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X-ray Structure-Guided Discovery of a Potent Benzimidazole Glutaminyl Cyclase Inhibitor That Shows Activity in a Parkinson’s Disease Mouse Model J. Med. Chem. (IF 7.3) Pub Date : 2024-05-31 Jun Mou, Xiang-Li Ning, Xin-Yue Wang, Shu-Yan Hou, Fan-Bo Meng, Cong Zhou, Jing-Wei Wu, Chunyan Li, Tao Jia, Xiaoai Wu, Yong Wu, Yongping Chen, Guo-Bo Li
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Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA J. Med. Chem. (IF 7.3) Pub Date : 2024-05-31 Erik J. Hicken, Karin Brown, Natalie C. Dwulet, John J. Gaudino, Erik P. Hansen, Dylan P. Hartley, John P. Kowalski, Ellen R. Laird, Nicholas C. Lazzara, Bin Li, Tung-Chung Mou, Marie F. Mutryn, Lauren Oko, Spencer Pajk, Robert W. Pipal, Rachel Z. Rosen, Russell Shelp, Anurag Singh, Jing Wang, Courtney E. Wise, Christina Wong, Jim Y. Wong
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Newly Designed Quasi-intrinsic Photosensitizers for Fluorescence Image-Guided Two-Photon Photodynamic Therapy with Type I/II Photoreactions J. Med. Chem. (IF 7.3) Pub Date : 2024-05-30 Xixi Cui, Hongxiu Yuan, Xiaolin Chen, Qingtian Meng, Changzhe Zhang
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Structure-Based Design and Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High Selectivity, Brain Penetration, and In Vivo Efficacy J. Med. Chem. (IF 7.3) Pub Date : 2024-05-31 Faridoon, Jiyue Zheng, Tao Zhang, Shuilong Tong, Tao Liu, Jiuen Cui, Haojie Xu, Di Hu, Ying Shen, Yajing Yin, Danhua Zhao, Chensheng Tan, Xue Dong, Jiali Chen, Feihong Ji, Chenhua Tong, Jie Jack Li, Jiapeng Li, Guiping Zhang
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Multiaction Pt(IV) Prodrugs Releasing Cisplatin and Dasatinib Are Potent Anticancer and Anti-Invasive Agents Displaying Synergism between the Two Drugs J. Med. Chem. (IF 7.3) Pub Date : 2024-05-31 Lenka Markova, Moumita Maji, Hana Kostrhunova, Vojtech Novohradsky, Jana Kasparkova, Dan Gibson, Viktor Brabec
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Systematic Structure–Activity Relationship Study of Nalfurafine Analogues toward Development of Potentially Nonaddictive Pain Management Treatments J. Med. Chem. (IF 7.3) Pub Date : 2024-05-30 Celsey M. St. Onge, Piyusha P. Pagare, Yi Zheng, Michelle Arriaga, David L. Stevens, Rolando E. Mendez, Justin L. Poklis, Matthew S. Halquist, Dana E. Selley, William L. Dewey, Matthew L. Banks, Yan Zhang
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A Unique Hybridization Route to Access Hydrazylnaphthalimidols as Novel Structural Scaffolds of Multitargeting Broad-Spectrum Antifungal Candidates J. Med. Chem. (IF 7.3) Pub Date : 2024-05-30 Jin-Xin Wang, Peng-Li Zhang, Lavanya Gopala, Jing-Song Lv, Jian-Mei Lin, Cheng-He Zhou
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Design, Synthesis, and Structure–Activity Relationships of Novel Peptide Derivatives of the Severe Acute Respiratory Syndrome-Coronavirus-2 Spike-Protein that Potently Inhibit Nicotinic Acetylcholine Receptors J. Med. Chem. (IF 7.3) Pub Date : 2024-05-30 Arik J. Hone, Ulises Santiago, Peta J. Harvey, Bassel Tekarli, Joanna Gajewiak, David J. Craik, Carlos J. Camacho, J. Michael McIntosh
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Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Hao Wu, Jeremy Murray, Noriko Ishisoko, Alexandra Frommlet, Gauri Deshmukh, Antonio DiPasquale, Melinda M. Mulvihill, Donglu Zhang, John G. Quinn, Robert A. Blake, Wayne J. Fairbrother, Jakob Fuhrmann
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Discovery of Novel ERα and Aromatase Dual-Targeting PROTAC Degraders to Overcome Endocrine-Resistant Breast Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Lilan Xin, Chao Wang, Yan Cheng, Hongli Wang, Xinyi Guo, Xiaofei Deng, Xiangping Deng, Baohua Xie, Hankun Hu, Chang Min, Chune Dong, Hai-Bing Zhou
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Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Loan Y. Vu, Dan Luo, Kai Johnson, Emily D. Denehy, Judy C. Songrady, Jocelyn Martin, Riya Trivedi, Alexia R. Alsum, Jakob D. Shaykin, Chhabi L. Chaudhary, Eric J. Woloshin, Lindsay Kornberger, Nazmul Bhuiyan, Sean Parkin, Qianru Jiang, Tao Che, Warren Alilain, Jill R. Turner, Michael T. Bardo, Thomas E. Prisinzano
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2-Aryl-1H-imidazo[4,5-f][1,10]phenanthroline-Based Binuclear Ru(II)/Ir(III)/Re(I) Complexes as Mitochondria Targeting Cancer Stem Cell Therapeutic Agents# J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Binoy Kar, Shanooja Shanavas, Arun Karmakar, Apoorva H. Nagendra, Seshu Vardhan, Suban K Sahoo, Bipasha Bose, Subrata Kundu, Priyankar Paira
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Discovery of Novel Non-Nucleoside Inhibitors Interacting with Dizinc Ions of CD73 J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Cunjian Shi, Longfeng Chang, Jie Wang, Jingqi Dai, Wenyue Xu, Jiangyang Tang, Wenyi Mei, Chen Zhang, Zedong Wang, Yichen Liao, Xingsen Zhang, Wenzhe Jiang, Guozhen Zhang, Zhenjiang Zhao, Yufang Xu, Lili Zhu, Honglin Li
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Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure J. Med. Chem. (IF 7.3) Pub Date : 2024-05-29 Jeremy M. Richter, Prashantha Gunaga, Navnath Yadav, Rajesh Onkardas Bora, Rajeev Bhide, Nagendra Rajugowda, Kavitha Govindrajulu, Sreenivasulu Godesi, Nagarjuna Akuthota, Prasanna Rao, Aneesh Sivaraman, Manoranjan Panda, Mahammed Kaspady, Anuradha Gupta, Arvind Mathur, Paul C. Levesque, Jyoti Gulia, Manoj Dokania, Manjunath Ramarao, Prashant Kole, Silvi Chacko, Kimberley A. Lentz, Sankara Sivaprasad
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Discovery and Optimization of N-Arylated Tetracyclic Dicarboximides That Target Primary Glioma Stem-like Cells J. Med. Chem. (IF 7.3) Pub Date : 2024-05-28 Hua-Yu Wang, Thu P. Nguyen, Alex C. Sternisha, Christopher L. Carroll, Bethany Cross, Lorraine Morlock, Noelle S. Williams, Samuel McBrayer, Deepak Nijhawan, Jef K. De Brabander
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Discovery of ITI-333, a Novel Orally Bioavailable Molecule Targeting Multiple Receptors for the Treatment of Pain and Other Disorders J. Med. Chem. (IF 7.3) Pub Date : 2024-05-28 Peng Li, Qiang Zhang, Hailin Zheng, Yupu Qiao, Gretchen L. Snyder, Terry Martin, Wei Yao, Lei Zhang, Robert E. Davis
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Discovery of the Selective and Orally Available Galectin-1 Inhibitor GB1908 as a Potential Treatment for Lung Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-28 Fredrik R. Zetterberg, Kristoffer Peterson, Ulf J. Nilsson, Kajsa Andréasson Dahlgren, Carl Diehl, Ian Holyer, Maria Håkansson, Areej Khabut, Barbro Kahl-Knutson, Hakon Leffler, Alison C. MacKinnon, James A. Roper, Robert J. Slack, Reihaneh Zarrizi, Anders Pedersen
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Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases J. Med. Chem. (IF 7.3) Pub Date : 2024-05-28 Oscar Mammoliti, Sébastien Martina, Pieter Claes, Ghjuvanni Coti, Roland Blanque, Catherine Jagerschmidt, Kenji Shoji, Monica Borgonovi, Steve De Vos, Florence Marsais, Line Oste, Evelyne Quinton, Miriam López-Ramos, David Amantini, Reginald Brys, Juan-Miguel Jimenez, René Galien, Steven van der Plas
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Chb-M′, an Inhibitor of the RUNX Family Binding to DNA, Induces Apoptosis in p53-Mutated Non-Small Cell Lung Cancer and Inhibits Tumor Growth and Repopulation In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-05-27 Yuki Hirose, Shinsuke Sato, Kaori Hashiya, Mitsuharu Ooga, Toshikazu Bando, Hiroshi Sugiyama
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Discovery of 3-((4-Benzylpyridin-2-yl)amino)benzamides as Potent GPR52 G Protein-Biased Agonists J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 Ryan E. Murphy, Pingyuan Wang, Saghir Ali, Hudson R. Smith, Daniel E. Felsing, Haiying Chen, Jia Zhou, John A. Allen
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Correction to “Unleashing the Potential of Camptothecin: Exploring Innovative Strategies for Structural Modification and Therapeutic Advancements” J. Med. Chem. (IF 7.3) Pub Date : 2024-05-22 Zheng Chen, Maoyu Liu, Ningyu Wang, Wenjing Xiao, Jianyou Shi
Page 3260. The structure of VIP236 (44) was incorrect in Figure 6. The corrected structure is shown here: Pages 3265 and 3266. In section 4.3.3, the payload released by VIP236 (44) was identified incorrectly; it is 21 and neither 19 nor 45 as written in the text on these pages. Three paragraphs in that section should be revised as follows: And VIP236 (44, Figure 6) is a SMDC that utilized an αvβ3 integrin-targeting
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Cyanomethylquinolones as a New Class of Potential Multitargeting Broad-Spectrum Antibacterial Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 Yi-Min Tan, Jing Zhang, Yu-Jia Wei, Yue-Gao Hu, Shu-Rui Li, Shao-Lin Zhang, Cheng-He Zhou
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Design, Synthesis, and Biological Evaluation of New 2,6,7-Substituted Purine Derivatives as Toll-like Receptor 7 Agonists for Intranasal Vaccine Adjuvants J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 Morgan Kim, Kyungseob Noh, Pyeongkeun Kim, Jae Ho Kim, Byeong Wook Choi, Ravi Singh, Junho Choi, Soo Bong Han, Seong Soon Kim, Eun-Young Lee, Myung Ae Bae, Daeho Shin, Meehyein Kim, Jin Hee Ahn
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Emerging Targets and Therapeutics in Immuno-Oncology: Insights from Landscape Analysis J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 Kavita A. Iyer, Julian Ivanov, Rumiana Tenchov, Krittika Ralhan, Yacidzohara Rodriguez, Janet M. Sasso, Sabina Scott, Qiongqiong Angela Zhou
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Structure-Based Design of a Potent and Selective YTHDC1 Ligand J. Med. Chem. (IF 7.3) Pub Date : 2024-05-24 František Zálešák, Francesco Nai, Marcin Herok, Elena Bochenkova, Rajiv K. Bedi, Yaozong Li, Francesco Errani, Amedeo Caflisch
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Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Fernando H. de Souza Gama, Luiz A. Dutra, Michael Hawgood, Caio Vinícius dos Reis, Ricardo A. M. Serafim, Marcos A. Ferreira, Jr., Bruno V. M. Teodoro, Jéssica Emi Takarada, André S. Santiago, Dimitrios-Ilias Balourdas, Ann-Sofie Nilsson, Bruno Urien, Vitor M. Almeida, Carina Gileadi, Priscila Z. Ramos, Anita Salmazo, Stanley N. S. Vasconcelos, Micael R. Cunha, Susanne Mueller, Stefan Knapp, Katlin
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Construction of 5-Fluorouracil and Gallium Corrole Conjugates for Enhanced Photodynamic Therapy J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Jing-He Cen, Qi-Hu Xie, Geng-Hong Guo, Shi-Yin Xu, Ze-Yu Liu, Yu-Hui Liao, Xiao-Ping Zhong, Hai-Yang Liu
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In Silico Assisted Identification, Synthesis, and In Vitro Pharmacological Characterization of Potent and Selective Blockers of the Epilepsy-Associated KCNT1 Channel J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Nunzio Iraci, Lidia Carotenuto, Tania Ciaglia, Giorgio Belperio, Francesca Di Matteo, Ilaria Mosca, Giusy Carleo, Manuela Giovanna Basilicata, Paolo Ambrosino, Rita Turcio, Deborah Puzo, Giacomo Pepe, Isabel Gomez-Monterrey, Maria Virginia Soldovieri, Veronica Di Sarno, Pietro Campiglia, Francesco Miceli, Alessia Bertamino, Carmine Ostacolo, Maurizio Taglialatela
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Anti-TNF Thioester Glucocorticoid Antibody–Drug Conjugate Fully Inhibits Inflammation with Minimal Effect on Systemic Corticosterone Levels in a Mouse Arthritis Model J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Christopher C. Marvin, Adrian D. Hobson, Michael J. McPherson, Martin E. Hayes, Meena V. Patel, Diana L. Schmidt, Tongmei Li, John T. Randolph, Agnieszka K. Bischoff, Julia Fitzgibbons, Lu Wang, Lu Wang, Axel Hernandez, Jr, Ying Jia, Christian A. Goess, Shaughn H. Bryant, Suzanne L. Mathieu, Jianwen Xu
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Site-Specific Antimicrobial Activity of a Dual-Responsive Ciprofloxacin Prodrug J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Catherine L. Ross, Aggie Lawer, Kathleen J. Sircombe, Daniel Pletzer, Allan B. Gamble, Sarah Hook
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Study of the Conformational Dynamics of Prolyl Oligopeptidase by Mass Spectrometry: Lessons Learned J. Med. Chem. (IF 7.3) Pub Date : 2024-05-23 Roos Van Elzen, Anne-Marie Lambeir
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Design of Selective PARP-1 Inhibitors and Antitumor Studies J. Med. Chem. (IF 7.3) Pub Date : 2024-05-22 Yiting Zhang, Xiangqian Li, Fang Liu, Xiaoyi Bai, Xiaochun Liu, Hao Sun, Chenxia Gao, Yuxi Lin, Pan Xing, Jiqiang Zhu, Ruihua Liu, Zemin Wang, Jiajia Dai, Dayong Shi
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Novel Acyl Thiourea-Based Hydrophobic Tagging Degraders Exert Potent Anti-Influenza Activity through Two Distinct Endonuclease Polymerase Acidic-Targeted Degradation Pathways J. Med. Chem. (IF 7.3) Pub Date : 2024-05-22 Xiaoyu Ma, Xueyun Wang, Feifei Chen, Wenting Zou, Junrui Ren, Lilan Xin, Pei He, Jinsen Liang, Zhichao Xu, Chune Dong, Ke Lan, Shuwen Wu, Hai-Bing Zhou
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Development of Penicillin-Based Carbonic Anhydrase Inhibitors Targeting Multidrug-Resistant Neisseria gonorrhoeae J. Med. Chem. (IF 7.3) Pub Date : 2024-05-22 Alessandro Bonardi, Alessio Nocentini, Simone Giovannuzzi, Niccolò Paoletti, Andrea Ammara, Silvia Bua, Nader S. Abutaleb, Abdallah S. Abdelsattar, Clemente Capasso, Paola Gratteri, Daniel P. Flaherty, Mohamed N. Seleem, Claudiu T. Supuran
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Discovery of Novel p53-MDM2 Inhibitor (RG7388)-Conjugated PlatinumIV Complexes as Potent Antitumor Agents J. Med. Chem. (IF 7.3) Pub Date : 2024-05-22 Wei Liu, Yi Ma, Youyou He, Yanhong Liu, Zhongjie Guo, Jin He, Xiaodong Han, Yujiao Hu, Muqiong Li, Ru Jiang, Shengzheng Wang
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Thiosemicarbazone Mixed-Valence Cu(I/II) Complex against Lung Adenocarcinoma Cells through Multiple Pathways Involving Cuproptosis J. Med. Chem. (IF 7.3) Pub Date : 2024-05-22 Aili Li, Kai Huang, Weiping Pan, Youru Wu, Yuwei Liang, ZhenLei Zhang, Daqi Wu, Libing Ma, Yi Gou
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Secondary Structure Stabilization of Macrocyclic Antimicrobial Peptides via Cross-Link Swapping J. Med. Chem. (IF 7.3) Pub Date : 2024-05-21 Nauman Nazeer, Navjote Kooner, Anupama Ghimire, Jan K. Rainey, William D. Lubell, Deniz Meneksedag-Erol, Marya Ahmed
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Metallacarboranes in Medicinal Chemistry: Current Advances and Future Perspectives J. Med. Chem. (IF 7.3) Pub Date : 2024-05-21 Michalina Gos, Jakub Cebula, Tomasz M. Goszczyński
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Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations J. Med. Chem. (IF 7.3) Pub Date : 2024-05-21 Clare Thomson, Peter Barton, Erin Braybrooke, Nicola Colclough, Zhiqiang Dong, Laura Evans, Nicolas Floc’h, Carine Guérot, David Hargreaves, Puneet Khurana, Songlei Li, Xiuwei Li, Andrew Lister, William McCoull, Lisa McWilliams, Jonathan P. Orme, Martin J. Packer, Aisha M. Swaih, Richard A. Ward, Poppy Winlow, Yang Ye
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Copper(II) Complexes with Isomeric Morpholine-Substituted 2-Formylpyridine Thiosemicarbazone Hybrids as Potential Anticancer Drugs Inhibiting Both Ribonucleotide Reductase and Tubulin Polymerization: The Morpholine Position Matters J. Med. Chem. (IF 7.3) Pub Date : 2024-05-21 Miljan N. M. Milunovic, Katerina Ohui, Iuliana Besleaga, Tatsiana V. Petrasheuskaya, Orsolya Dömötör, Éva A. Enyedy, Denisa Darvasiova, Peter Rapta, Zuzana Barbieriková, Daniel Vegh, Szilárd Tóth, Judit Tóth, Nóra Kucsma, Gergely Szakács, Ana Popović-Bijelić, Ayesha Zafar, Jóhannes Reynisson, Anatoly D. Shutalev, Ruoli Bai, Ernest Hamel, Vladimir B. Arion
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Discovery of Quinazoline and Quinoline-Based Small Molecules as Utrophin Upregulators via AhR Antagonism for the Treatment of Duchenne Muscular Dystrophy J. Med. Chem. (IF 7.3) Pub Date : 2024-05-21 Surojit Ghosh, Mohammad Umar Arshi, Satyajit Ghosh, Moumita Jash, Samya Sen, Kamel Mamchaoui, Sudipta Bhattacharyya, Nirmal Kumar Rana, Surajit Ghosh
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Thermodynamics-Guided Design Reveals a Cooperative Hydrogen Bond in DC-SIGN-targeted Glycomimetics J. Med. Chem. (IF 7.3) Pub Date : 2024-05-21 Dilara D. Nemli, Xiaohua Jiang, Roman P. Jakob, Laura Muñoz Gloder, Oliver Schwardt, Said Rabbani, Timm Maier, Beat Ernst, Jonathan Cramer
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Development of Novel Phosphonodifluoromethyl-Containing Phosphotyrosine Mimetics and a First-In-Class, Potent, Selective, and Bioavailable Inhibitor of Human CDC14 Phosphatases J. Med. Chem. (IF 7.3) Pub Date : 2024-05-20 Jiajun Dong, Brenson A. Jassim, Kedric L. Milholland, Zihan Qu, Yunpeng Bai, Yiming Miao, Jinmin Miao, Yuan Ma, Jianping Lin, Mark C. Hall, Zhong-Yin Zhang
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Structure-Based Optimization of Novel Sterol 24-C-Methyltransferase Inhibitors for the Treatment of Candida albicans Infections J. Med. Chem. (IF 7.3) Pub Date : 2024-05-19 Xue Wang, Xueyang Jin, Fabao Zhao, Zejun Xu, Wenzhuo Tan, Jiaozhen Zhang, Yuliang Xu, Xiaoyi Luan, Min Fang, Zhiyu Xie, Wenqiang Chang, Hongxiang Lou
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An Improved PDE6D Inhibitor Combines with Sildenafil To Inhibit KRAS Mutant Cancer Cell Growth J. Med. Chem. (IF 7.3) Pub Date : 2024-05-17 Pelin Kaya, Elisabeth Schaffner-Reckinger, Ganesh babu Manoharan, Vladimir Vukic, Alexandros Kiriazis, Mirko Ledda, Maria Burgos Renedo, Karolina Pavic, Anthoula Gaigneaux, Enrico Glaab, Daniel Kwaku Abankwa
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1,4-Disubstituted Piperazin-2-Ones as Selective Late Sodium Current Inhibitors with QT Interval Shortening Properties in Isolated Rabbit Hearts J. Med. Chem. (IF 7.3) Pub Date : 2024-05-17 Hui Yang, Mengqin Jing, Chao Tian, Bingxun Li, Weiming Liao, Wei Wang, Yunzhe Li, Xiaowei Wang, Guifang Duan, Qi Sun, Zhuo Huang, Lin Wu
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WLB-87848, a Selective σ1 Receptor Agonist, with an Unusually Positioned NH Group as Positive Ionizable Moiety and Showing Neuroprotective Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-05-16 Ute Christmann, Lourdes Garriga, Ana Virginia Llorente, José Luis Díaz, Rosalía Pascual, Magda Bordas, Albert Dordal, Mónica Porras, Sandra Yeste, Raquel F. Reinoso, José Miguel Vela, Carmen Almansa
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Discovery of Novel Azaindoles as Potent and Selective PI3Kδ Inhibitors for Treatment of Multiple Sclerosis J. Med. Chem. (IF 7.3) Pub Date : 2024-05-16 Mengyao Yu, Xian Wang, Yongmei Tang, Longling Wang, Xueping Hu, Qinjie Weng, Jiajia Wang, Sunliang Cui
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Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs J. Med. Chem. (IF 7.3) Pub Date : 2024-05-16 Julian Breidenbach, Rabea Voget, Yaoyao Si, Alexandra Hingst, Tobias Claff, Katharina Sylvester, Valentina Wolf, Vesa Krasniqi, Abibe Useini, Norbert Sträter, Yukino Ogura, Atsushi Kawaguchi, Christa E. Müller, Michael Gütschow
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Diagnosis of Melanoma with 61Cu-Labeled PET Tracer J. Med. Chem. (IF 7.3) Pub Date : 2024-05-16 Szilvia Bunda, Ibolya Kálmán-Szabó, Norbert Lihi, Zita Képes, Dezső Szikra, Judit Peline Szabo, István Timári, Dániel Szücs, Nóra V. May, Gábor Papp, György Trencsényi, Ferenc K. Kálmán
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Discovery and Structure–Activity Relationship of Cadazolid: A First-In-Class Quinoxolidinone Antibiotic for the Treatment of Clostridioides difficile Infection J. Med. Chem. (IF 7.3) Pub Date : 2024-05-16 Georg Rueedi, Philippe Panchaud, Astrid Friedli, Jean-Luc Specklin, Christian Hubschwerlen, Anne-Catherine Blumstein, Patrick Caspers, Michel Enderlin-Paput, Loïc Jacob, Christopher Kohl, Hans H. Locher, Philippe Pfaff, Christine Schmitt, Peter Seiler, Daniel Ritz
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Hit-to-Lead Optimization of the Natural Product Oridonin as Novel NLRP3 Inflammasome Inhibitors with Potent Anti-Inflammation Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Chen He, Junkai Liu, Junda Li, Hongyu Wu, Chenyang Jiao, Xiaotong Ze, Shengtao Xu, Zheying Zhu, Wenjie Guo, Jinyi Xu, Hong Yao
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Rigid Fe(III) Chelate with Phosphonate Pendants: A Stable and Effective Extracellular MRI Contrast Agent J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Ling He, Haiyu Wang, Zuhua Zeng, Lei Zhong, Qingxuan Tang, Junlai Yu, Jia Tian, Tianwei Liu, Jiang Zhu
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Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Marie-Gabrielle Braun, Avi Ashkenazi, Ramsay E. Beveridge, Georgette Castanedo, Heidi Ackerly Wallweber, Maureen H. Beresini, Kevin R. Clark, Tom De Bruyn, Liqiang Fu, Paul Gibbons, Fan Jiang, Susan Kaufman, David Kan, James R. Kiefer, Jean-Philippe Leclerc, Alexandre Lemire, Cuong Ly, Ehud Segal, Jessica Sims, Weiru Wang, Wentao Wei, Liang Zhao, Jacob B. Schwarz, Joachim Rudolph
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Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Hina Andleeb, Roger L. Papke, Clare Stokes, Katrin Richter, Sara M. Herz, Ka Chiang, Siva R. Raju Kanumuri, Abhisheak Sharma, M. Imad Damaj, Veronika Grau, Nicole A. Horenstein, Ganesh A. Thakur
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Identification of Novel Potent NSD2-PWWP1 Ligands Using Structure-Based Design and Computational Approaches J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Luca Carlino, Peter C. Astles, Bryony Ackroyd, Afshan Ahmed, Christina Chan, Gavin W. Collie, Ian L. Dale, Daniel H. O’Donovan, Caroline Fawcett, Paolo di Fruscia, Andrea Gohlke, Xiaoxiao Guo, Jessie Hao-Ru Hsu, Bethany Kaplan, Alexander G. Milbradt, Sarah Northall, Dušan Petrović, Emma L. Rivers, Elizabeth Underwood, Alice Webb
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Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Shuanghu Wang, Zhihua Kong, Yaru Shi, Chuxiao Shao, Wei Wang, Zhenhong Su, Jin Liu, Yingxing Zhou, Xiaoting Fei, Binbin Cheng, Jianjun Chen, Yiyu Lu, Jian Xiao
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Nonclassical Zwitterions as a Design Principle to Reduce Lipophilicity without Impacting Permeability J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Henrik Möbitz, Birger Dittrich, Stephane Rodde, Ross Strang
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Enhancing Molecular Property Prediction through Task-Oriented Transfer Learning: Integrating Universal Structural Insights and Domain-Specific Knowledge J. Med. Chem. (IF 7.3) Pub Date : 2024-05-15 Yanjing Duan, Xixi Yang, Xiangxiang Zeng, Wenxuan Wang, Youchao Deng, Dongsheng Cao