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Medicinal Chemistry Gone Wild J. Med. Chem. (IF 7.3) Pub Date : 2024-04-25 Tesko Chaganti, Chun-Yi Tsai, Yu-Pu Juang, Mohamed Abdelalim, Tim Cernak
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Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-04-25 Qiwen Sun, Yuxiu Chu, Nana Zhang, Rui Chen, Lili Wang, Jiangxia Wu, Yongxi Dong, Hongliang Li, Ling Wang, Lei Tang, Changyou Zhan, Ji-Quan Zhang
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Structure-Based Rational and General Strategy for Stabilizing Single-Chain T-Cell Receptors to Enhance Affinity J. Med. Chem. (IF 7.3) Pub Date : 2024-04-25 Jia-Ling Zou, Kai-Xiang Chen, Xiao-Juan Wang, Zheng-Chang Lu, Xian-Hui Wu, Yun-Dong Wu
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Artificial Intelligence-Assisted Optimization of Antipigmentation Tyrosinase Inhibitors: De Novo Molecular Generation Based on a Low Activity Lead Compound J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Hong Cai, Wenchao Chen, Jing Jiang, Hao Wen, Xinyu Luo, Junjie Li, Liuxin Lu, Rui Zhao, Xinhua Ni, Yinyan Sun, Jiahui Wang, Zhen Li, Bin Ju, Xiaoying Jiang, Renren Bai
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Correction to “Development of Cytotoxic GW7604-Zeise’s Salt Conjugates as Multitarget Compounds with Selectivity for Estrogen Receptor-Positive Tumor Cells” J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Patricia Grabher, Paul Kapitza, Nikolas Hörmann, Amelie Scherfler, Martin Hermann, Michael Zwerger, Hristo P. Varbanov, Brigitte Kircher, Daniel Baecker, Ronald Gust
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Psychoplastogenic DYRK1A Inhibitors with Therapeutic Effects Relevant to Alzheimer’s Disease J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Hunter T. Warren, Hannah N. Saeger, Robert J. Tombari, Milan Chytil, Kurt Rasmussen, David. E. Olson
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Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sedative Effect J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Zixiang Li, Rufeng Ye, Qian He, Jiashuo Lu, Yanting Sun, Xiujian Sun, Siyuan Tang, Shuyang Hu, Jingrui Chai, Linghui Kong, Xiaoning Liu, Jing Chen, Yun Fang, Yingjie Lan, Qiong Xie, Jinggen Liu, Liming Shao, Wei Fu, Yujun Wang, Wei Li
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Druglike, 18F-labeled PET Tracers Targeting Fibroblast Activation Protein J. Med. Chem. (IF 7.3) Pub Date : 2024-04-24 Muhammet Tanc, Nicolò Filippi, Yentl Van Rymenant, Sergei Grintsevich, Isabel Pintelon, Marlies Verschuuren, Joni De Loose, Emile Verhulst, Euy Sung Moon, Lorenzo Cianni, Sigrid Stroobants, Koen Augustyns, Frank Roesch, Ingrid De Meester, Filipe Elvas, Pieter Van der Veken
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Discovery of a Novel Orally Bioavailable FLT3-PROTAC Degrader for Efficient Treatment of Acute Myeloid Leukemia and Overcoming Resistance of FLT3 Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-24 Junwei Wang, Quanjin Rong, Lei Ye, Bingqian Fang, Yifan Zhao, Yu Sun, Haikun Zhou, Dan Wang, Jinting He, Zhenzhen Cui, Qijian Zhang, Di Kang, Lihong Hu
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Discovery of Novel Dual Inhibitors Targeting Mutant IDH1 and NAMPT for the Treatment of Glioma with IDH1Mutation J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Fei Wen, Gang Gui, Xiaoyu Wang, Anqi Qin, Tianfang Ma, Hui Chen, Chunzheng Li, Xiaoming Zha
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Development of Prolinol Containing Inhibitors of Hypoxanthine–Guanine–Xanthine Phosphoribosyltransferase: Rational Structure-Based Drug Design J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Dianne T. Keough, Magdalena Petrová, Gordon King, Michal Kratochvíl, Radek Pohl, Eva Doleželová, Alena Zíková, Luke W. Guddat, Dominik Rejman
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Virtual Screening Strategies for Identifying Novel Chemotypes J. Med. Chem. (IF 7.3) Pub Date : 2024-04-23 Stuart Lang, Martin J. Slater
The identification of active compounds, or a series of compounds, is the crucial first step in all drug discovery projects. Ideally these compounds should display, or have the potential to display after optimization, good physical chemistry, and drug like properties. Screening, both physical and virtual, is a process that involves interrogating a protein target of interest with large numbers of compounds
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Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Jiankang Hu, Hongrui Xu, Tianbang Wu, Cheng Zhang, Hui Shen, Ruibo Dong, Qingqing Hu, Qiuping Xiang, Shuang Chai, Guolong Luo, Xiaoshan Chen, Yumin Huang, Xiaofan Zhao, Chao Peng, Xishan Wu, Bin Lin, Yan Zhang, Yong Xu
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Discovery and Structure–Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT2A Receptor Agonists J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Emil M. Ro̷rsted, Anders A. Jensen, Gints Smits, Karla Frydenvang, Jesper L. Kristensen
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Design of Evodiamine–Glucose Conjugates with Improved In Vivo Antitumor Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-04-22 Zhe Wu, Shuqiang Chen, Zhipeng Chen, Guoqiang Dong, Defeng Xu, Chunquan Sheng
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Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles J. Med. Chem. (IF 7.3) Pub Date : 2024-04-20 Salma M. Hefny, Tarek F. El-Moselhy, Nabaweya El-Din, Simone Giovannuzzi, Thamer Bin Traiki, Mansoor-Ali Vaali-Mohammed, Ahmed M. El-Dessouki, Koki Yamaguchi, Masaharu Sugiura, Moataz A. Shaldam, Claudiu T. Supuran, Maha-Hamadien Abdulla, Wagdy M. Eldehna, Haytham O. Tawfik
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Lead Optimization of Butyrolactone I as an Orally Bioavailable Antiallergic Agent Targeting FcγRIIB J. Med. Chem. (IF 7.3) Pub Date : 2024-04-19 Chun-Lan Xie, Hong-Xiu Xiao, Pei-Fang Song, Qing-Mei Liu, Haoxiang Wei, Liang Wu, Guang-Hao Zhu, Guang-Ming Liu, Yandong Zhang, Ping Wang, Xian-Wen Yang
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FETPY: a Diiron(I) Thio–Carbyne Complex with Prominent Anticancer Activity In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-04-19 Ekatarina Mihajlović, Lorenzo Biancalana, Sanja Jelača, Lorenzo Chiaverini, Biljana Dojčinović, Duško Dunđerović, Stefano Zacchini, Sanja Mijatović, Danijela Maksimović-Ivanić, Fabio Marchetti
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Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer’s Disease J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Ji Eun Park, Chhabi L. Chaudhary, Deepak Bhattarai, Kyung Bo Kim
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Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Esra Balıkçı, Anne-Sophie M. C. Marques, Ludwig G. Bauer, Raina Seupel, James Bennett, Brigitt Raux, Karly Buchan, Klemensas Simelis, Usha Singh, Catherine Rogers, Jennifer Ward, Carol Cheng, Tamas Szommer, Kira Schützenhofer, Jonathan M. Elkins, David L. Sloman, Ivan Ahel, Oleg Fedorov, Paul E. Brennan, Kilian V. M. Huber
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Selective Elimination of Senescent Cancer Cells by Galacto-Modified PROTACs J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Mengyang Chang, Feng Gao, Giri Gnawali, Hang Xu, Yue Dong, Xiang Meng, Wenpan Li, Zhiren Wang, Byrdie Lopez, Jennifer S. Carew, Steffan T. Nawrocki, Jianqin Lu, Qing-Yu Zhang, Wei Wang
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Gemfibrozil-Platinum(IV) Precursors for New Enhanced-Starvation and Chemotherapy In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Xue-Qing Song, Xu Guo, Yi-Xin Ding, Yi-Xuan Han, Zhi-Hao You, Yali Song, Yanan Yuan, Longfei Li
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Monophosphoryl Lipid A-Rhamnose Conjugates as a New Class of Vaccine Adjuvants J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Rajendra Rohokale, Jiatong Guo, Zhongwu Guo
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Arene–Arene Coupled Disulfamethazines (or Sulfadiazine)-Phenanthroline-Metal(II) Complexes were Synthesized by In Situ Reactions and Inhibited the Growth and Development of Triple-Negative Breast Cancer through the Synergistic Effect of Antiangiogenesis, Anti-Inflammation, Pro-Apoptosis, and Cuproptosis J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Bing-Bing Xu, Nan Jin, Ji-Cheng Liu, Ai-Qiu Liao, Hong-Yu Lin, Xiu-Ying Qin
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Discovery of a Meisoindigo-Derived PROTAC as the ATM Degrader: Revolutionizing Colorectal Cancer Therapy via Synthetic Lethality with ATR Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-18 Ting-Ting Liu, Qing Wang, Yuxing Zhou, Baixin Ye, Tingting Liu, Linyang Yan, Jinbao Fan, Jiahao Xu, Yingjun Zhou, Zanxian Xia, Xu Deng
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Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-04-17 Lufeng Zheng, Yuxin Zhang, Shuang Mei, Tianyuan Xie, Yunting Zou, Yuting Wang, Han Jing, Shengtao Xu, Pierre Dramou, Zhen Xu, Jindong Li, Yang Zhou, Miao-Miao Niu
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Structural Elucidation and Antiviral Activity of Covalent Cathepsin L Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-17 Sven Falke, Julia Lieske, Alexander Herrmann, Jure Loboda, Katarina Karničar, Sebastian Günther, Patrick Y. A. Reinke, Wiebke Ewert, Aleksandra Usenik, Nataša Lindič, Andreja Sekirnik, Klemen Dretnik, Hideaki Tsuge, Vito Turk, Henry N. Chapman, Winfried Hinrichs, Gregor Ebert, Dušan Turk, Alke Meents
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Design, Synthesis, and Biological Evaluation of β-Trifluoroethoxydimethyl Selenides as Potent Antiosteoporosis Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-04-17 Yao Wu, Bin Li, Linkun Ying, Yao Chen, Yuxin Zhang, Chaoming Hu, Yichi Zhang, Lele Yi, Weiwei Xue, Shengbin Huang, Zengqiang Song
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Synthesis and Structure–Activity Relationships for Glutamate Transporter Allosteric Modulators J. Med. Chem. (IF 7.3) Pub Date : 2024-04-16 Andréia C. K. Fontana, Adi N.R. Poli, Jitendra Gour, Yellamelli V.V. Srikanth, Nicholas Anastasi, Devipriya Ashok, Apeksha Khatiwada, Katelyn L. Reeb, Mary Hongying Cheng, Ivet Bahar, Scott M. Rawls, Joseph M. Salvino
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Mitochondria-Selective Dicationic Small-Molecule Ligand Targeting G-Quadruplex Structures for Human Colorectal Cancer Therapy J. Med. Chem. (IF 7.3) Pub Date : 2024-04-16 Bo-Xin Zheng, Wei Long, Wende Zheng, Yaoxun Zeng, Xiao-Chun Guo, Ka-Hin Chan, Meng-Ting She, Alan Siu-Lun Leung, Yu-Jing Lu, Wing-Leung Wong
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Targeting KRAS Diversity: Covalent Modulation of G12X and Beyond in Cancer Therapy J. Med. Chem. (IF 7.3) Pub Date : 2024-04-15 Tonia Kirschner, Matthias P. Müller, Daniel Rauh
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Rational Design of a Novel Class of Human ClpP Agonists through a Ring-Opening Strategy with Enhanced Antileukemia Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-04-15 Xinrong Xiang, Zhengyi Dai, Baozhu Luo, Ninglin Zhao, Song Liu, Jing Sui, Jiasheng Huang, Yuanzheng Zhou, Jinlong Gu, Jiangnan Zhang, Tao Yang, Rui Bao, Youfu Luo
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Design, Synthesis, and Pharmacological Evaluation of Spiro[carbazole-3,3′-pyrrolidine] Derivatives as cGAS Inhibitors for Treatment of Acute Lung Injury J. Med. Chem. (IF 7.3) Pub Date : 2024-04-15 Mingjie Chen, Shuyue Lei, Zihua Zhou, Meng Wang, Chunlan Feng, Xiaoling Gao, Chunyong Ding, Zilan Song, Wei Tang, Ao Zhang
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Structure-Guided Discovery and Preclinical Assessment of Novel (Thiophen-3-yl)aminopyrimidine Derivatives as Potent ERK1/2 Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-13 Wen Shuai, Huan Xiao, Panpan Yang, Yiwen Zhang, Faqian Bu, Yongya Wu, Qiu Sun, Guan Wang, Liang Ouyang
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Discovery of Novel Aryl Triazolone Dihydropyridines (ATDPs) Targeting Highly Conserved Residue W229 as Promising HIV-1 NNRTIs J. Med. Chem. (IF 7.3) Pub Date : 2024-04-13 Yanying Sun, Zhenzhen Zhou, Na Wang, Fabao Zhao, Ying Liu, Xiaoxuan Xu, Xiaohan Wang, Zhenbang Gou, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Dongwei Kang, Xinyong Liu
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Iridium(III)-Based PD-L1 Agonist Regulates p62 and ATF3 for Enhanced Cancer Immunotherapy J. Med. Chem. (IF 7.3) Pub Date : 2024-04-13 Dongping Deng, Mengmeng Wang, Yan Su, Hongbao Fang, Yuncong Chen, Zhi Su
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Molecular Imaging of Alzheimer’s Disease-Related Sigma-1 Receptor in the Brain via a Novel Ru-Mediated Aromatic 18F-deoxyfluorination Probe J. Med. Chem. (IF 7.3) Pub Date : 2024-04-12 Ping Bai, Frederick A. Bagdasarian, Yulong Xu, Yanli Wang, Yongle Wang, Ashley Gomm, Yanting Zhou, Rui Wu, Hsiao-Ying Wey, Rudolph E. Tanzi, Can Zhang, Yu Lan, Changning Wang
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Discovery of the First-in-Class G9a/GLP PROTAC Degrader J. Med. Chem. (IF 7.3) Pub Date : 2024-04-11 Julia Velez, Yulin Han, Hyerin Yim, Peiyi Yang, Zhijie Deng, Kwang-su Park, Md Kabir, H. Ümit Kaniskan, Yan Xiong, Jian Jin
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Discovery and Characterization of a Novel Cereblon-Recruiting PRC1 Bridged PROTAC Degrader J. Med. Chem. (IF 7.3) Pub Date : 2024-04-12 Md Kabir, Lihuai Qin, Kaixiu Luo, Yan Xiong, Rebecca A. Sidi, Kwang-Su Park, Jian Jin
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Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease J. Med. Chem. (IF 7.3) Pub Date : 2024-04-12 Yugendar R. Alugubelli, Jing Xiao, Kaustav Khatua, Sathish Kumar, Long Sun, Yuying Ma, Xinyu R. Ma, Veerabhadra R. Vulupala, Sandeep Atla, Lauren R. Blankenship, Demonta Coleman, Xuping Xie, Benjamin W. Neuman, Wenshe Ray Liu, Shiqing Xu
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Discovery of YFJ-36: Design, Synthesis, and Antibacterial Activities of Catechol-Conjugated β-Lactams against Gram-Negative Bacteria J. Med. Chem. (IF 7.3) Pub Date : 2024-04-10 Fangjun Liu, Qunhuan Kou, Hongyuan Li, Yangzhi Cao, Meng Chen, Xin Meng, Yinyong Zhang, Ting Wang, Hui Wang, Dan Zhang, Yushe Yang
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Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles J. Med. Chem. (IF 7.3) Pub Date : 2024-04-11 Moritz Schwarz, Maksym Kurkunov, Florian Wittlinger, Ramona Rudalska, Guiqun Wang, Martin Peter Schwalm, Alexander Rasch, Benedikt Wagner, Stefan A. Laufer, Stefan Knapp, Daniel Dauch, Matthias Gehringer
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Comparative Study of Sonodynamic and Photoactivated Cancer Therapies with Re(I)-Tricarbonyl Complexes Comprising Phenanthroline Ligands J. Med. Chem. (IF 7.3) Pub Date : 2024-04-11 Rajesh Kushwaha, Virendra Singh, Silda Peters, Ashish Kumar Yadav, Tumpa Sadhukhan, Biplob Koch, Samya Banerjee
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Synthesis and Structure–Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT2 Receptor Agonist J. Med. Chem. (IF 7.3) Pub Date : 2024-04-09 Geoffrey B. Varty, Clinton E. Canal, Tina A. Mueller, Joshua A. Hartsel, Richa Tyagi, Ken Avery, Michael E. Morgan, Amy C. Reichelt, Pradip Pathare, Erik Stang, Michael G. Palfreyman, Alex Nivorozhkin
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Targeting Myeloid Leukemia-1 in Cancer Therapy: Advances and Directions J. Med. Chem. (IF 7.3) Pub Date : 2024-04-10 Hongguang Deng, Yu Han, Liang Liu, Hong Zhang, Dan Liu, Jiachen Wen, Min Huang, Linxiang Zhao
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Reducing PD-L1 Expression by Degraders and Downregulators as a Novel Strategy to Target the PD-1/PD-L1 Pathway J. Med. Chem. (IF 7.3) Pub Date : 2024-04-10 Zhijie Wang, Lin Yuan, Xiaotong Liao, Xia Guo, Jianjun Chen
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Discovery of a Novel Potent Tetrazole Antifungal Candidate with High Selectivity and Broad Spectrum J. Med. Chem. (IF 7.3) Pub Date : 2024-04-10 Tingjunhong Ni, Yumeng Hao, Zichao Ding, Xiaochen Chi, Fei Xie, Ruina Wang, Junhe Bao, Lan Yan, Liping Li, Ting Wang, Dazhi Zhang, Yuanying Jiang
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Design, Synthesis, and Biological Evaluation of Novel Arylomycins against Multidrug-Resistant Gram-Negative Bacteria J. Med. Chem. (IF 7.3) Pub Date : 2024-04-10 Yinyong Zhang, Dan Zhang, Wenhao Zhao, Hongyuan Li, Zhengyu Lu, Bin Guo, Xin Meng, Xianli Zhou, Yushe Yang
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Potentiating Activity of GmhA Inhibitors on Gram-Negative Bacteria J. Med. Chem. (IF 7.3) Pub Date : 2024-04-10 François Moreau, Dmytro Atamanyuk, Markus Blaukopf, Marek Barath, Mihály Herczeg, Nuno M. Xavier, Jérôme Monbrun, Etienne Airiau, Vivien Henryon, Frédéric Leroy, Stéphanie Floquet, Damien Bonnard, Robert Szabla, Chris Brown, Murray S. Junop, Paul Kosma, Vincent Gerusz
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Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP-Deleted Cancers J. Med. Chem. (IF 7.3) Pub Date : 2024-04-10 Kevin M. Cottrell, Kimberly J. Briggs, Douglas A. Whittington, Haris Jahic, Janid A. Ali, Charles B. Davis, Shanzhong Gong, Deepali Gotur, Lina Gu, Patrick McCarren, Matthew R. Tonini, Alice Tsai, Erik W. Wilker, Hongling Yuan, Minjie Zhang, Wenhai Zhang, Alan Huang, John P. Maxwell
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Correction to “Steric Blockade of Oxy-Myoglobin Oxidation by Thiosemicarbazones: Structure–Activity Relationships of the Novel PPP4pT Series’’ J. Med. Chem. (IF 7.3) Pub Date : 2024-04-10 Tharushi P. Wijesinghe, Busra Kaya, Miguel A. Gonzálvez, Jeffrey R. Harmer, Mahan Gholam Azad, Paul V. Bernhardt, Mahendiran Dharmasivam, Des R. Richardson
Page 15472. In the Acknowledgments, a funding body was inadvertently omitted, although their support played a pivotal role in the successful completion of this research endeavor. The following should be added as the fourth sentence in the published article’s Acknowledgments section: D.R.R. appreciates a Senior Research Grant from Tour de Cure – Soiree for a Cure 2021. This article has not yet been
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Discovery of a Novel CSF-1R Inhibitor with Highly Improved Pharmacokinetic Profiles and Superior Efficacy in Colorectal Cancer Immunotherapy J. Med. Chem. (IF 7.3) Pub Date : 2024-04-09 Qi Lv, Hongqiong Yang, Dan Wang, Haikun Zhou, Juan Wang, Yishu Zhang, Dapeng Wu, Ying Xie, Yingshan Lv, Lihong Hu, Junwei Wang
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Promising Anticancer Prodrugs Based on Pt(IV) Complexes with Bis-organosilane Ligands in Axial Positions J. Med. Chem. (IF 7.3) Pub Date : 2024-04-09 Francisco Navas, Ana Chocarro-Calvo, Patricia Iglesias-Hernández, Paloma Fernández-García, Victoria Morales, José Manuel García-Martínez, Raúl Sanz, Antonio De la Vieja, Custodia García-Jiménez, Rafael A. García-Muñoz
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Discovery of 2-Amide-3-methylester Thiophenes that Target SARS-CoV-2 Mac1 and Repress Coronavirus Replication, Validating Mac1 as an Antiviral Target J. Med. Chem. (IF 7.3) Pub Date : 2024-04-09 Sarah Wazir, Tomi A. O. Parviainen, Jessica J. Pfannenstiel, Men Thi Hoai Duong, Daniel Cluff, Sven T. Sowa, Albert Galera-Prat, Dana Ferraris, Mirko M. Maksimainen, Anthony R. Fehr, Juha P. Heiskanen, Lari Lehtiö
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Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises J. Med. Chem. (IF 7.3) Pub Date : 2024-04-09 Kosmas Alexandros Pervanidis, Giovanni Danilo D’Angelo, Jörn Weisner, Sven Brandherm, Daniel Rauh
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Identification of Cellular Protein Targets of a Half-Sandwich Iridium(III) Complex Reveals Its Dual Mechanism of Action via Both Electrophilic and Oxidative Stresses J. Med. Chem. (IF 7.3) Pub Date : 2024-04-05 Robin Ramos, Anthi Karaiskou, Candice Botuha, Sadek Amhaz, Michaël Trichet, Florent Dingli, Jérémy Forté, France Lam, Alexis Canette, Chloé Chaumeton, Murielle Salome, Thomas Chenuel, Céline Bergonzi, Philippe Meyer, Sylvain Bohic, Damarys Loew, Michèle Salmain, Joëlle Sobczak-Thépot
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Discovery of Highly Potent Solute Carrier 13 Member 5 (SLC13A5) Inhibitors for the Treatment of Hyperlipidemia J. Med. Chem. (IF 7.3) Pub Date : 2024-04-04 Li’ao Zhang, Wenjun Hu, Huimin Guo, Qiushuang Sun, Xi Xu, Zhiyu Li, Zhixia Qiu, Jinlei Bian
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Design, Synthesis, and In Vivo Evaluation of Isosteviol Derivatives as New SIRT3 Activators with Highly Potent Cardioprotective Effects J. Med. Chem. (IF 7.3) Pub Date : 2024-04-04 Zhenyu Chen, Zhiyin Li, Ruilong Xu, Yufeng Xie, Dehuai Li, Yu Zhao
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Pd2Spermine as an Alternative Therapeutics for Cisplatin-Resistant Triple-Negative Breast Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-04-08 Tatiana J. Carneiro, Ana L. M. Batista de Carvalho, Martin Vojtek, Raquel C. Laginha, Maria Paula M. Marques, Carmen Diniz, Ana M. Gil
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Design and Synthesis of Novel Ultralong-Acting Peptides as EDP-EBP Interaction Inhibitors for Pulmonary Fibrosis Treatment J. Med. Chem. (IF 7.3) Pub Date : 2024-04-08 Yixiang Wang, Fanghan Xue, Wei Cheng, Qian Zhao, Nazi Song, Zihan Shi, Han Liu, Yu Li, Qinglin Tang, Qi Liu, Yiqing Wang, Fangfang Zhang, Xianxing Jiang