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Enzyme Inhibition as a Potential Therapeutic Strategy to Treat COVID-19 Infection Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-14 Lukas Paulsson-Habegger, Andrew K. Snabaitis, Stephen P. Wren
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Discovery of novel 2-phenylamino-4-prolylpyrimidine derivatives as TRK/ALK dual inhibitors with promising antitumor effects Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-08 Tong Li, Changtao Li, Jing Yang, Ming Guo, Zhi Cao, Xinyu Wang, Nan Jiang, Xin Zhai
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Discovery of potent and selective Bcl-2 inhibitors with acyl sulfonamide skeleton Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Bin Wang, Weiwei Feng, Jinan Wang, Yuanzhen Dong, Yanlong Liu, Yiyan Yao, Jianqing Zhang, Wei Shi, Limin Liu, Hongying Zhang, Xiangyi He, Xiayun Chang, Xiaojin Wang, Hongjiang Xu, Fei Liu, Jun Feng
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Chemiluminescent probe for the detection of inverse electron demand Diels-Alder reaction between tetrazine and trans-Cyclooctene Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-08 Kui Wu, Maksim Royzen
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Design and Construction of a Stereochemically Diverse Piperazine-Based DNA Encoded Chemical Library Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-13 Srinivas Chamakuri, Mee-Kyung Chung, Errol L. G. Samuel, Kevin A. Tran, Ying-Chu Chen, Pranavanand Nyshadham, Conrad Santini, Martin M. Matzuk, Damian W. Young
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Synthesis and biological evaluation of 3,5-substituted pyrazoles as possible antibacterial agents Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-12 Matthew Payne, Amy L. Bottomley, Anthony Och, Anjar P. Asmara, Elizabeth J. Harry, Alison T. Ung
The emergence of multi-drug resistant bacteria has increased the need for novel antibiotics to help overcome what may be considered the greatest threat to modern medicine. Here we report the synthesis of fifteen novel 3,5-diaryl-1H- pyrazoles obtained via one-pot cyclic oxidation of a chalcone and hydrazine-monohydrate. The synthesised pyrazoles were then screened against Staphylococcus aureus and
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Computational Studies of Molecular Pre-Organization Through Macrocyclization: Conformational Distribution Analysis of Closely Related Non-macrocyclic and Macrocyclic Analogs Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-11 Gustav Olanders, Peter Brandt, Christian Sköld, Anders Karlén
Macrocycles form an important compound class in medicinal chemistry due to their interesting structural and biological properties. To help design macrocycles, it is important to understand how the conformational preferences are affected upon macrocyclization of a lead compound. To address this, we collected a unique data set of protein-ligand complexes containing “non-macrocyclic” (“linear”) ligands
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Benzothiophene derivatives as selective estrogen receptor covalent antagonists: Design, synthesis and anti-ERα activities Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-06 Chengfeng Bai, Shuangjie Wu, Shengnan Ren, Meiqi Zhu, Guoshun Luo, Hua Xiang
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Antiviral evaluation of hydroxyethylamine analogs: Inhibitors of SARS-CoV-2 main protease (3CLpro), a virtual screening and simulation approach Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-04 Yash Gupta, Sumit Kumar, Samantha E. Zak, Krysten A. Jones, Charu Upadhyay, Neha Sharma, Saara-Anne Azizi, Rahul S. Kathayat, Poonam, Andrew S. Herbert, Ravi Durvasula, Bryan C. Dickinson, John M. Dye, Brijesh Rathi, Prakasha Kempaiah
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Recent progress in covalent warheads for in vivo targeting of endogenous proteins Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-27 Naoya Shindo, Akio Ojida
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SAR of novel benzothiazoles targeting an allosteric pocket of DENV and ZIKV NS2B/NS3 proteases Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-04 Hannah Maus, Fabian Barthels, Stefan Josef Hammerschmidt, Katja Kopp, Benedikt Millies, Andrea Gellert, Alessia Ruggieri, Tanja Schirmeister
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Synthesis, Microbiological Evaluation and Structure Activity Relationship Analysis of Linezolid Analogues with Different C5-acylamino Substituents Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-08 Christos Matsingos, Taha Al-Adhami, Shirin Jamshidi, Charlotte Hind, Melanie Clifford, J. Mark Sutton, Khondaker Miraz Rahman
Antimicrobial resistance and lack of new antibiotics to treat multidrug-resistant (MDR) bacteria is a significant public health problem. There is a discovery void and the pipeline of new classes of antibiotics in clinical development is almost empty. Therefore, it is important to understand the structure activity relationships (SAR) of current chemical classes as that can help the drug discovery community
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Design, Synthesis, and Biological Evaluation of Novel Bcr-AblT315I Inhibitors Incorporating Amino Acids as Flexible Linker Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-08 Xiaoyan Pan, Nanxin Liu, Qingqing Zhang, Kai Wang, Yanchen Li, YuanYuan Shan, Zilong Li, Jie Zhang
Despite the success of imatinib in CML therapy through Bcr-Abl inhibition, acquired drug resistance occurs over time in patients. In particular, the resistance caused by T315I mutation remains a challenge in clinic. Herein, we embarked on a structural optimization campaign aiming at discovery of novel Bcr-Abl inhibitors toward T315I mutant based on previously reported dibenzoylpiperazin derivatives
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Zinc ionophores isolated from Terminalia bellirica fruit rind extract protect against cardiomyocyte hypoxia/reoxygenation injury Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-09-06 Vijaya Lakshmi Bodiga, Praveen Kumar Vemuri, Madhukar Rao Kudle, Sreedhar Bodiga
The study aimed to isolate and characterize zinc ionophores from Terminalia bellirica fruit using a liposome assay and test its utility in H9c2 rat cardiomyoblasts cells subjected to hypoxia/reoxygenation. Ethyl acetate extract that exhibited zinc ionophore activity was resolved to yield three polyphenols that were characterized as epicatechin-3-gallate (ECG), epigallocatechin-3-gallate (EGCG) and
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Progress in the development of small molecular inhibitors of the Bruton’s tyrosine kinase (BTK) as a promising cancer therapy Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-10 Xiu-Juan Liu, Xu-Liu, Xiao-Jing Pang, Xin -Ying Yuan, Guang-Xi Yu, Yin-Ru Li, Yong-Feng Guan, Yan-Bing Zhang, Jian Song, Qiu-Rong Zhang, Sai-Yang Zhang
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Design, synthesis, and target identification of new hypoxia-inducible factor 1 (HIF-1) inhibitors containing 1-alkyl-1H-pyrazole-3-carboxamide moiety Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-30 Marina Sakai, Nobuaki Takahashi, Hiroaki Ikeda, Yutaka Furutani, Shoko Higuchi, Takehiro Suzuki, Naoshi Dohmae, Sayaka Kobayashi, Hiroshi Harada, Soichi Kojima, Tomokazu Matsuura, Akira Hattori, Hideaki Kakeya
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Synthesis, in Vitro Cytotoxicity and Biological Evaluation of Twenty Novel 1,3-Benzenedisulfonyl Piperazines as Antiplatelet Agents Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-30 Xiu-jie LIU, Yan WANG, Xiao WANG, Zhi-hao ZHANG
In order to discover antiplatelet drugs with novel structures and expand our research scope, total twenty 1,3-benzenedisulfonyl piperazines, were designed and synthesized. These target compounds were divided into two series, namely 4-methoxy-1,3-benzenedisulfonyl piperazines of series 1 and 4-ethoxy-1,3-benzenedisulfonyl piperazines of series 2. With adenosine diphosphate (ADP), arachidonic acid (AA)
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Identification of new [1,2,4]triazolo[4,3-a]quinoxalines as potent VEGFR-2 tyrosine kinase inhibitors: design, synthesis, anticancer evaluation, and in silico studies Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-28 Nawaf A. Alsaif, Mohammed S. Taghour, Mohammed M. Alanazi, Ahmad J. Obaidullah, Wael A. Alanazi, Abdullah Alasmari, Hussam Albassam, Mohammed A. Dahab, Hazem A. Mahdy
Tumor angiogenesis is mainly regulated by VEGFR-2. In this study, a new series of [1,2,4]triazolo[4,3-a]quinoxaline based-derivatives has been designed and synthesized to develop new anti-proliferative and anti-VEGFR-2 members. Anti-proliferative activities of the synthesized compounds were tested against MCF-7 and HepG2 cell lines. Compound 19a exhibited the highest activity towards both MCF-7 and
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Inhibition of amyloid formation of amyloid β (1-42), amylin and insulin by 1,5-diazacyclooctanes, a spermine-acrolein conjugate Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-28 Risako Kunitomi, Ambara R. Pradipta, Haruka Kawabe, Nadine Lobsiger, Katsunori Tanaka, Tamotsu Zako
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CYPlebrity: Machine learning models for the prediction of inhibitors of cytochrome P450 enzymes Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-28 Wojciech Plonka, Conrad Stork, Martin Šícho, Johannes Kirchmair
The vast majority of approved drugs are metabolized by the five major cytochrome P450 (CYP) isozymes, 1A2, 2C9, 2C19, 2D6 and 3A4. Inhibition of CYP isozymes can cause drug-drug interactions with severe pharmacological and toxicological consequences. Computational methods for the fast and reliable prediction of the inhibition of CYP isozymes by small molecules are therefore of high interest and relevance
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Further SAR Studies on Natural Template Based Neuroprotective Molecules for the Treatment of Alzheimer’s Disease Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-28 Yash Pal Singh, Gauri Shankar, Shagufta Jahan, Gourav Singh, Navneet Kumar, Atanu Barik, Prabhat Upadhyay, Lovejit Singh, Kajal Kamble, Gireesh Kumar Singh, Sanjay Tiwari, Prabha Garg, Sarika Gupta, Gyan Modi
In our earlier paper, we described ferulic acid (FA) template based novel series of multifunctional cholinesterase (ChE) inhibitors for the management of AD. This report has further extended the structure-activity relationship (SAR) studies of this series of molecules in a calibrated manner to improve upon the ChEs inhibition and antioxidant property to identify the novel potent multifunctional molecule
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Synthesis and evaluation of new mixed “2 + 1” Re, 99mTc and 186Re tricarbonyl dithiocarbamate complexes with different monodentate ligands Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-19 Antonio Shegani, Myrto Ischyropoulou, Ioanna Roupa, Christos Kiritsis, Konstantina Makrypidi, Afroditi Papasavva, Catherine Raptopoulou, Vassilis Psycharis, Heather M. Hennkens, Maria Pelecanou, Minas S. Papadopoulos, Ioannis Pirmettis
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Erratum to "De novo design with deep generative models based on 3D similarity scoring" [Bioorg. Med. Chem. 44 (2021) 116308]. Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-27 Kostas Papadopoulos,Kathryn A Giblin,Jon Paul Janet,Atanas Patronov,Ola Engkvist
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Synthesis and Evaluation of Squaramide and Thiosquaramide Inhibitors of the DNA Repair Enzyme SNM1A Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-25 Mark Berney, William Doherty, Werner Theodor Jauslin, Manav T Manoj, Eva-Maria Dürr, Joanna Francelle McGouran
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Synthesis, antitumor activity and in silico analyses of amino acid derivatives of artepillin C, drupanin and baccharin from green propolis Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-19 Débora Munhoz Rodrigues, Gisele Bulhões Portapilla, Guilherme Martins Silva, Andressa Duarte, Cristiana Gonçalez Rotta, Carlos Henrique Tomich de Paula da Silva, Sérgio de Albuquerque, Jairo Kenupp Bastos, Vanessa Leiria Campo
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A novel tricyclic β-lactam exhibiting potent antibacterial activities against carbapenem-resistant Enterobacterales: Synthesis and structure-activity-relationships Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-11 Jun Sato, Hiroki Kusano, Toshiaki Aoki, Satoru Shibuya, Katsuki Yokoo, Kazuo Komano, Takuya Oguma, Shuhei Matsumoto, Takafumi Sato, Kazuya Yasuo, Kenji Yamawaki
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Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2 Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-11 Daibao Wei, Tianwen Hu, Yumin Zhang, Wei Zheng, Haitao Xue, Jingshan Shen, Yuanchao Xie, Haji A. Aisa
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Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-12 Haiyan Yao, Quanping Guo, Mengran Wang, Rui Wang, Zhaoqing Xu
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Antiviral fungal metabolites and some insights into their contribution to the current COVID-19 pandemic Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-13 Jacqueline Aparecida Takahashi, Bianca Vianna Rodrigues Barbosa, Matheus Thomaz Nogueira Silva Lima, Patrícia Gomes Cardoso, Christiane Contigli, Lúcia Pinheiro Santos Pimenta
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Design, Synthesis and Biological Evaluation of Novel Acridine and Quinoline Derivatives as Tubulin Polymerization Inhibitors with Anticancer Activities Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-23 Yichang Ren, Yong Ruan, Binbin Cheng, Ling Li, Jin Liu, Yuyu Fang, Jianjun Chen
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Virtual screening and biological evaluation of PPARγ antagonists as potential anti-prostate cancer agents Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-13 Suliman Almahmoud, Catherine C. Elix, Jeremy O. Jones, Corey R. Hopkins, Jonathan L. Vennerstrom, Haizhen A. Zhong
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Harmine-inspired design and synthesis of benzo[d]imidazo[2,1-b]thiazole derivatives bearing 1,3,4-oxadiazole moiety as potential tumor suppressors Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-13 Tianming Zhao, Yu Yang, Jing Yang, Youbao Cui, Zhi Cao, Daiying Zuo, Xin Zhai
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Design, synthesis and anti-fibrosis evaluation of imidazo[1,2–a]pyridine derivatives as potent ATX inhibitors Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-13 Yuxiang Chen, Hongrui Lei, Tong Li, Youbao Cui, Xinyu Wang, Zhi Cao, Huinan Wu, Xin Zhai
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A review upon medicinal perspective and designing rationale of DPP-4 inhibitors Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-10 Shubham Kumar, Anu Mittal, Amit Mittal
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Cysteine proteases as potential targets for anti-trypanosomatid drug discovery Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-13 Wagner A.S. Judice, Letícia Silva Ferraz, Rayssa de Mello Lopes, Luan dos Santos Vianna, Fábio da Silva Siqueira, Juliana F. Di Iorio, Laura de Azevedo Maffeis Dalzoto, Mariana Nascimento Romero Trujilho, Taiz dos Reis Santos, Maurício F.M. Machado, Tiago Rodrigues
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High allele discrimination in the typing of single nucleotide polymorphisms of miRNA Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-12 Fumie Takei, Misaki Akiyama, Minori Dateki
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Design, synthesis, and antitumor activity evaluation of steroidal oximes Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Ana R. Gomes, Ana S. Pires, Ana M. Abrantes, Ana C. Gonçalves, Saul C. Costa, Carla L. Varela, Elisiário T. Silva, Maria F. Botelho, Fernanda M.F. Roleira
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In vivo organic synthesis by metal catalysts Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Tsung-Che Chang, Katsunori Tanaka
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Discovery of 1,3,4-Oxadiazole Derivatives as Potential Antitumor Agents Inhibiting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-18 Lincheng Fang, Jiping Tian, Kaixuan Zhang, Xiaoyi zhang, Yingqiao Liu, Zhibo Cheng, Jinpei Zhou, Huibin Zhang
Inhibition of the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction by small-molecule inhibitors is emerging cancer immunotherapy. A series of novel 1,3,4-oxadiazole derivatives were designed, synthesized, and evaluated for their activities in vitro and vivo to find potent inhibitors of the PD-1/PD-L1 interaction. Among them, compound Ⅱ-14 exhibited outstanding biochemical
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Design, synthesis, and biological evaluation of potent 1,2,3,4-tetrahydroisoquinoline derivatives as anticancer agents targeting NF-κB signaling pathway Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-18 Seongrak Sim, Sumi Lee, Seungyun Ko, Bich Phuong Bui, Phuong Linh Nguyen, Jungsook Cho, Kiho Lee, Jong-Soon Kang, Jae-Kyung Jung, Heesoon Lee
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Biofunctional supramolecular hydrogels fabricated from a short self-assembling peptide modified with bioactive sequences for the 3D culture of breast cancer MCF-7 cells Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-11 Jyh Yea Chia, Takayuki Miki, Hisakazu Mihara, Hiroshi Tsutsumi
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New FDA oncology small molecule drugs approvals in 2020: Mechanism of action and clinical applications Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-09 Thais Cristina Mendonça Nogueira, Marcus Vinicius Nora de Souza
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EGFR-targeted prodrug activation using bioorthogonal alkene-azide click-and-release chemistry Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Jessica M. Fairhall, Júlia C. Camilli, Blake H. Gibson, Sarah Hook, Allan B. Gamble
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Antiviral strategies targeting host factors and mechanisms obliging +ssRNA viral pathogens Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Supreeti Mahajan, Shweta Choudhary, Pravindra Kumar, Shailly Tomar
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Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Zonghui Ma, Ling Jiang, Bingyan Li, Dailin Liang, Yu Feng, Li Liu, Cheng Jiang
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Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Huarong Yang, Qing Li, Mingzhi Su, Fang Luo, Yahua Liu, Daoping Wang, Yanhua Fan
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Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Sigrid Schwarthoff, Nicolas Tischer, Henrike Sager, Bianca Schätz, Marius M. Rohrbach, Ihar Raztsou, Dina Robaa, Friedemann Gaube, Hans-Dieter Arndt, Thomas Winckler
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Synthesis of acyclic nucleoside phosphonates targeting flavin-dependent thymidylate synthase in Mycobacterium tuberculosis Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-06 Nicolas G. Biteau, Vincent Roy, Jean-Christophe Lambry, Hubert F. Becker, Hannu Myllykallio, Luigi A. Agrofoglio
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Synthesis and duplex-forming ability of oligonucleotides modified with 4′-C,5′-C-methylene-bridged nucleic acid (4′,5′-BNA) Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Takao Yamaguchi, Chika Yamamoto, Masahiko Horiba, Hiroshi Aoyama, Satoshi Obika
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Development of curcumin-based amyloid β aggregation inhibitors for Alzheimer's disease using the SAR matrix approach Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Rohmad Yudi Utomo, Yasunobu Asawa, Satoshi Okada, Hyun Seung Ban, Atsushi Yoshimori, Jürgen Bajorath, Hiroyuki Nakamura
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Preparation, Biological & Cheminformatics-based Assessment of N2,N4-diphenylpyrimidine-2,4-diamine as Potential Kinase-targeted Antimalarials Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-08 Borvornwat Toviwek, Oraphan Phuangsawai, Adchatawut Konsue, Supa Hannongbua, Jennifer Riley, Nicole Mutter, Mark Anderson, Lauren Webster, Irene Hallyburton, Kevin D Read, M. Paul Gleeson
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Kinetic and Structural Investigations of Novel Inhibitors of Human Epithelial 15-Lipoxygenase-2 Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-05 Wan-Chen Tsai, Nathan C. Gilbert, Amanda Ohler, Michelle Armstrong, Steven Perry, Chakrapani Kalyanaraman, Adam Yasgar, Ganesha Rai, Anton Simeonov, Ajit Jadhav, Melissa Standley, Hsiau-Wei Lee, Phillip Crews, Anthony T. Iavarone, Matthew P. Jacobson, David B. Neau, Adam R. Offenbacher, Marcia Newcomer, Theodore R. Holman
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Docking and Mutagenesis Studies Lead to Improved Inhibitor Development of ML355 for Human Platelet 12-lipoxygenase Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-04 Wan-Chen Tsai, Ansari M. Aleem, Jennyfer Tena, Mirella Rivera-Velazquez, Harman Singh Brah, Sarvind Tripathi, Melinee D'silva, Jerry L. Nadler, Chakrapani Kalyanaraman, Mathew P. Jacobson, Theodore Holman
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Designed, synthesized and biological evaluation of proteolysis targeting chimeras (PROTACs) as AR degraders for prostate cancer treatment Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-07-26 Jian-Jia Liang, Hang Xie, Rui-Hua Yang, Ni Wang, Zi-Jun Zheng, Chen Zhou, Ya-Lei Wang, Zhi-Jia Wang, Hong-Min Liu, Li-Hong Shan, Yu Ke
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Elaboration of a benzofuran scaffold and evaluation of binding affinity and inhibition of Escherichia coli DsbA: A fragment-based drug design approach to novel antivirulence compounds Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-07-22 Luke F. Duncan, Geqing Wang, Olga V. Ilyichova, Rabeb Dhouib, Makrina Totsika, Martin J. Scanlon, Begoña Heras, Belinda M. Abbott
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Concise solid-phase synthesis enables derivatisation of YEATS domain cyclopeptide inhibitors for improved cellular uptake Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-02 Yixiang Jiang, Sha Liu, Gaofei Tian, Hayden Jit Hei Cheung, Xin Li, Xiang David Li
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Design and synthesis of β-carboline derivatives with nitrogen mustard moieties against breast cancer Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-08-02 Jianan Sun, Jiesen Wang, Xinyan Wang, Xu Hu, Hao Cao, Jiao Bai, Dahong Li, Huiming Hua
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Bioorthogonal strategies for the in vivo synthesis or release of drugs Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-07-15 Boris Lozhkin, Thomas R. Ward
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Identification of isoform/domain-selective fragments from the selection of DNA-encoded dynamic library Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-07-25 Yu Zhou, Wenyin Shen, Jianzhao Peng, Yuqing Deng, Xiaoyu Li
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Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer Bioorg. Med. Chem. (IF 3.641) Pub Date : 2021-07-22 Xuan Yang, Dacheng Fan, Aidan Henry Troha, Hyunjun Max Ahn, Kun Qian, Bo Liang, Yuhong Du, Haian Fu, Andrey A. Ivanov
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