huaqing Cui
Herein we report our investigation concerning the development of Human neutrophil elastase (hNE) inhibitors for the treatment of Acute Respiratory Distress Syndrome (ARDS). Various benzenesulfonic acid derived compounds were synthesized and evaluated as competitive inhibitors of hNE. Biological screening revealed that compound 4f shows moderate inhibitory activity (IC50 = 35.2 μM) against hNE. Compound
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DDR1 and DDR2: a review on signaling pathway and small molecule inhibitors as an anticancer agent Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-12 Gurubasavaraja Swamy Purawarga Matada, Arka Das, Prasad Sanjay Dhiwar, Abhishek Ghara
Cancer is the 2nd most fatal disease around the globe. Various receptors have been showed to be overexpressed and/or mutated in numerous cancers. Discoidin domain receptors 1 (DDR1) and 2 (DDR2) are one of the novel receptor tyrosine kinases (RTKs), which have been proved to regulate various cellular signaling pathways, cell proliferation, adhesion, migration, matrix remodeling, and dysregulation of
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Synthesis of 4-oxotetrahydropyrimidine-1(2H)-carboxamides derivatives as capsid assembly modulators of hepatitis B virus Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-11 Nicky Hwang, Haiqun Ban, Junjun Chen, Julia Ma, Hui Liu, Patrick Lam, John Kulp, Stephan Menne, Jinhong Chang, Ju-Tao Guo, Yanming Du
We report herein the synthesis and evaluation of phenyl ureas derived from 4-oxotetrahydropyrimidine as novel capsid assembly modulators of hepatitis B virus (HBV). Among the derivatives, compound 27 (58031) and several analogs showed an activity of submicromolar EC50 against HBV and low cytotoxicities (>50 μM). Structure–activity relationship studies revealed a tolerance for an additional group at
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Synthesis of macrocyclic α -ketoamide as a selective and reversible immunoproteasome inhibitor Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-11 Rui Ding, Daniel J. Wilson, Liqiang Chen
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α-Glucosidase and α-amylase inhibition, molecular modeling and pharmacokinetic studies of new quinazolinone-1,2,3-triazole-acetamide derivatives Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-09 Ali Yavari, Maryam Mohammadi-Khanaposhtani, Shahram Moradi, Saeed Bahadorikhalili, Roghayeh Pourbagher, Nasrin Jafari, Mohammad Ali Faramarzi, Ebrahim Zabihi, Mohammad Mahdavi, Mahmood Biglar, Bagher Larijani, Haleh Hamedifar, Mir Hamed Hajimiri
In this study, a new series of quinazolinone-1,2,3-triazole-acetamide hybrids 8a–m, using by molecular hybridization of the potent α-glucosidase inhibitor pharmacophores, was designed and evaluated against carbohydrate-hydrolyzing enzymes α-glucosidase and α-amylase. All the synthesized compounds with IC50 values in the range of 45.3 ± 1.4 µM to 195.5 ± 4.7 µM were significantly more potent than standard
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Anti-HCMV activity by an irreversible p97 inhibitor LC-1310 Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-09 Yan Wang, Ruben Soto-Acosta, Rui Ding, Liqiang Chen, Robert J. Geraghty
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New amino acid clubbed Schiff bases inhibit carbonic anhydrase II, α-glucosidase, and urease enzymes: in silico and in vitro Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-09 Kashif Rafiq, Majid Khan, Niaz Muhammed, Ajmal Khan, Najeeb Ur Rehman, Balqees Essa Mohammad Al-Yahyaei, Mohammed Khiat, Sobia Ahsan Halim, Zarbad Shah, Rene Csuk, Ahmed Al-Harrasi
Combating pathological conditions related to hyperactivity of enzymes remains a formidable challenge for health. Small molecules therapy constitutes one of the means to circumvent the medical disorders resulting from enzyme hyperactivity. In this regard, we have synthesized structurally diverse amino acid hybrid Schiff bases (5a–5l and 10a–10k) and evaluated them for carbonic anhydrase II, α-glucosidase
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Molecular hybridization based design and synthesis of new benzo[5,6]chromeno[2,3-b]-quinolin-13(14H)-one analogs as cholinesterase inhibitors Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-08 Baswaraju Macha, Ravindra Kulkarni, Chandrakant Bagul, Anil Kumar Garige, Raghuramrao Akkinepally, Achaiah Garlapati
A Series of new tacrine analogs were designed, synthesized, characterized by respective spectral data and evaluated for cholinesterase inhibitory activity to be useful in Alzheimer’s disease. Most of the synthesized compounds showed good in vitro inhibitory activities toward acetyl cholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. Among the compounds, 6i, 6o and 6r with increased saturated
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Facile one-pot sequential synthesis of novel diaryl urea derivatives and evaluation of their in vitro cytotoxicity on adenocarcinoma cells Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-07 Fereshteh Azimian, Maryam Hamzeh-Mivehroud, Javid Shahbazi Mojarrad, Salar Hemmati, Siavoush Dastmalchi
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Theoretical and experimental verification of molecular properties of novel benzamide derivatives using computational platforms and in vitro antibacterial activity Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-05 Poonam M. Wanjari, Santosh N. Mokale, Avinash V. Bharati, Vishwas N. Ingle
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Phosphoramidate conjugates of 3′-azido-3′-deoxythymidine glycerolipid derivatives and amino acid esters: synthesis and anti-HIV activity Med. Chem. Res. (IF 1.783) Pub Date : 2021-01-05 Elizaveta S. Darnotuk, Andrei E. Siniavin, Nikolay V. Shulga, Eduard V. Karamov, Natal’ya S. Shastina
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RF-3192C and other polyketides from the marine endophytic Aspergillus niger ASSB4: structure assignment and bioactivity investigation Med. Chem. Res. (IF 1.783) Pub Date : 2020-12-01 Manar M, Mahmoud, Ahmed S, Abdel-Razek, Abdelaaty Hamed, Hesham S. M, Soliman, Larissa V, Ponomareva, Jon S, Thorson, Khaled A, Shaaban, Mohamed Shaaban
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Design and synthesis of nature-inspired chromenopyrroles as potential modulators of mitochondrial metabolism Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-30 Paul Schilf, Vunnam Srinivasulu, Maria L. Bolognesi, Saleh Ibrahim, Amin F. Majdalawieh, Imad A. Abu-Yousef, Hany A. Omar, Raafat ElAwady, Taleb H. Al-Tel
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Indazole scaffold: a generalist for marketed and clinical drugs Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-25 Yaquan Cao, Chunying Luo, Pu Yang, Pan Li, Chunli Wu
More and more attention has been paid to the structurally diverse indazole analogs in recent years which are widely present in numerous commercially available drugs. Indazole-containing derivatives are endowed with a broad range of biological properties, such as anti-inflammatory, antibacterial, anti-HIV, antiarrhythmics, antifungal and antitumor activities. This review is a guide for pharmacologists
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Thiazole-based and thiazolidine-based protein tyrosine phosphatase 1B inhibitors as potential anti-diabetes agents Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-25 Kexin Chen, Xu Yao, Ting Tang, Li-Mei Chen, Can Xiao, Jing-Yi Wang, Hong-Fei Chen, Zhong-Xing Jiang, Yi Liu, Xing Zheng
As a disease closely related to the metabolic syndrome, diabetes has become a public health issue that severely affects many people’s quality of life. The search for novel anti-diabetic agents remains the cornerstone to control this challenging disease. Protein tyrosine phosphatase 1B (PTP1B), a negative regulator of insulin and leptin signaling pathways, has turned out to be a potential target of
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Design, synthesis and biological evaluation of Schiff’s base derivatives as multifunctional agents for the treatment of Alzheimer’s disease Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-25 Jian Shi, Yi Zhou, Keren Wang, Qinge Ma, Rongrui Wei, Qingfeng Li, Yiyang Zhao, Zhanpin Qiao, Shuang Liu, Yumin Leng, Wenmin Liu, Zhipei Sang
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Antioxidant and acetylcholinesterase inhibition activity of aliphatic and aromatic edaravone derivatives Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-23 Victor Wagner Barajas-Carrillo, Arturo Estolano-Cobián, Laura Díaz-Rubio, Rocío Rosario Ayllón-Gutiérrez, Ricardo Salazar-Aranda, Raúl Díaz-Molina, Víctor García-González, Horacio Almanza-Reyes, Ignacio A. Rivero, Joaquín G. Marrero, Iván Córdova-Guerrero
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Synthesis and biological evaluation of novel N -substituted nipecotic acid derivatives with tricyclic cage structures in the lipophilic domain as GABA uptake inhibitors Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-22 Heinrich-Karl A. Rudy, Georg Höfner, Klaus T. Wanner
A new class of GABA reuptake inhibitors with sterically demanding, highly rigid tricyclic cage structures as the lipophilic domain was synthesized and investigated in regard to their biological activity at the murine GABA transporters (mGAT1–mGAT4). The construction of these compounds, consisting of nipecotic acid, a symmetric tricyclic amine, and a plain hydrocarbon linker connecting the two subunits
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Biological targets of 92 alkaloids isolated from Papaver genus: a perspective based on in silico predictions Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-21 Omer Bayazeid, Funda N. Yalçın
With its high level of phytochemical and botanical variability, Papaver genus contains several species with many subspecies yielding more than 170 alkaloids. Papaver species have been used as sedative, hypnotic, analgesic, and antidepressant. The aim of this study is to shed light on the structure–activity relationship of alkaloids isolated from Papaver genus. All alkaloids isolated from Papaver genus
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Simple methods of modification of daunorubicin on the daunosamine nitrogen atom Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-20 Valery K. Brel, Aleksandra A. Moiseeva, Oleg I. Artyushin, Lada V. Anikina, Zinaida S. Klemenkova
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4-benzylideneisoquinoline-1,3( 2H , 4H )-diones as tyrosyl DNA phosphodiesterase 2 (TDP2) inhibitors Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-19 Sameera Senaweera, Tianyu He, Haixi Cui, Hideki Aihara, Zhengqiang Wang
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Tankyrase inhibitors: emerging and promising therapeutics for cancer treatment Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-17 Anu Verma, Ashwani Kumar, Arshiya Chugh, Sunil Kumar, Parvin Kumar
Cancer is a disease portrayed by the uncontrolled growth of irregular cells. Tankyrase, a member of poly(ADP-ribose)polymerase family, mediates Wnt signal transduction and has emerged as a new molecular target for the therapy of different kinds of cancer. Wnt/β-catenin signaling functions significantly in a wide scope of biological events, such as the upkeep of genomic stability, transcriptional control
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Design, synthesis, and evaluation of different scaffold derivatives against NS2B-NS3 protease of dengue virus Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-17 Lata R. Ganji, Lekha Gandhi, Venkataramana Musturi, Meena A. Kanyalkar
The number of deaths or critical health issues is a threat in the infection caused by Dengue virus, which complicates the situation, as only symptomatic treatment is the current solution. In this regard we have targeted the dengue protease NS2B-NS3 that is responsible for the replication. The series was designed with the help of molecular modeling approach using docking protocols. The series comprised
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Benzilydene and thiourea derivatives as new classes of carbonic anhydrase inhibitors: an in vitro and molecular docking study Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-17 Shama Qaiser, Mohammad S. Mubarak, Sajda Ashraf, Muhammad Saleem, Zaheer Ul-Haq, Muhammad Safdar, Abdur Rauf, Tareq Abu-Izneid, Malak I. Qadri, Aneela Maalik
Carbonic anhydrase-II (CA-II) catalyzes reversible hydration of carbon dioxide leading to the formation of bicarbonate and a proton. CA-II inhibitors act as biomarkers and therapeutic targets for various diseases such as epilepsy, glaucoma, leukemia, and cystic fibrosis. In the present work, a number of thiourea and benzylidene derivatives were evaluated as CA-II inhibitors. For this, detection of
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Potent antiproliferative active agents: novel bis Schiff bases and bis spiro β-lactams bearing isatin tethered with butylene and phenylene as spacer and DNA/BSA binding behavior as well as studying molecular docking Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-11 Mohammad Bashiri, Aliasghar Jarrahpour, S. Masoud Nabavizadeh, Somaye Karimian, Banafsheh Rastegari, Elahe Haddadi, Edward Turos
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Novel approach of multi-targeted thiazoles and thiazolidenes toward anti-inflammatory and anticancer therapy—dual inhibition of COX-2 and 5-LOX enzymes Med. Chem. Res. (IF 1.783) Pub Date : 2020-11-01 Jaismy Jacob P, Manju S L
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NF-κB regulation by bisbenzylisoquinoline alkaloids in human T cells: a structure–activity relationship study Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-19 Wencheng Xu, Shuhe Chen, Xiaoqin Wang, Junichi Kusano, Ryusei Yamamoto, Hiroto Matsuda, Yoshikazu Hara, Yoshiaki Fujii, Seiichi Hayashi, Sachiko Tanaka, Kentaro Sugiyama, Haruki Yamada, Toshihiko Hirano
Suppressive potencies of tetrandrine, isotetrandrine, fangchinoline, berbamine, dauricine, cepharanthine, and armepavine on expression and activation of NF-κB in MOLT-4 cells, MOLT-4/DNR cells, peripheral blood mononuclear cells (PBMCs) of healthy subjects and PBMCs of dialysis patients were compared. In MOLT-4 cells, the suppressive potencies evaluated by the IC50 values were isotetrandrine > cep
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Triphenylphosphonium conjugates of 1,2,3-triazolyl nucleoside analogues. Synthesis and cytotoxicity evaluation Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-29 Irina Yu. Strobykina, Olga V. Andreeva, Mayya G. Belenok, Marina N. Semenova, Victor V. Semenov, Roman N. Chuprov-Netochin, Anastasiya S. Sapunova, Alexandra D. Voloshina, Alexey B. Dobrynin, Vyacheslav E. Semenov, Vladimir E. Kataev
A series of triphenylphosphonium (TPP) conjugates of 1,2,3-triazolyl analogues of several pyrimidine nucleosides was synthesized and evaluated for the in vitro cytotoxicity against human cancer cell lines M-HeLa, MCF-7, PANC-1, PC-3, DU145, SKOV-3, A275, and normal human cell line WI-38. In these TPP-conjugates triphenylphosphonium cation was attached via a tetramethylene chain to the N-3 atom of the
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Functionalized imidazolium-based ionic liquids: biological activity evaluation, toxicity screening, spectroscopic, and molecular docking studies Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-23 Maria M. Trush, Ivan V. Semenyuta, Diana Hodyna, Alla D. Ocheretniuk, Sergey I. Vdovenko, Sergiy P. Rogalsky, Larisa E. Kalashnikova, Volodymyr Blagodatnyi, Oleksandr L. Kobzar, Larisa O. Metelytsia
A series of long-chain imidazolium-based ionic liquids (ILs) 1-dodecyl-3-methylimidazolium chloride (1), 1,3-bis(octyloxycarbonylmethyl)imidazolium chloride (2) and 1-dodecyloxycarbonylmethyl-3-methyloxycarbonylmethylimidazolium chloride (3), were synthesized and evaluated as antimicrobials against a wide range of bacteria and fungi. Toxicological risks of selected compounds were assessed using the
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Antifungal activity of aminoalcohols and diamines against dermatophytes and yeast Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-23 César A. Caneschi, Bruno A. de Oliveira, Angelina M. de Almeida, Renata P. do Carmo, Francislene J. Martins, Mauro V. de Almeida, Nádia R. B. Raposo
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Novel amide analogues of quinazoline carboxylate display selective antiproliferative activity and potent EGFR inhibition Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-19 Anjleena Malhotra, Ranju Bansal, Clarissa Esmeralda Halim, Celestial T. Yap, Gautam Sethi, Alan Prem Kumar, Mahendra Bishnoi, Kamalendra Yadav
In the present study, a novel series of quinazoline derivatives is developed for cancer therapy. All the synthesised analogues were evaluated against a panel of 60 human cancer cell lines for the antiproliferative activity. Significant and selective growth inhibition of several solid tumour cell lines such as NCI-H322M, NCI-H522 (non-small cell lung cancer), IGROV1, SK-OV-3 (ovarian cancer), TK-10
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Design, synthesis and biological evaluation of novel 1,5-disubstituted isatin derivatives as antitumor agents Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-23 Huijun Zhuo, Zhen Zhang, Yang Liu, Jingya Zhang, Guisen Zhao
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New Pt(II) complexes with 3 ’ -methyl tetrahydro-4 H -thiopyranspiro-5 ’ -hydantoin: synthesis, theoretical and cytotoxic investigation Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-30 Adriana Georgieva Bakalova, Rossen Todorov Buyukliev, Emilyia Demireva Cherneva
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Synthesis, biological evaluation and molecular docking studies of Combretastatin A-4 phosphoramidates as novel anticancer prodrugs Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-26 Shaowu Zhang, Tang Li, Wan Pang, Jingjing Wu, Fulong Wu, Yangyang Liu, Fanhong Wu
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Phytochemistry, pharmacology and medicinal uses of Cola (Malvaceae) family: a review Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-26 Abiche Ekalu, James D. Habila
Cola belongs to the family Malvaceae and contains 125 Cola plants. Among the Cola species, Cola acuminata and Cola nitida are the most studied for their pharmacology effects. Cola contains phytochemicals such as alkaloids, caffeine, theobromine, theophylline, quinic acid, chlorogenic acid, purine, (−)-epicatechin, (+)-catechin, sterols, anthraquinones, flavonoid glycosides, cardenolides, tannins, rostratanic
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Organotin (IV) complexes from Schiff bases ligands based on 2-amino-3-hydroxypyridine: synthesis, characterization, and cytotoxicity Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-22 José M. Galván-Hidalgo, Diana M. Roldán-Marchán, Arturo González-Hernández, Teresa Ramírez-Apan, Antonio Nieto-Camacho, Simón Hernández-Ortega, Elizabeth Gómez
A multicomponent reaction was used as a synthetic strategy to prepare organotin (IV) complexes, 2-amino-3-hydroxypyridine, saliciladehydes 5-R-substituted (H, CH3, OCH3, C(CH)3, F, Cl, Br, I, NO2), and dibutyltin(IV) oxide were used as starting materials. The complexes were analyzed by IR, UV–Visible, MS, NMR of 1H, 13C, 119Sn. The complex 3a was structurally identified by X-ray crystallography, which
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A convenient synthesis, reactions and biological evaluation of novel pyrazolo[3,4- b ]selenolo[3,2- e ]pyrazine heterocycles as potential anticancer and antimicrobial agents Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-22 Remon M. Zaki, Mokhtar A. Abdul-Malik, Saber H. Saber, Shaban M. Radwan, Adel M. Kamal El-Dean
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Synthesis of pyrazinamide analogues and their antitubercular bioactivity Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-23 First A. Wati, Prisna U. Adyarini, Sri Fatmawati, Mardi Santoso
The Yamaguchi reaction is widely and generally applied to synthesize esters and lactones. It involves 2,4,6-trichlorobenzoyl chloride as the Yamaguchi reagent, 4-dimethylaminopyridine, and triethylamine. Pyrazinamide is a crucial first-line drug for tuberculosis treatment, therefore their analogues are interesting in organic synthesis. In general, the synthesis pyrazinamide analogues involve reaction
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First in class ( S , E )-11-[2-(arylmethylene)hydrazono]-PBD analogs as selective CB2 modulators targeting neurodegenerative disorders Med. Chem. Res. (IF 1.783) Pub Date : 2020-10-04 David Mingle, Meirambek Ospanov, Mohamed O. Radwan, Nicole Ashpole, Masami Otsuka, Samir A. Ross, Larry A. Walker, Abbas G. Shilabin, Mohamed A. Ibrahim
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Synthesis of novel selenotetrazole purine derivatives and their potential chemotherapeutic activities Med. Chem. Res. (IF 1.783) Pub Date : 2020-10-02 Gulay Dilek, Ishak Ozel Tekin, Burak Coban, Ali Disli, Zuhal Gercek
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Aryl-enclosed polyketides from mangrove sediment associated bacterium Bacillus amyloliquefaciens attenuating pro-inflammatory 5-lipoxygenase Med. Chem. Res. (IF 1.783) Pub Date : 2020-08-28 Kajal Chakraborty, Lakshmi Rajan, Prima Francis
Two aryl-enclosed polyketides were identified from the ethyl acetate extract of mangrove sediment associated bacterium Bacillus amyloliquefaciens, and were characterized as 1-(8-hydroxy-1-oxoisochroman-3-yl)propyl 4′-(6′-hydroxy-8′-oxotetrahydrofuran-5′-yl)acetate (compound 1) and 6′a-(3′-(1′-(8-hydroxy-1-oxoisochroman-3-yl)propoxy)-3′-oxoethyl)-8′-oxotetrahydrofuran-6′-yl butyrate (compound 2) by
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Identification of potential anti-inflammatory and melanoma cytotoxic compounds from Aegiceras corniculatum Med. Chem. Res. (IF 1.783) Pub Date : 2020-08-29 Le Ba Vinh, Nguyen Viet Phong, Irshad Ali, Gao Dan, Young Sang Koh, Hoang Le Tuan Anh, Do Thi Van Anh, Seo Young Yang, Young Ho Kim
Many chemicals found in mangroves reportedly exhibit potent anticancer, antibacterial, anti-inflammatory, antioxidant, and antitumor properties. Several of such compounds include feature unique structures and display interesting pharmacological effects. Few medicinal mangrove plants from Vietnam have been characterized with regard to their chemical constituents. Aegiceras corniculatum (L.) Blanco is
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Radiosynthesis of [ 11 C]EI1 for imaging EZH2 using positron emission tomography Med. Chem. Res. (IF 1.783) Pub Date : 2020-09-14 Hao Wang, Yu Lan, Ping Bai, Zude Chen, Shenglin Luo, Yulong Xu, Stephanie Fiedler, Robin Striar, Changning Wang
Enhancer of zeste homolog 2 (EZH2) is responsible for the methylation of lysine 27 of histone H3 (H3K27) leading to transcriptional repression. Consequently, EZH2 is related with several diseases including cancers, as overexpressed EZH2 can down-regulate cancer suppressor genes. Therefore, EZH2 became a promising target for cancer treatment and diagnosis and in vivo imaging of EZH2 is critical for
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