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A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Bing-ling Peng, Ting Ran, Xue Chen, Jian-cheng Ding, Zi-rui Wang, Wen-juan Li, Wen Liu
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Development of Inhibitors, Probes, and PROTAC Provides a Complete Toolbox to Study PARK7 in the Living Cell J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Yuqing Jia, Merve Oyken, Robbert Q. Kim, Rayman T.N. Tjokrodirijo, Arnoud H. de Ru, Antonius P. A. Janssen, Stephan M. Hacker, Peter A. van Veelen, Paul P. Geurink, Aysegul Sapmaz
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Brain-Penetrant Macrocycles: Design Considerations, Future Prospects, and Call for Papers J. Med. Chem. (IF 7.3) Pub Date : 2024-05-07 Cori A. Malinky, Aaron M. Bender
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Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update J. Med. Chem. (IF 7.3) Pub Date : 2024-05-06 Laura Hillebrand, Xiaojun Julia Liang, Ricardo A. M. Serafim, Matthias Gehringer
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Antitumor Activity and Mechanistic Insights of a Mitochondria-Targeting Cu(I) Complex J. Med. Chem. (IF 7.3) Pub Date : 2024-05-06 Siyu Xu, Yashuai Hao, Xinyi Xu, Lu Huang, Yuqiong Liang, Jia Liao, Jie-Ru Yang, Yang Zhou, Mingdong Huang, Ke-Zhao Du, Cen Zhang, Peng Xu
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Discovery of 2,6-Naphthyridine Analogues as Selective FGFR4 Inhibitors for Hepatocellular Carcinoma J. Med. Chem. (IF 7.3) Pub Date : 2024-05-05 Heesook Oh, Jisook Kim, Seung Hyun Jung, Tae Hee Ha, Young Gil Ahn, Gibeom Nam, Kyeongwon Moon, Pargat Singh, In Su Kim
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Discovery of BIO-8169─A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Magnus Pfaffenbach, Philippe N. Bolduc, Zhili Xin, Fang Gao, Ryan Evans, Terry Fang, Jayanth V. Chodaparambil, Kate L. Henry, Pei Li, Steven Mathieu, Claire Metrick, Jorge A. Vera Rebollar, Rong-Fang Gu, Christie-Ann Mccarl, John Silbereis, Emily A. Peterson
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Design, Synthesis, Bioactive Evaluation, and Molecular Dynamics Simulation of Novel 4H-Pyrano[3,2-c]pyridine Analogues as Potential Sterol 14α-Demethylase (CYP51) Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-05-04 Ailing Bao, Wenjing Jiang, Xiansong Xie, Deyuan Wang, Ziquan Deng, Jingwen Wang, Weiyi Li, Xiaorong Tang, Yingkun Yan
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Triazoles in Medicinal Chemistry: Physicochemical Properties, Bioisosterism, and Application J. Med. Chem. (IF 7.3) Pub Date : 2024-05-03 Qianwen Guan, Shuaishuai Xing, Lei Wang, Jiawei Zhu, Can Guo, Chunlei Xu, Qun Zhao, Yulan Wu, Yao Chen, Haopeng Sun
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Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Yunhang Guo, Hai Xue, Nan Hu, Ye Liu, Hanzi Sun, Desheng Yu, Ling Qin, Gongyin Shi, Fan Wang, Lei Xin, Weihua Sun, Fan Zhang, Xiaomin Song, Shuran Li, Qiang Wei, Ying Guo, Yong Li, Xiaoxin Liu, Shuaishuai Chen, Taichang Zhang, Yue Wu, Dan Su, Yutong Zhu, Aiying Xu, Haipeng Xu, Shasha Yang, Zhijun Zheng, Junhua Liu, Xuefei Yang, Xi Yuan, Yuan Hong, Xuebing Sun, Yin Guo, Changyou Zhou, Xuesong Liu, Lai
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Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl-1 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-02 Giulia Alboreggia, Parima Udompholkul, Carlo Baggio, Kendall Muzzarelli, Zahra Assar, Maurizio Pellecchia
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Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to Cathepsin A Are More Efficient in Delivering Antiviral Active Metabolites to the Lung J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Jiapeng Li, Daniel Macedo de Melo Jorge, Weiwen Wang, Shuxin Sun, Tristan Frum, Yu-An Hang, Yueting Liu, Xingwu Zhou, Jingcheng Xiao, Xinwen Wang, Jason R. Spence, Christiane E. Wobus, Hao-Jie Zhu
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Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Jianyu Xu, Hongyun Qi, Zhen Wang, Ling Wang, Barbara Steurer, Xin Cai, Jinxin Liu, Alex Aliper, Man Zhang, Feng Ren, Alex Zhavoronkov, Xiao Ding
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Discovery of Selective Proteolysis-Targeting Chimera Degraders Targeting PTP1B as Long-Term Hypoglycemic Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Zunhua Yang, Yuqi Ying, Shaobing Cheng, Jiamin Wu, Ziwei Zhang, Pei Hu, Jian Xiong, Huilan Li, Qing Zeng, Zhifang Cai, Yulin Feng, Yuanying Fang
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Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Nunzia Cristiano, Alexandre Cabayé, Isabelle Brabet, Ralf Glatthar, Amelie Tora, Cyril Goudet, Hugues-Olivier Bertrand, Anne Goupil-Lamy, Peter J. Flor, Jean-Philippe Pin, Isabelle McCort-Tranchepain, Francine C. Acher
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[52Mn]Mn-BPPA-Trastuzumab: A Promising HER2-Specific PET Radiotracer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-01 Ngô Minh Toàn, Adrienn Vágner, Gábor Nagy, Gábor Ország, Tamás Nagy, Csaba Csikos, Balázs Váradi, Gergő Zoltán Sajtos, István Kapus, Zoltán Szoboszlai, Dezső Szikra, György Trencsényi, Gyula Tircsó, Ildikó Garai
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Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Lianchao Liu, Abhijit Parolia, Yihan Liu, Caiyun Hou, Tongchen He, Yuanyuan Qiao, Sanjana Eyunni, Jie Luo, Chungen Li, Yongxing Wang, Fengtao Zhou, Weixue Huang, Xiaomei Ren, Zhen Wang, Arul M. Chinnaiyan, Ke Ding
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A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19 J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Charlotte M. N. Allerton, Joel T. Arcari, Lisa M. Aschenbrenner, Melissa Avery, Bruce M. Bechle, Mohammad Amin Behzadi, Britton Boras, Leanne M. Buzon, Rhonda D. Cardin, Natasha R. Catlin, Anthony A. Carlo, Karen J. Coffman, Alyssa Dantonio, Li Di, Heather Eng, Kathleen A. Farley, Rose Ann Ferre, Steven S. Gernhardt, Scott A. Gibson, Samantha E. Greasley, Siennah R. Greenfield, Brett L. Hurst, Amit
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Discovery of a New Anti-Inflammatory Agent from Anemoside B4 Derivatives and Its Therapeutic Effect on Colitis by Targeting Pyruvate Carboxylase J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Lijuan Lv, Qiurong Li, Kexin Wang, Jianping Zhao, Kejun Deng, Ran Zhang, Zhong Chen, Ikhlas A. Khan, Chunshan Gui, Suxiang Feng, Shilin Yang, Yanli Liu, Qiongming Xu
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A Nonbactericidal Anionic Antimicrobial Peptide Provides Prophylactic and Therapeutic Efficacies against Bacterial Infections in Mice by Immunomodulatory–Antithrombotic Duality J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Yanmei He, Shimei Ruan, Guozhu Liang, Jing Hao, Xiaoyan Zhou, Zhuorui Li, Lixian Mu, Jing Wu, Hailong Yang
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New Improved cGMP Analogues to Target Rod Photoreceptor Degeneration J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Oswaldo Pérez, Agnese Stanzani, Li Huang, Nicolaas Schipper, Thorsteinn Loftsson, Martin Bollmark, Valeria Marigo
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Illuminating Dark Chemical Matter Using the Cell Painting Assay J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Axel Pahl, Jie Liu, Sohan Patil, Soheila Rezaei Adariani, Beate Schölermann, Jens Warmers, Jana Bonowski, Sandra Koska, Yasemin Akbulut, Carina Seitz, Sonja Sievers, Slava Ziegler, Herbert Waldmann
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Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Min Zhao, Neng Ye, Ling Liu, Rui-Jia Zhang, Na Li, Jing Peng, Xiao-Ying Cai, Xue-Qin Jiang, Kai-Yue Su, Xin-Lu Zhang, Qian-Ru Rao, Kong-Jun Liu, De-Xin Deng, Ai-Hua Peng, Ming-Hai Tang, Li-Juan Chen, Wen-Shuang Wu, Hao-Yu Ye
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Discovery of Potent Multikinase Type-II Inhibitors Targeting CDK5 in the DFG-out Inactive State with Promising Potential against Glioblastoma J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Zahra R. Khan, Philip J. Welsby, Izabela Stasik, Joseph M. Hayes
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Multitarget μ-Opioid Receptor Agonists─Neuropeptide FF Receptor Antagonists Induce Potent Antinociception with Reduced Adverse Side Effects J. Med. Chem. (IF 7.3) Pub Date : 2024-04-30 Jolien De Neve, Khadija Elhabazi, Simon Gonzalez, Claire Herby, Séverine Schneider, Valérie Utard, Rosine Fellmann-Clauss, Nathalie Petit-Demouliere, Sandra Lecat, Mélanie Kremer, Aurelia Ces, François Daubeuf, Charlotte Martin, Steven Ballet, Frédéric Bihel, Frédéric Simonin
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Concurrent Optimizations of Efficacy and Blood–Brain Barrier Permeability in New Macrocyclic LRRK2 Inhibitors for Potential Parkinson’s Disease Therapeutics J. Med. Chem. (IF 7.3) Pub Date : 2024-04-29 Kewon Kim, Ahyoung Jang, Hochul Shin, Inhae Ye, Ji Eun Lee, Taeho Kim, Hwangseo Park, Sungwoo Hong
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Exploring Subsite Selectivity within Plasmodium vivax N-Myristoyltransferase Using Pyrazole-Derived Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-04-29 Diego Rodríguez-Hernández, Michael K. Fenwick, Rachael Zigweid, Banumathi Sankaran, Peter J. Myler, Per Sunnerhagen, Alexis Kaushansky, Bart L. Staker, Morten Grøtli
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Identification of Potent and Selective Inhibitors of Acanthamoeba: Structural Insights into Sterol 14α-Demethylase as a Key Drug Target J. Med. Chem. (IF 7.3) Pub Date : 2024-04-29 Tatiana Y. Hargrove, David C. Lamb, Zdzislaw Wawrzak, Marcus Hull, Steven L. Kelly, F. Peter Guengerich, Galina I. Lepesheva
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Discovery of Urea Derivatives of Celastrol as Selective Peroxiredoxin 1 Inhibitors against Colorectal Cancer Cells J. Med. Chem. (IF 7.3) Pub Date : 2024-04-28 Yang Li, Yuyuan Zhu, Fan-Fan Shang, Lin Xu, Defang Jiang, Bin Sun, Lei Zhang, Cheng Luo, Ao Zhang, Hao Zhang, Chunyong Ding
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Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation J. Med. Chem. (IF 7.3) Pub Date : 2024-04-27 Yasheng Zhu, Xiuquan Ye, Yuxing Wu, Hao Shen, Zeyu Cai, Fei Xia, Wenjian Min, Yi Hou, Liping Wang, Xiao Wang, Yibei Xiao, Peng Yang
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Development of Benziodarone Analogues with Enhanced Potency for Selective Binding to Transthyretin in Human Plasma J. Med. Chem. (IF 7.3) Pub Date : 2024-04-26 Mineyuki Mizuguchi, Yusuke Nakagawa, Takeshi Yokoyama, Takuya Okada, Kanako Fujii, Kanoko Takahashi, Nguyen Ngoc Thanh Luan, Yuko Nabeshima, Kayoko Kanamitsu, Shinsaku Nakagawa, Shiori Yamakawa, Mitsuharu Ueda, Yukio Ando, Naoki Toyooka
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Design, Synthesis, and Investigation of the Pharmacokinetics and Anticancer Activities of Indenoisoquinoline Derivatives That Stabilize the G-Quadruplex in the MYC Promoter and Inhibit Topoisomerase I J. Med. Chem. (IF 7.3) Pub Date : 2024-04-26 Yichen Han, Adam Buric, Venkat Chintareddy, Mercedes DeMoss, Luying Chen, Jonathan Dickerhoff, Robyn De Dios, Pooran Chand, Randall Riggs, Danzhou Yang, Mark Cushman
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The C-terminal Region of D-DT Regulates Molecular Recognition for Protein–Ligand Complexes J. Med. Chem. (IF 7.3) Pub Date : 2024-04-26 Andrew Parkins, Aliyah Veronica R. Pilien, Alexander M. Wolff, Christopher Argueta, Jasmine Vargas, Shahrzad Sadeghi, Andreas H. Franz, Michael C. Thompson, Georgios Pantouris
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Design, Synthesis, and Evaluation of Dihydropyrimidine Derivatives as Selective PDE1 Inhibitors for the Treatment of Liver Fibrosis J. Med. Chem. (IF 7.3) Pub Date : 2024-04-26 Zheng-Jiong Zhao, Mei-Yan Jiang, Meng-Xing Huang, Yi-Yi Yang, Ling-Ling Feng, Chen Zhang, Yi-You Huang, Hai-Bin Luo, Yinuo Wu
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Celebrating the 60th Anniversary of the MIKIW Meeting-in-Miniature: Virtual Special Issue J. Med. Chem. (IF 7.3) Pub Date : 2024-04-26 Terry W. Moore, William C. K. Pomerantz
This article references 19 other publications. This article has not yet been cited by other publications. This article references 19 other publications.
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Recent Progress in DNA Damage Response-Targeting PROTAC Degraders J. Med. Chem. (IF 7.3) Pub Date : 2024-04-25 Binbin Cheng, Xiaoting Fei, Zongbao Ding, Xiaopeng Peng, Zhenhong Su, Wei Pan, Jianjun Chen
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Depletion and Downregulation of Hydrogen Sulfide Using an Activatable Probe for Promoting Photothermal Therapy toward Colorectal Cancers J. Med. Chem. (IF 7.3) Pub Date : 2024-04-25 Xuemei Dong, Hongyu Wu, Ziwen Zhang, Jie Sun, Chengjun Dong, Lixin Sun, Rongchen Wang, Xianfeng Gu, Chunchang Zhao
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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