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Minimalist Natural ORPphilin Macarangin B Delineates OSBP Biological Function J. Med. Chem. (IF 6.8) Pub Date : 2024-12-20 Gwenaëlle Jézéquel, Zoé Grimanelli, Carole Guimard, Joëlle Bigay, Juliano Haddad, Jérôme Bignon, Cécile Apel, Vincent Steinmetz, Laurie Askenatzis, Hélène Levaïque, Clara Pradelli, Van Cuong Pham, Doan T. M. Huong, Marc Litaudon, Romain Gautier, Chaker El Kalamouni, Bruno Antonny, Sandy Desrat, Bruno Mesmin, Fanny Roussi
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MoA Studies of the TEAD P-Site Binding Ligand MSC-4106 and Its Optimization to TEAD1-Selective Amide M3686 J. Med. Chem. (IF 6.8) Pub Date : 2024-12-20 Timo Heinrich, Daniel Schwarz, Carl Petersson, Jakub Gunera, Sakshi Garg, Richard Schneider, Marina Keil, Lisa Grimmeisen, Andrea Unzue Lopez, Lisa Albers, Sarah Schlesiger, Alessia Gambardella, Joerg Bomke, Emma Carswell, Heike Schilke, Patrizia Diehl, Benjamin Doerfel, Djordje Musil, Elisabeth Trivier, Rebecca Broome, Sam Marshall, Alexander Balsiger, Erik Friedrich, Ana R. Lemos, Sandra P. Santos
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Identification of Novel Organo-Se BTSA-Based Derivatives as Potent, Reversible, and Selective PPARγ Covalent Modulators for Antidiabetic Drug Discovery J. Med. Chem. (IF 6.8) Pub Date : 2024-12-20 Fangyuan Chen, Qingmei Liu, Lei Ma, Cuishi Yan, Haiman Zhang, Zhi Zhou, Wei Yi
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Identification of Novel Human 15-Lipoxygenase-2 (h15-LOX-2) Inhibitors Using a Virtual Screening Approach J. Med. Chem. (IF 6.8) Pub Date : 2024-12-19 Lucas G. Viviani, Thais S. Iijima, Erika Piccirillo, Leandro Rezende, Thiago G. P. Alegria, Luis Eduardo S. Netto, Antonia T.-do Amaral, Sayuri Miyamoto
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Fluorinated Coumarin Derivatives as Selective PET Tracer for MAO-B Imaging J. Med. Chem. (IF 6.8) Pub Date : 2024-12-19 Nan Wu, Xiaojun Zhang, Yuying Li, Jinming Zhang, Mengchao Cui
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Design, Synthesis, and Biological Evaluation of 2-Arylaminopyrimidine Derivatives as Dual Cathepsin L and JAK Inhibitors for the Treatment of Acute Lung Injury J. Med. Chem. (IF 6.8) Pub Date : 2024-12-19 Chunwei Shen, Zhengtong Mao, Tianpeng Chen, Yingying Wei, Tao Zhou, Ningyuan Zhong, Gaoyang Zhu, Qiwen Shi, Zheyu Xie, Huajun Zhao, Xingxian Zhang
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Identification of an Isoxazole Derivative as an Antitubercular Compound for Targeting the FadD Enzymes of Mycobacterium tuberculosis J. Med. Chem. (IF 6.8) Pub Date : 2024-12-18 Nidhi Rani, Raju S. Rajmani, Avadhesha Surolia
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Eradication of Therapy-Resistant Cancer Stem Cells by Novel Telmisartan Derivatives J. Med. Chem. (IF 6.8) Pub Date : 2024-12-18 Anna M. Schoepf, Maximilian Gebhart, Martin Federspiel, Isabel Heidegger, Martin Puhr, Madlen Hotze, Marcel Kwiatkowski, Andreas Pircher, Dominik Wolf, Sieghart Sopper, Ronald Gust, Stefan Salcher
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Hypoxia Activated Nitric Oxide Donor Compounds for the Prevention and Treatment of Myocardial Hypoxia-Induced Injury J. Med. Chem. (IF 6.8) Pub Date : 2024-12-18 Wanxiang Yang, Wen Zhou, Shaohua Gou
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Impact of Linker Composition on VHL PROTAC Cell Permeability J. Med. Chem. (IF 6.8) Pub Date : 2024-12-18 Yordanos Esubalew Abeje, Lianne H. E. Wieske, Vasanthanathan Poongavanam, Stefanie Maassen, Yoseph Atilaw, Philipp Cromm, Lutz Lehmann, Mate Erdelyi, Daniel Meibom, Jan Kihlberg
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Discovery of N-Trifluoromethylated Noscapines as Novel and Potent Agents for the Treatment of Glioblastoma J. Med. Chem. (IF 6.8) Pub Date : 2024-12-17 Guangwei Cui, Yuhang Fan, Yue Yang, Yiwen Ma, Haiyang Deng, Pan Wang, Yuxin Zhu, Jian Li, Jinlian Wei, Yongqiang Zhang
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Modulating the Potency of BRD4 PROTACs at the Systems Level with Amine-Acid Coupling Reactions J. Med. Chem. (IF 6.8) Pub Date : 2024-12-17 Andrew McGrath, Haiyan Huang, Jean-Francois Brazeau, Zirong Zhang, Christopher O. Audu, Nadeem A. Vellore, Lu Zhu, Zhicai Shi, Jennifer D. Venable, Christine F. Gelin, Tim Cernak
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Pivotal Role of the Intracellular Microenvironment in the High Photodynamic Activity of Cationic Phthalocyanines J. Med. Chem. (IF 6.8) Pub Date : 2024-12-17 Dmitry A. Bunin, Roman A. Akasov, Alexander G. Martynov, Maria P. Stepanova, Svetlana V. Monich, Aslan Yu. Tsivadze, Yulia G. Gorbunova
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Guardians at the Gate: Optimization of Small Molecule Entry Inhibitors of Ebola and Marburg Viruses J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Malaika D. Argade, Jazmin Galván Achi, Ryan Bott, Kimberly M. Morsheimer, Callum D. Owen, Christian A. Zielinski, Arsen M. Gaisin, Mario Alvarez, Terry W. Moore, Fan Bu, Fang Li, Michael Cameron, Manu Anantpadma, Robert A. Davey, Norton P. Peet, Lijun Rong, Irina N. Gaisina
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Structure-Based Development of Novel Spiro-Piperidine ASH1L Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Guang Huang, Rhiannon Stevens, Devon G. Hucek, Trupta Purohit, Shuangjiang Li, Hongzhi Miao, Elise Trost, Geoff Hewett, Bradley Clegg, Se Ra Park, Krishani Rajanayake, Bo Wen, Duxin Sun, Tomasz Cierpicki, Jolanta Grembecka
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Recent Advances of Metal Complexes in the Treatment of Hepatocellular Carcinoma J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Zhongren Xu, Yu Liu, Jiaqi Yang, Fuwei Li, Wukun Liu
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Combinatorial Synthesis toward the Discovery of Highly Cytotoxic Fe(III) Complexes J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Felix Niemeier, Lisa-Marie Servos, Zisis Papadopoulos, Nicolás Montesdeoca, Kaixin Ni, Sascha Heinrich, Johannes Karges
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Precise Carrier-Free Pt(IV)-Nanobombs for Apoptosis/Ferroptosis Synergistic Tumor Therapy: A New Effective Method to Obtain Good Chemotherapy and Low Toxicity J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Xu Guo, Xue-Jiao Liang, Jia-Le Liu, Zhi-Hui Li, Zhihao You, Dandan Zhao, Yali Song, Longfei Li, Xue-Qing Song
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Discovery of N-Phenyl-5-propyl-1H-pyrazole-3-carboxamide, with Selective Inhibition and Degradation of HDAC6 for the Treatment of Acute Liver Injury J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Hao Cui, Guodong Zhang, Liyuan Zhang, Shilong Sun, Kang Yang, Aixin Gen, Penfeng Wang, Hui Wang, Qing-Qing Zhou, Hongmei Li, Yadong Chen, Yuqin Yao, Tao Lu, Lei Zhang, Yong Zhu
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Evaluation of Dynamic Light Scattering as an Effective Quality Control Method for Aggregates in Radiolabeled Antibodies J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Huu Bao Nguyen, Hyun Park, Jeong Eun Lim, Thuy Tien Nguyen, Hwan Hui Kim, Kyeongwon Kim, Jung Young Kim, Kyo Chul Lee, Jeongsoo Yoo
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Antibody-Vincristine Conjugates as Potent Anticancer Therapeutic Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Agathe Boos, Julien Most, Héloïse Cahuzac, Louis Moreira da Silva, François Daubeuf, Stéphane Erb, Sarah Cianférani, Oscar Hernandez-Alba, Constantin Semenchenko, Igor Dovgan, Sergii Kolodych, Alexandre Detappe, Françoise Dantzer, Alain Wagner, Maria Zeniou, Guilhem Chaubet
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Design, Synthesis, and Biochemical Evaluation of Novel MLK3 Inhibitors: A Target Hopping Example J. Med. Chem. (IF 6.8) Pub Date : 2024-12-16 Pascal Sander, Martin P. Schwalm, Andreas Krämer, Lewis Elson, Alexander Rasch, Benedikt Masberg, Roland Selig, Adrian Sievers-Engler, Michael Lämmerhofer, Susanne Müller, Stefan Knapp, Wolfgang Albrecht, Stefan A. Laufer
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In Silico Enabled Discovery of KAI-11101, a Preclinical DLK Inhibitor for the Treatment of Neurodegenerative Disease and Neuronal Injury J. Med. Chem. (IF 6.8) Pub Date : 2024-12-13 H. Rachel Lagiakos, Yefen Zou, Hideyuki Igawa, Eric Therrien, Morgan Lawrenz, Mitsunori Kato, Mats Svensson, Felicia Gray, Kristian Jensen, Markus K. Dahlgren, Robert D. Pelletier, Karen Dingley, Jeffrey A. Bell, Zhijian Liu, Yuansong Jiang, Hua Zhou, Robert J. Skene, Zhe Nie
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A Putative Frizzled 7-Targeting Compound Acts as a Firefly Luciferase Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-12-13 Julia Kinsolving, Lukas Grätz, Jan Hendrik Voss, Bente Löw, Emily Shorter, Baptiste Jude, Johanna T Lanner, Stefan Löber, Peter Gmeiner, Gunnar Schulte
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Journal of Medicinal Chemistry Collection: Drug Discovery in Italy J. Med. Chem. (IF 6.8) Pub Date : 2024-12-13 Antonella Ciancetta, Maria Laura Bolognesi
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Discovery of a Novel Mutant-Selective Epidermal Growth Factor Receptor Inhibitor Using an In Silico Enabled Drug Discovery Platform J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Hideyuki Igawa, Zef A. Konst, Eric Therrien, Mee Shelley, Heidi Koldsø, Pieter H. Bos, Ana Negri, Andreas Verras, Jiaye Guo, Markus K. Dahlgren, Adam Levinson, Brendan T. Parr, Suresh E. Kurhade, Prashant Latthe, Rajesha Shetty, Sridhar Santhanakrishnan, Katherine Amberg-Johnson, Alan S. Futran, Christian Atsriku, Robert D. Pelletier, Zhijian Liu, Jeffrey A. Bell, Sathesh Bhat, Mats Svensson, Aleksey
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Preferential Synaptic Type of GABA-A Receptor Ligands Enhancing Neuronal Survival and Facilitating Functional Recovery After Ischemic Stroke J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Barbara Mordyl, Nikola Fajkis-Zajączkowska, Katarzyna Szafrańska, Agata Siwek, Monika Głuch-Lutwin, Paweł Żmudzki, Jakub Jończyk, Tadeusz Karcz, Karolina Słoczyńska, Elżbieta Pękala, Bartosz Pomierny, Weronika Krzyżanowska, Jakub Jurczyk, Alicja Skórkowska, Aleksandra Sałach, Magdalena Jastrzębska-Więsek, Maria Walczak, Maciej Tadeusz Gawlik, Magdalena Smolik, Marcin Kolaczkowski, Monika Marcinkowska
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Development and Characterization of a High-Affinity Selective Galectin-3 Mouse Tool Compound in Mouse Models of Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Kristoffer Peterson, Ulf J. Nilsson, Lise Gravelle, Ian Holyer, Karl Jansson, Barbro Kahl-Knutson, Hakon Leffler, Alison C. MacKinnon, James A. Roper, Robert J. Slack, Henrik von Wachenfeldt, Anders Pedersen, Fredrik R. Zetterberg
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Deciphering the Comprehensive Structure–Activity Relationship of Sunshinamide for Breast Cancer Therapy through Dual Modulation of Apoptotic and Ferroptotic Pathways via TrxR1 and Gpx4 Inhibition J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Akash Chatterjee, Joyanta Mondal, Subhojit Paul, Himangshu Sharma, Rajib Kumar Goswami, Prosenjit Sen
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Correction to “NN1213 – A Potent, Long-Acting, and Selective Analog of Human Amylin” J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Kirsten Dahl, Kirsten Raun, Jakob Lerche Hansen, Christian Poulsen, Charlotta D. de la Cour, Trine Ryberg Clausen, Ann Maria Kruse Hansen, Linu M. John, Annette Plesner, Gao Sun, Morten Schlein, Rikke Bjerring Skyggebjerg, Thomas Kruse
Correction: The following paragraph previously on page 11691 is now the footnote for Table 12 on page 11693. “Data are mean ± SEM measured as percent food intake relative to vehicle in rats after a single sc injection of 30 nmol/kg of the test substance. Data for cagrilintide have been published previously7 giving rise to 85% and 84% reduction of food intake in the periods from 0–24 h and 24–48 h,
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Toward Dose Prediction at Point of Design J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Dries Van Rompaey, Siladitya Ray Chaudhuri, Mazen Ahmad, Justin Cisar, An Van Den Bergh, Jeremy Ash, Zhe Wu, Marian C. Bryan, James P. Edwards, Renee DesJarlais, Jörg Kurt Wegner, Hugo Ceulemans, Kaushik Mitra, David Polidori
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Overcoming Resistance to FLT3-ITD Therapeutics J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Campbell McInnes
FLT3-ITD (internal tandem duplication) is a key driver of acute myeloid leukemia (AML), and several FDA-approved drugs target this mutant kinase. This Viewpoint describes the discovery of inhibitors targeting point mutants and the development of SILA123, a highly potent and selective type II FLT3 inhibitor. In in vivo studies, SILA-123 significantly suppressed tumor growth in allograft models, demonstrating
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Discovery of VU6024578/BI02982816: An MGlu1 Positive Allosteric Modulator with Efficacy in Preclinical Antipsychotic and Cognition Models J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Carson W. Reed, Jacob F. Kalbfleisch, Jeremy A. Turkett, Trevor A. Trombley, Anthony F. Nastase, Paul K. Spearing, Daniel H. Haymer, Mohammad Moshin Sarwar, Marc Quitalig, Jonathan W. Dickerson, Annie L. Blobaum, Olivier Boutaud, Patrizia Voehringer, Niklas Schuelert, Hyekyung P. Cho, Colleen M. Niswender, Jerri M. Rook, Henning Priepke, Daniel Ursu, P. Jeffrey Conn, Bruce J. Melancon, Craig W. Lindsley
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Correction to “Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005” J. Med. Chem. (IF 6.8) Pub Date : 2024-12-12 Patrick Papa, Brandon Whitefield, Deborah S. Mortensen, Dan Cashion, Dehua Huang, Eduardo Torres, Jason Parnes, John Sapienza, Joshua Hansen, Matthew Correa, Mercedes Delgado, Roy Harris, Sayee Hegde, Stephen Norris, Sogole Bahmanyar, Veronique Plantevin-Krenitsky, Zheng Liu, Katerina Leftheris, Ashutosh Kulkarni, Brydon Bennett, Eun Mi Hur, Garth Ringheim, Godrej Khambatta, Henry Chan, Jeffrey Muir
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Probing the Biomolecular Interactions of DNA/HSA with the New Sn(IV) Complex and Computational Perspectives: Design, Synthesis, Characterization, Anticancer Activity, and Molecular Modeling Approach J. Med. Chem. (IF 6.8) Pub Date : 2024-12-11 Manal Shamsi, Waddhaah M. Al-Asbahy, Hakim Q. N. Al-Areqi, Fahad A. M. Alzowahi
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Discovery of Novel Thiophene-Based Baloxavir Derivatives as Potent Cap-Dependent Endonuclease Inhibitors for Influenza Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-12-10 Yongzhi Chen, Kunyu Lu, Binhao Rong, Yuanmei Wen, Guanguan Li, Shuo Li, Deyin Guo, Qifan Zhou, Shuwen Liu, Xumu Zhang
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Redesigning Berberines and Sanguinarines to Target Soluble Epoxide Hydrolase for Enhanced Anti-Inflammatory Efficacy J. Med. Chem. (IF 6.8) Pub Date : 2024-12-10 Xing-Zhou Liu, Xiao-Yu Du, Wei-Song Xie, Jing Ding, Min-Zhen Zhu, Zi-Qiang Feng, Hao Wang, Yue Feng, Ming-Jia Yu, Si-Meng Liu, Wen-Tian Liu, Xin-Hong Zhu, Jian-Hua Liang
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Erlotinib-Gold(I) Complex Induces Leukemia Cell DC Differentiation and Remodels the Immunosuppressive Microenvironment J. Med. Chem. (IF 6.8) Pub Date : 2024-12-10 Xiaoxuan Yu, Yanyu Zhou, Xiaoyan Ma, Wan Zhang, Fuwei Li, Fengyu Jiang, Yawen Wang, Qin Zhang, Wukun Liu
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Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-12-10 Jeffrey W. Johannes, Amber Y. S. Balazs, Derek Barratt, Michal Bista, Matthew D. Chuba, Sabina Cosulich, Susan E. Critchlow, Sébastien L. Degorce, Paolo Di Fruscia, Scott D. Edmondson, Kevin J. Embrey, Stephen Fawell, Avipsa Ghosh, Sonja J. Gill, Anders Gunnarsson, Sudhir M. Hande, Tom D. Heightman, Paul Hemsley, Giuditta Illuzzi, Jordan Lane, Carrie J.B. Larner, Elisabetta Leo, Lina Liu, Andrew Madin
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Constrained β-Hairpins Targeting the EphA4 Ligand Binding Domain J. Med. Chem. (IF 6.8) Pub Date : 2024-12-10 Anne Marie Prentiss, Carlo Baggio, James Pagett, Anna O. Kulinich, Iryna M. Ethell, Kendall Muzzarelli, Zahra Assar, Maurizio Pellecchia
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Experimental and Computational Studies on Domain-Swapped Structure Stabilization of an Antibody Light Chain by Disulfide Bond Introduction J. Med. Chem. (IF 6.8) Pub Date : 2024-12-10 Wahyu Fitriana, Takahiro Sakai, Lian Duan, Kowit Hengphasatporn, Yasuteru Shigeta, Tsuyoshi Mashima, Taizo Uda, Emi Hifumi, Shun Hirota
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Move over COVID, Tuberculosis Is Once again the Leading Cause of Death from a Single Infectious Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-12-09 Tomayo Berida, Craig W. Lindsley
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Enhancing COVID-19 Vaccine Efficacy: Dual Adjuvant Strategies with TLR7/8 Agonists and Glycolipids J. Med. Chem. (IF 6.8) Pub Date : 2024-12-09 Ke Li, Xing Hu, Xin-Yi Tu, Mao-Ying Xian, Lei-Lei Huang, Ting Huang, Rui Luo, Hui Jin, Zheng Liu
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Targeting HMGB1 and Its Interaction with Receptors: Challenges and Future Directions J. Med. Chem. (IF 6.8) Pub Date : 2024-12-09 Pingping Shen, Libang Zhang, Xuewa Jiang, Boyang Yu, Jian Zhang
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Discovery of PF-07265028, A Selective Small Molecule Inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1) for the Treatment of Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-12-09 Rebecca A. Gallego, Sujin Cho-Schultz, Matthew Del Bel, Anne-Marie Dechert-Schmitt, Joyann S. Donaldson, Mingying He, Mehran Jalaie, Rob Kania, Jean Matthews, Michele McTigue, Jamison B. Tuttle, Hud Risley, Dahui Zhou, Ru Zhou, Omar K. Ahmad, Louise Bernier, Simon Berritt, John Braganza, Zecheng Chen, Julie A. Cianfrogna, Michael Collins, Cinthia Costa Jones, Ciaran N. Cronin, Carl Davis, Klaus Dress
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Modulating Phosphorylation by Proximity-Inducing Modalities for Cancer Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-12-09 Qiuyue Zhang, Jia Yu, Qidong You, Lei Wang
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Current Status and Perspectives of Novel Radiopharmaceuticals with Heterologous Dual-targeted Functions: 2013–2023 J. Med. Chem. (IF 6.8) Pub Date : 2024-12-08 Zuojie Li, Qing Ruan, Yuhao Jiang, Qianna Wang, Guangxing Yin, Junhong Feng, Junbo Zhang
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Development of a New Vaccine Adjuvant System Based on the Combination of the Synthetic TLR4 Agonist FP20 and a Synthetic QS-21 Variant J. Med. Chem. (IF 6.8) Pub Date : 2024-12-08 Mohammed Monsoor Shaik, Samuel Pasco, Alessio Romerio, Carlo Pifferi, Silvia Sesana, Francesca Re, Charl Xavier Bezuidenhout, Silvia Bracco, Alberto Fernandez-Tejada, Juan Anguita, Francesco Peri
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Elaborate Structural Modifications Yielding Novel Boron-Containing N-Substituted Oseltamivir Derivatives as Potent Neuraminidase Inhibitors with Significantly Improved Broad-Spectrum Antiresistance Profiles J. Med. Chem. (IF 6.8) Pub Date : 2024-12-07 Jiwei Zhang, Ruifang Jia, Huinan Jia, Ping Li, Yuanmin Jiang, Anna Bonomini, Chiara Bertagnin, Qiaojie Xu, Zhou Tan, Xiuli Ma, Arianna Loregian, Bing Huang, Xinyong Liu, Peng Zhan
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Discovery of Novel MyD88 Inhibitor A5S to Alleviate Acute Lung Injury with Favorable Drug-like Properties J. Med. Chem. (IF 6.8) Pub Date : 2024-12-07 Pan Chen, Yu Zou, Xiemin Wang, Zhichao Chen, Ke Dong, Jun Yang, Yaqian Cui, Jing Gu, Xinyi Wu, Xiaobo Li, Ying Zhou, Mi Guo, Zhiwei Zheng, Qi Chen, Weiwei Zhu, Di Wu, Lina Yin, Lingfeng Chen, Qin Ouyang, Guang Liang, Qidong Tang
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Structure-Based Discovery of a Series of Covalent, Orally Bioavailable, and Selective BFL1 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-12-06 Adeline Palisse, Tony Cheung, Aileen Blokhuis, Thomas Cogswell, Bruna S. Martins, Rick Riemens, Rick Schellekens, Giovanni Battocchio, Chimed Jansen, Matthew A. Cottee, Kimberly Ornell, Claudia Sacchetto, Leonardo Leon, Maaike van Hoek- Emmelot, Mark Bostock, Brooke Leann Brauer, Kevin Beaumont, Simon C. C. Lucas, Samiyah Ahmed, J. Henry Blackwell, Ulf Börjesson, Andrea Gohlke, Iva Monique T. Gramatikov
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Discovery of a Novel Non-invasive AR PROTAC Degrader for the Topical Treatment of Androgenetic Alopecia J. Med. Chem. (IF 6.8) Pub Date : 2024-12-06 Xinfei Mao, Weitong Hu, Mingfei Wu, Yuyuan Jin, Jingyi Zhao, Yihua Xu, Bizhi Li, Wentao Wang, Yiquan Wu, Jingyu Zhang, Ao Pang, Yuheng Jin, Tianyuan Zhang, Wenhai Huang, Jinxin Che, Jianqing Gao, Xiaowu Dong
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Discovery of MT-7117 (Dersimelagon Phosphoric Acid): A Novel, Potent, Selective, and Nonpeptidic Orally Available Melanocortin 1 Receptor Agonist J. Med. Chem. (IF 6.8) Pub Date : 2024-12-06 Atsushi Sato, Kenji Morokuma, Takashi Adachi, Junki Andou, Masahiko Miyashiro, Tsuyoshi Suzuki, Yuko Kawano, Masahiro Kondo, Akihito Ogasawara, Mika Ide, Yasuo Yamamoto
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Selectively Antagonizing the NOD1-Mediated Inflammatory Signaling Pathway Mitigates the Gastric Inflammation Induced by Helicobacter pylori Infection J. Med. Chem. (IF 6.8) Pub Date : 2024-12-05 Xinhua Liu, Dan Wang, Xiduan Wei, Dan Yang, Yao Ma, Gang Liu
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Improving the Stability and Anti-Infective Activity of Sea Turtle AMPs Using Multiple Structural Modification Strategies J. Med. Chem. (IF 6.8) Pub Date : 2024-12-05 Zifan Ye, Zhouye Xu, Jianhong Ouyang, Wenzhuang Shi, Shuangyu Li, Xu Wang, Binjuan Lu, Kang Wang, Yipeng Wang
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Discovery of CHF-6523, an Inhaled Selective PI3Kδ Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-12-05 Paolo Bruno, Daniele Pala, Alessandra Micoli, Mauro Corsi, Alessandro Accetta, Laura Carzaniga, Paolo Ronchi, Claudio Fiorelli, Michele Formica, Daniela Pizzirani, Roberta Mazzucato, Sara Guariento, Serena Bertolini, Cataldo Martucci, Andrew Dennis Allen, Valentina Mileo, Silvia Capacchi, Paola Maria Gallo, Alessandro Fioni, Sergio Xanxo Fernandez, Gino Villetti, Paola Puccini, Maurizio Civelli, Matilde
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Discovery and Optimization of Dihydroquinolin-2(1H)-ones as Novel Highly Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension J. Med. Chem. (IF 6.8) Pub Date : 2024-12-05 Bei Zhang, Zhong-Kai Zou, Jian-Fan Cai, Wen-Ming Tan, Jun-Wei Chen, Wei-En Li, Jing-Nan Liang, Wei-Pei Wu, Gang Wang, Xiao-Hong Ruan, Pei-Liang Zhao
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An Activatable Heavy-Atom-Free Upconversion Photosensitizer for Targeted Imaging and Treatment of Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-12-05 Chao Zhao, Wanlu Sun, Yanyan Zhu, Xiaoyan Huang, Ye Sun, Hai-Yan Wang, Yi Pan, Yi Liu
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Discovery of ART0380, a Potent and Selective ATR Kinase Inhibitor Undergoing Phase 2 Clinical Studies for the Treatment of Advanced or Metastatic Solid Cancers J. Med. Chem. (IF 6.8) Pub Date : 2024-12-04 Christopher L. Carroll, Michael G. Johnson, Yanbing Ding, Zhijun Kang, R. S. K. Vijayan, Jennifer P. Bardenhagen, Cheng Fang, David Lapointe, Meng Li, Chiu-Yi Liu, Xiaobing Lv, XiaoYan Ma, Jihai Pang, Hannah E. Shepard, Catalina Suarez, Anne Ju Yau, Christopher C. Williams, Qi Wu, Robert A. Heald, Helen M. R. Robinson, Graeme C. M. Smith, Jason B. Cross, Mary K. Geck Do, Yongying Jiang, Sarah Lively
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Structure-Guided Discovery of Subtype Selective SIRT6 Inhibitors with a β-Carboline Skeleton for the Treatment of Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-12-04 Chaowei Liang, Siyu Wang, Dongyan Feng, Shenglin Wang, Chao Zheng, Ying Qu, Weirenbo Wang, Yongzhi Ma, Haonan Li, Hangao Yang, Hao Cao, Huiming Hua, Maosheng Cheng, Dahong Li
更新日期：2024-12-20
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