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Discovery of Potent Kappa Opioid Receptor Agonists Derived from Akuammicine J. Med. Chem. (IF 6.8) Pub Date : 2024-11-20 Madeline R. Hennessy, Simone M. Creed, Anna M. Gutridge, Lisa E. Rusali, Dan Luo, Bakhtyar Sepehri, Elizabeth S. Rhoda, José A. Villegas, Richard M. van Rijn, Andrew P. Riley
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Modular Assembly of Heterotrifunctional Molecules Enabled by Iodosulfonylation of Allenes and Subsequent Amination J. Med. Chem. (IF 6.8) Pub Date : 2024-11-20 Xiaofeng Lin, Chuxiong Peng, Shijie Liu, Jianpin Xiang, Binyan Lin, Qichen Zhan, Peng Cao, Tao Cao
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A Bifunctional Sulfide Donor Approach for Ischemic Stroke: Leveraging Butylphthalide as a Carrier for Sulfide Prodrug J. Med. Chem. (IF 6.8) Pub Date : 2024-11-20 Wen Peng, Jianru Liu, Zhen Li, Yuanan Wang, Yangqian Sun, Yanzhao Chen, David J. Lefer, Weiwei Guo, Yueqin Zheng
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Lysine-Targeted Covalent Inhibitors of PI3Kδ Synthesis and Screening by In Situ Interaction Upgradation J. Med. Chem. (IF 6.8) Pub Date : 2024-11-19 Bo Yuan, Yifan Feng, Mengyan Ma, Weiming Duan, Yujie Wu, Jiaxin Liu, Hong-Yi Zhao, Zhe Yang, San-Qi Zhang, Minhang Xin
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Advancements in NMDA Receptor-Targeted Antidepressants: From d-Cycloserine Discovery to Preclinical Efficacy of Lu AF90103 J. Med. Chem. (IF 6.8) Pub Date : 2024-11-19 Erhad Ascic, Mauro Marigo, Laurent David, Kjartan Frisch Herrik, Morten Grupe, Charlotte Hougaard, Arne Mørk, Christopher R. Jones, Lassina Badolo, Kristen Frederiksen, Harrie C. M. Boonen, Henrik Sindal Jensen, John Paul Kilburn
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Prodrug Strategy to Address Impaired Oral Absorption of a Weakly Basic TYK2 Inhibitor Caused by a Gastric Acid-Reducing Agent J. Med. Chem. (IF 6.8) Pub Date : 2024-11-19 Murugaiah A M Subbaiah, Thangeswaran Ramar, Maheswara Reddy, Sankara Sivaprasad LVJ, Shekhar Yeshwante, Srikanth Sridhar, Salil Desai, Manoj Chiney, Elizabeth A. Dierks, Arvind Mathur, Ryan Moslin, David S. Weinstein
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Discovery of First Branched-Chain Ketoacid Dehydrogenase Kinase (BDK) Inhibitor Clinical Candidate PF-07328948 J. Med. Chem. (IF 6.8) Pub Date : 2024-11-19 Kevin J. Filipski, Luis A. Martinez-Alsina, Matthew R. Reese, Edelweiss Evrard, Leanne M. Buzon, Kimberly O. Cameron, Yuan Zhang, Karen J. Coffman, James Bradow, Bethany L. Kormos, Shenping Liu, John D. Knafels, Parag V. Sahasrabudhe, Jie Chen, Amit S. Kalgutkar, Andrew J. Bessire, Christine C. Orozco, Amanda Balesano, Matthew A. Cerny, Eliza Bollinger, Allan R. Reyes, Brigitte Laforest, Amy Rosado
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Opportunities and Challenges of Arginase Inhibitors in Cancer: A Medicinal Chemistry Perspective J. Med. Chem. (IF 6.8) Pub Date : 2024-11-18 Mariacristina Failla, Maria Cristina Molaro, Marica Erminia Schiano, Marta Serafini, Gioele Antonio Tiburtini, Eleonora Gianquinto, Riccardo Scoccia, Chiara Battisegola, Maria Grazia Rimoli, Konstantin Chegaev, Giuseppe Ercolano, Loretta Lazzarato, Francesca Spyrakis, Federica Sodano
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Correction to “Discovery of a Covalent Inhibitor of Pro-Caspase-1 Zymogen Blocking NLRP3 Inflammasome Activation and Pyroptosis” J. Med. Chem. (IF 6.8) Pub Date : 2024-11-18 Dongyi Cao, Ruiying Xi, Hongye Li, Zhonghui Zhang, Xiaoke Shi, Shanshan Li, Yujie Jin, Wanli Liu, Guolin Zhang, Xiaohua Liu, Shunxi Dong, Xiaoming Feng, Fei Wang
Page 15888. In the Covalent Molecular Docking section, first sentence, “SEESAR” should be corrected as “Schrödinger suite version 2022-4”. In the third sentence, “N═C–S–R” should be corrected as “–N–(C═S)–R”. This article has not yet been cited by other publications.
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De Novo Discovery of a Noncovalent Cell-Penetrating Bicyclic Peptide Inhibitor Targeting SARS-CoV-2 Main Protease J. Med. Chem. (IF 6.8) Pub Date : 2024-11-18 Yahong Tan, Jinyue Yang, Min Wang, Qi Peng, Yongqi Li, Lifeng Fu, Mengmeng Zhang, Jiang Wu, Guanya Yang, Christopher John Hipolito, Youming Zhang, Jianxun Qi, Yi Shi, Yizhen Yin
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First-In-Class Thiosemicarbazone Metal Complexes Targeting the Sigma-2 Receptor (S2R) as an Innovative Strategy against Pancreatic Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-17 Alessandra Barbanente, Joanna Kopecka, Daniele Vitone, Mauro Niso, Rosanna Rizzi, Corrado Cuocci, Francesca Serena Abatematteo, Francesco Mastropasqua, Nicola Antonio Colabufo, Nicola Margiotta, Fabio Arnesano, Chiara Riganti, Carmen Abate
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4-(Pyrazolyl)benzenesulfonamide Ureas as Carbonic Anhydrases Inhibitors and Hypoxia-Mediated Chemo-Sensitizing Agents in Colorectal Cancer Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-11-17 Wagdy M. Eldehna, Mohamed Fares, Alessandro Bonardi, Moscos Avgenikos, Fady Baselious, Matthias Schmidt, Tarfah Al-Warhi, Hatem A. Abdel-Aziz, Robert Rennert, Thomas S. Peat, Claudiu T. Supuran, Ludger A. Wessjohann, Hany S. Ibrahim
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Discovery of Selective PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects by Targeting the Metal Pocket J. Med. Chem. (IF 6.8) Pub Date : 2024-11-15 Mei-Yan Jiang, Chen Zhang, Qing-Hua Huang, Ling-Ling Feng, Yi-Yi Yang, Qian Zhou, Hai-Bin Luo, Yinuo Wu
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A Phenotypic High-Throughput Screen Identifies Small Molecule Modulators of Endogenous RGS10 in BV-2 Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-11-15 Shwetal Talele, Stephanie Gonzalez, Julia Trudeau, Ahmad Junaid, Cody A Loy, Ryan A. Altman, Benita Sjögren
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Discovery of 1-(Phenylsulfonyl)-1,2,3,4-tetrahydroquinoline Derivative as Orally Bioavailable and Safe RORγt Inverse Agonists for Potential Treatment of Rheumatoid Arthritis J. Med. Chem. (IF 6.8) Pub Date : 2024-11-15 Shan-Liang Sun, Hong-Jiang Xu, Xiao-Long Jiang, Jian Zhou, Wei Shi, Xiao-Jin Wang, Wei Song, Xia-Yun Chang, Xue-Qin Ma, Xiao-Fang Zou, Shi-Han Wu, Jin Yang, Qing-Qing Li, Zi-Xuan Wang, Jiao Cai, Shao-Peng Yu, Qing-Xin Wang, Tian-Hua Wei, Jia-Zhen Wu, Zhen-Jiang Tong, Yun Zhou, Yi-Bo Wang, Yan-Cheng Yu, Xue-Jiao Leng, Ning Ding, Zhi-Hao Shi, Wei-Chen Dai, Xin Xue, Nian-Guang Li, Xiao-Long Wang
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Discovery and Preclinical Characterization of Fulacimstat (BAY 1142524), a Potent and Selective Chymase Inhibitor As a New Profibrinolytic Approach for Safe Thrombus Resolution J. Med. Chem. (IF 6.8) Pub Date : 2024-11-14 Chantal Fürstner, Jens Ackerstaff, Heinrich Meier, Alexander Straub, Joachim Mittendorf, Jens Schamberger, Martina Schäfer, Kirsten Börngen, Hannah Jörißen, Dmitry Zubov, Katja Zimmermann, Adrian Tersteegen, Volker Geiss, Elke Hartmann, Barbara Albrecht-Küpper, Pedro D’Orléans-Juste, Catherine Lapointe, Laurence Vincent, Stefan Heitmeier, Hanna Tinel
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Discovery and Optimization of First-in-Class Molecular Glue Degraders of the WIZ Transcription Factor for Fetal Hemoglobin Induction to Treat Sickle Cell Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-11-14 John Ryan Kerrigan, Noel M. Thomsen, Artiom Cernijenko, Sarah E. Kochanek, Janetta Dewhurst, Gary O’Brien, Nathaniel F. Ware, Carina C. Sanchez, James R. Manning, Xiaolei Ma, Elizabeth Ornelas, Nikolas A. Savage, James R. Partridge, Andrew W. Patterson, Philip Lam, Natalie A. Dales, Simone Bonazzi, Sneha Borikar, Amelia E. Hinman, Pamela Y. Ting
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Discovery of Novel 5-Cyano-3-phenylindole-Based LSD1/HDAC Dual Inhibitors for Colorectal Cancer Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-11-14 Hui-Juan Zhu, Hui-Min Zhou, Xiao-Xiao Zhou, Shi-Jie Li, Meng-Jie Zheng, Zhen Xu, Wen-Jing Dai, Yi-Bo Ban, Meng-Yao Zhang, Yi-Zhe Zhang, Jia-Rui Lu, Yong-Tao Xu, Sai-Qi Wang, Xiao-Jing Shi, Ying-Chao Duan
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Light-Activable Inhibitor Overcomes Antimicrobial Resistance and Regulates Antibacterial Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-11-14 Zhuang Ma, Boxuan Hou, Anhui Liao, Ying Tan, Chunyan Tan, Yuyang Jiang
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Design and Synthesis of Acyclic Boronic Acid Arginase Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-14 Jason D. Shields, Brian M. Aquila, David Emmons, M. Raymond V. Finlay, Eric T. Gangl, Chungang Gu, Scott N. Mlynarski, Jens Petersen, Petar Pop-Damkov, Li Sha, Iain Simpson, Siavash Tavakoli, Sharon Tentarelli, Haixia Wang, Qing Ye, XiaoLan Zheng
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Generation of BT-Amide, a Bone-Targeted Pyk2 Inhibitor, Effective via Oral Administration, for the Prevention of Glucocorticoid-Induced Bone Loss J. Med. Chem. (IF 6.8) Pub Date : 2024-11-14 Xiuqi Wang, Amy Y. Sato, Silvia Marino, Nisreen Akel, Gunnar Boysen, Alexei G. Basnakian, Teresita M. Bellido, Hong-Yu Li
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Design, Synthesis, and Biological Evaluation of Novel Diaminopyrimidine Macrocycles as Fourth Generation Reversible EGFR Inhibitors That Overcome Clinical Resistance to Osimertinib Mediated by C797S Mutation J. Med. Chem. (IF 6.8) Pub Date : 2024-11-13 Shiliang Hu, Linjiang Tong, Qiao Qin, Jiaxin Wen, Yan Li, Fang Feng, Kunzhong Wu, Yang Zhou, Jinsai Shang, Junjian Wang, Jinbao Liu, Hua Xie, Xiaoyun Lu
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Design, Synthesis, and Biological Evaluation of New Selective PDE4 Inhibitors for Topical Treatment of Psoriasis J. Med. Chem. (IF 6.8) Pub Date : 2024-11-13 Dengqin He, Gang Li, Jia-Qiang Wu, Yan Geng, Xudong Qian, Yuanhui Liu, Yanghui Ou, Mengjie Li, Jun Wang, Wei Pan, Guoping Zhang, Dandan Chen, Jiaxin Chen, Zichen Xu, Hengming Ke, Hongliang Yao
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Covalent Targeting of Histidine Residues with Aryl Fluorosulfates: Application to Mcl-1 BH3 Mimetics J. Med. Chem. (IF 6.8) Pub Date : 2024-11-12 Giulia Alboreggia, Parima Udompholkul, Emma L. Atienza, Kendall Muzzarelli, Zahra Assar, Maurizio Pellecchia
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Prioritization of Eleven-Nineteen-Leukemia Inhibitors as Orally Available Drug Candidates for Acute Myeloid Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2024-11-12 Xuejiao Shirley Guo, Sandeep Atla, Satyanarayana Nyalata, Yugendar R. Alugubelli, Peng-Hsun Chase Chen, Shiqing Xu, Wenshe Ray Liu
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Proline Analogues in Drug Design: Current Trends and Future Prospects J. Med. Chem. (IF 6.8) Pub Date : 2024-11-12 Vladimir Kubyshkin, Pavel K. Mykhailiuk
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Unnatural Amino Acids: Strategies, Designs, and Applications in Medicinal Chemistry and Drug Discovery J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Krishna K. Sharma, Komal Sharma, Kamya Rao, Anku Sharma, Gajanan K. Rathod, Shams Aaghaz, Naina Sehra, Rajesh Parmar, Brett VanVeller, Rahul Jain
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Synthesis and Pharmacological Characterization of Fluorescent Ligands Targeting the Angiotensin II Receptors Derived from Agonists, β-Arrestin-Biased Agonists, and Antagonists J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Céline Delaitre, Michel Boisbrun, Samir Acherar, André Dias, Alexandra Kleinclauss, Mathilde Achard, Mélissa Colin, Trung Minh Nguyen, Nicolas Humbert, Khawla Chmeis, Karen L. Martinez, Nicolas Gilles, Philippe Robin, Sandra Lecat, François Dupuis
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Modulatory Role of Pantropic Cell Signaling Pathways in the Antimigratory and Antiproliferative Action of Triazole Chelated Iridium(III) Complexes in Cervical Cancer Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Anushka Mondal, Bishnu Das, Souvik Karmakar, Soumili Pani, Shrabani Khan, Parna Gupta, Jayasri Das Sarma
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Discovery of the First-in-Class Dual-Target ROCK/HDAC Inhibitor with Potent Antitumor Efficacy in Vivo That Trigger Antitumor Immunity J. Med. Chem. (IF 6.8) Pub Date : 2024-11-10 Churu Mao, Jiebin Fang, Shijie Zou, Yun Huang, Xiaoming Chen, Xia Ding, Zhangyun Fang, Ningjing Zhang, Yijie Lou, Zhe Chen, Wanjing Ding, Zhongjun Ma
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Structure-Guided Design of Affinity/Covalent-Bond Dual-Driven Inhibitors Targeting the AMP Site of FBPase J. Med. Chem. (IF 6.8) Pub Date : 2024-11-09 Hongxuan Cao, Zeyue Huang, Zheng Liu, Xiao Zhang, Yanliang Ren, Muhammad Salman Hameed, Li Rao, Nokwanda P. Makunga, Georgi M. Dobrikov, Jian Wan
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Discovery of a Novel Macrocyclic Noncovalent CDK7 Inhibitor for Cancer Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-11-09 Hongfu Lu, Yihong Zhang, Jinxin Liu, Tao Jiang, Xiang Yu, Haoyu Zhang, Tao Liang, Jingjing Peng, Xin Cai, Xiaoling Lan, Jinmin Ren, Mei Ge, Jingyang Zhang, Jingjin Shang, Jiaojiao Yu, Hongcan Ren, Qiang Liu, Jinting Gao, Lili Tang, Xiao Ding, Man Zhang, Alex Aliper, Qiang Lu, Fusheng Zhou, Jiong Lan, Feng Ren, Alex Zhavoronkov
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Discovery of SD-436: A Potent, Highly Selective and Efficacious STAT3 PROTAC Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Renqi Xu, Haibin Zhou, Longchuan Bai, Donna McEachern, Dimin Wu, Ranjan Kumar Acharyya, Mi Wang, Jelena Tošović, Chao-Yie Yang, Krishnapriya Chinnaswamy, Jennifer L. Meagher, Jeanne A. Stuckey, Cai Liu, Meilin Wang, Bo Wen, Duxin Sun, Shaomeng Wang
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Recent Progress and Future Perspectives on Anti-Hyperuricemic Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Zhiqiang Sun, Xuewen Zhang, Zean Zhao, Xiaoxun Li, Jianxin Pang, Jianjun Chen
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Closing the Design–Make–Test–Analyze Loop: Interplay between Experiments and Predictions Drives PROTACs Bioavailability J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Zulma Santisteban Valencia, Jennifer Kingston, Filip Miljković, Hannah Rowbottom, Nadia Mann, Sophie Davies, Martin Ekblad, Silvio Di Castro, Karolina Kwapień, Erik Malmerberg, Stig D. Friis, Thomas Lundbäck, Tomas Leek, Johan Wernevik
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Discovery of Thiazole Carboxamides as Novel Vanin-1 Inhibitors for Inflammatory Bowel Disease Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Tao Xie, Gao-Yao Cao, Shize Zhang, Meng-Ke Li, Xin Jin, Liu Liu, Guangji Wang, Le Zhen
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Structure–Activity Relationships and Discovery of (S)-5-(tert-Butyl)-11-(difluoromethoxy)-9-methoxy-2-oxo-1,2,5,6-tetrahydropyrido[2′,1′:2,3]imidazo[4,5-h]quinoline-3-carboxylic Acid (AB-161), a Novel Orally Available and Liver-Centric HBV RNA Destabilizer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Dimitar Gotchev, Shuai Chen, Benjamin Dugan, Bruce D. Dorsey, Xu Wang, Muhammad Sheraz, Rose Kowalski, Fei Liu, Sunny Tang, Tim Chiu, Troy Harasym, Ingrid E. Graves, Emily P. Thi, Jeremy D. Mason, Nathan Overholt, Ravi Dugyala, Angela M. Lam, Andrew G. Cole, Michael J. Sofia
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A Fast Method to Monitor Tyrosine Kinase Inhibitor Mechanisms J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Alejandro Fernández, Margarida Gairí, María Teresa González, Miquel Pons
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Discovery of CHD1 Antagonists for PTEN-Deficient Prostate Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Rebecca L. Johnson, Amanda L. Graboski, Fengling Li, Jacqueline L. Norris-Drouin, William G. Walton, Cheryl H. Arrowsmith, Matthew R. Redinbo, Stephen V. Frye, Lindsey I. James
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Discovery of SZJK-0421: A Novel Potent, Low Toxicity, Selective Second Generation of CRM1 Inhibitor for the Treatment of Both Hematological and Solid Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Hang Miao, Yanru Qin, DingLu Shao, Qinghua Chen, Yupeng Pan, Meng Lei, Ruokun Wu, Xinran Ye, Xueyuan Wang, Yongqiang Zhu
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Development of N-(4-(1H-Imidazol-1-yl)phenyl)-4-chlorobenzenesulfonamide, a Novel Potent Inhibitor of β-Catenin with Enhanced Antitumor Activity and Metabolic Stability J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Michela Puxeddu, Lele Ling, Silvia Ripa, Michele D’Ambrosio, Marianna Nalli, Anastasia Parisi, Pietro Sciò, Antonio Coluccia, Arianna Granese, Martina Santelli, Domiziana Masci, Petra Cuřínová, Chiara Naro, Claudio Sette, Arianna Pastore, Mariano Stornaiuolo, Chiara Bigogno, Giulio Dondio, Laura Di Magno, Gianluca Canettieri, Te Liu, Romano Silvestri, Giuseppe La Regina
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Discovery of 5-Nitro-N-(3-(trifluoromethyl)phenyl) Pyridin-2-amine as a Novel Pure Androgen Receptor Antagonist against Antiandrogen Resistance J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Huating Wang, Xuwen Wang, Haiyang Zhong, Lvtao Cai, Weitao Fu, Xin Chai, Jianing Liao, Rong Sheng, Luhu Shan, Xiaohong Xu, Lei Xu, Peichen Pan, Tingjun Hou, Dan Li
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Small-Molecule Modulators Targeting Coactivator-Associated Arginine Methyltransferase 1 (CARM1) as Therapeutic Agents for Cancer Treatment: Current Medicinal Chemistry Insights and Emerging Opportunities J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Shuqing Li, Wanyi Pan, Chengpeng Tao, Zhihao Hu, Binbin Cheng, Jianjun Chen, Xiaopeng Peng
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Antiplasmodial and Insecticidal Activities of Third-Generation Ivermectin Hybrids J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Parth, Sofia Santana, Catarina Rôla, Carla Bastos Oliveira, Miguel Prudêncio, Kamaljit Singh, Diana Fontinha
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Single Amine or Guanidine Modification on Norvancomycin and Vancomycin to Overcome Multidrug-Resistance through Augmented Lipid II Binding and Increased Membrane Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Xiaolei Bian, Zhifu Chen, Fang Li, Yuanyuan Xie, Yi Li, Youhong Luo, Xiangman Zou, Hui Wang, Jingwen Zhang, Xiaowen Wang, Jinyong Zhang, Dongliang Guan
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Medicinal Chemistry Education: Emphasize Fundamentals and Skillfully Integrate Knowledge J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Shaoqing Du, Xueping Hu, Craig W. Lindsley, Peng Zhan
Medicinal chemistry is an interdisciplinary field that aims to discover innovative drugs and synthesize drug molecules at the intersection of chemistry and biology. In the field of medicinal chemistry education, it is essential to establish a robust foundation by emphasizing fundamental principles of chemistry and biology. This strategy not only imparts students with a comprehensive understanding of
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Structure-Based Design of Covalent SARS-CoV-2 Papain-like Protease Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Bin Tan, Xueying Liang, Ahmadullah Ansari, Prakash Jadhav, Haozhou Tan, Kan Li, Francesc Xavier Ruiz, Eddy Arnold, Xufang Deng, Jun Wang
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Inhibition of Human Salivary and Pancreatic α-Amylase by Resveratrol Oligomers J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Rizliya Visvanathan, Dang Truong Le, Sushil Dhital, Topul Rali, Rohan A. Davis, Gary Williamson
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Discovery of Highly Selective Inhibitors of Microtubule-Associated Serine/Threonine Kinase-like (MASTL) J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Rebecca A. Gallego, Stephanie Scales, Chad Toledo, Marin Auth, Louise Bernier, Madeline Berry, Sonja Brun, Loanne Chung, Carl Davis, Wade Diehl, Klaus Dress, Koleen Eisele, Jeff Elleraas, Jason Ewanicki, Yvette Fobian, Samantha Greasley, Eric C. Greenwald, Ted W. Johnson, Penney Khamphavong, Jennifer Lafontaine, Jian Li, Angelica Linton, Michael Maestre, Nichol Miller, Anwar Murtaza, Ryan L. Patman
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Target Ligand Separation and Identification of Isoforsythiaside as a Histone Lysine-Specific Demethylase 1 Covalent Inhibitor Against Breast Cancer Metastasis J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Mengzhen Gu, Xiaoqing Xu, Xiaoping Wang, Yun Wang, Yu Zhao, Xiaoxian Hu, Lu Zhu, Zhenzhong Deng, Chao Han
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Expanding the Solvent/Protein Region Occupation of the Non-Nucleoside Reverse Transcriptase Inhibitor Binding Pocket for Improved Broad-Spectrum Anti-HIV-1 Efficacy: from Rigid Phenyl-Diarylpyrimidines to Flexible Hydrophilic Piperidine-Diarylpyrimidines J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Wen-Juan Huang, Christophe Pannecouque, Erik De Clercq, Angela Corona, Stefania Maloccu, Enzo Tramontano, Shuai Wang, Fen-Er Chen
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Medicinal Chemistry Education and Training J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Craig W. Lindsley
I decided to weigh in on the ongoing discussion about medicinal chemistry education and training with my thoughts on the matter, as I began my career in industry (Parke-Davis, Eli Lilly and Merck) and later moved into academia (Vanderbilt University/Warren Center for Neuroscience Drug Discovery). First and foremost, training in synthetic organic chemistry is essential. A deep understanding of mechanistic
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A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins J. Med. Chem. (IF 6.8) Pub Date : 2024-11-04 Suzanne Ackloo, Fengling Li, Magda Szewczyk, Almagul Seitova, Peter Loppnau, Hong Zeng, Jin Xu, Shabbir Ahmad, Yelena A Arnautova, A. J. Baghaie, Serap Beldar, Albina Bolotokova, Paolo A. Centrella, Irene Chau, Matthew A. Clark, John W. Cuozzo, Saba Dehghani-Tafti, Jeremy S. Disch, Aiping Dong, Antoine Dumas, Jianwen A. Feng, Pegah Ghiabi, Elisa Gibson, Justin Gilmer, Brian Goldman, Stuart R Green
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Optimization of Antiproliferative Properties of Triimine Copper(II) Complexes J. Med. Chem. (IF 6.8) Pub Date : 2024-11-04 Katarzyna Choroba, Bartosz Zowiślok, Sławomir Kula, Barbara Machura, Anna M. Maroń, Karol Erfurt, Cristiana Marques, Sandra Cordeiro, Pedro V. Baptista, Alexandra R. Fernandes
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Identification of Oral Bioavailable Coumarin Derivatives as Potential AR Antagonists Targeting Prostate Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-04 Jinbiao Liao, Jianing Liao, Minkui Zhang, Yanzhen Yu, Lvtao Cai, Kaixin Le, Weitao Fu, Yiyang Qin, Tingjun Hou, Dan Li, Rong Sheng
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Pan-Transcriptional Enhanced Associated Domain Palmitoylation Pocket Covalent Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-11-02 Jinhyuk Kim, Hadong Kim, Jongwan Kim, Seon Yeon Cho, Sungho Moon, Youngki Yoo, Hanseong Kim, Jin Kwan Kim, Hyejin Jeon, Wan Namkung, Gyoonhee Han, Kyoung Tai No
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Azobenzene-Tagged Photopeptides Exhibiting Excellent Selectivity and Light-Induced Cytotoxicity in MCF-7 Cells over HeLa and A549 J. Med. Chem. (IF 6.8) Pub Date : 2024-11-02 Sambit Pradhan, Surajit Sarker, Pakkirisamy Thilagar
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Discovery of ERD-1233 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader for the Treatment of ER+ Human Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Ranjan Kumar Acharyya, Rohan Kalyan Rej, Biao Hu, Zhixiang Chen, Dimin Wu, Jianfeng Lu, Hoda Metwally, Donna McEachern, Yu Wang, Wei Jiang, Longchuan Bai, Jelena Tošović, Christina L. Gersch, Guozhang Xu, Weihong Zhang, WenXue Wu, E. Scott Priestley, Zhihua Sui, Farzad Sarkari, Bo Wen, Duxin Sun, James M. Rae, Shaomeng Wang
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Palladium-Mediated Bioorthogonal System for Prodrug Activation of N-Benzylbenzamide-Containing Tubulin Polymerization Inhibitors for the Treatment of Solid Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Jinlong Li, Tong Zhang, Di Wu, Chen He, Haoxiang Weng, Tiandong Zheng, Jie Liu, Hong Yao, Jichao Chen, Yansong Ren, Zheying Zhu, Jinyi Xu, Shengtao Xu
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Synthesis and Biological Evaluation of New Chalcogen Semicarbazone (S, Se) and Their Azole Derivatives against Chagas Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Mercedes Rubio-Hernández, Verónica Alcolea, Elany Barbosa da Silva, Miriam A. Giardini, Thaís H. M Fernandes, Nuria Martínez-Sáez, Anthony J. O’Donoghue, Jair L. Siqueira-Neto, Silvia Pérez-Silanes
更新日期：2024-11-12
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