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Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor J. Med. Chem. (IF 7.3) Pub Date : 2024-03-27 Yan Xiong, Holger Greschik, Catrine Johansson, Ludwig Seifert, Vicki Gamble, Kwang-su Park, Vincent Fagan, Fengling Li, Irene Chau, Masoud Vedadi, Cheryl H. Arrowsmith, Paul Brennan, Oleg Fedorov, Manfred Jung, Gillian Farnie, Jing Liu, Udo Oppermann, Roland Schüle, Jian Jin
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Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-03-26 Zhixiang Chen, Mi Wang, Dimin Wu, Lijie Zhao, Hoda Metwally, Wei Jiang, Yu Wang, Longchuan Bai, Donna McEachern, Jie Luo, Meilin Wang, Qiuxia Li, Aleksas Matvekas, Bo Wen, Duxin Sun, Arul M. Chinnaiyan, Shaomeng Wang
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Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator J. Med. Chem. (IF 7.3) Pub Date : 2024-03-26 Christopher G. Thomson, Thomas D. Aicher, Weiwei Cheng, Hongwen Du, Crissy Dudgeon, An-Hu Li, Baozhong Li, Eric Lightcap, Diheng Luo, Mark Mulvihill, Pengwei Pan, Benjamin F. Rahemtulla, Alan C. Rigby, Bradley Sherborne, Sanjeev Sood, David Surguladze, Eric P. A. Talbot, Feven Tameire, Simon Taylor, Yi Wang, Paulina Wojnarowicz, Fenfen Xiao, Savithri Ramurthy
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Correction to “Discovery of RORγ Allosteric Fluorescent Probes and Their Application: Fluorescence Polarization, Screening, and Bioimaging” J. Med. Chem. (IF 7.3) Pub Date : 2024-03-26 Yan-Cheng Yu, Zhen-Jiang Tong, Xiao-Ting Liang, Jia-Zhen Wu, Yu-Jing Xu, Jing-Jing Wang, Meng-Yuan Zhang, Tian-Hua Wei, Jin Yang, Yi-Bo Wang, Qing-Xin Wang, Qing-Qing Li, Zi-Xuan Wang, Xue-Jiao Leng, Ning Ding, Xin Xue, Shan-Liang Sun, Nian-Guang Li, Xiao-Long Wang
The author list requires correction. The names “Zixuan Wang” and “XueJiao Leng” should be updated to “Zi-Xuan Wang” and “Xue-Jiao Leng,” respectively. The changes are reflected in the authorship of this Correction. This article has not yet been cited by other publications.
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Targeting the CSF-1/CSF-1R Axis: Exploring the Potential of CSF1R Inhibitors in Neurodegenerative Diseases J. Med. Chem. (IF 7.3) Pub Date : 2024-03-26 Jihyun Baek, Joonhong Jun, Hyejin Kim, Hyunah Bae, Haebeen Park, Hyunwook Cho, Songhee Han, Ho Chul Shin, Jung-Mi Hah
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Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector J. Med. Chem. (IF 7.3) Pub Date : 2024-03-25 Mathieu Pizzonero, Rhalid Akkari, Xavier Bock, Romain Gosmini, Elsa De Lemos, Béranger Duthion, Gregory Newsome, Thi-Thu-Trang Mai, Virginie Roques, Hélène Jary, Jean-Michel Lefrancois, Laetitia Cherel, Vanessa Quenehen, Marielle Babel, Nuria Merayo, Natacha Bienvenu, Oscar Mammoliti, Ghjuvanni Coti, Adeline Palisse, Marlon Cowart, Anurupa Shrestha, Stephen Greszler, Steven Van Der Plas, Koen Jansen
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Drug Repurposing of ACT001 to Discover Novel Promising Sulfide Prodrugs with Improved Safety and Potent Activity for Neutrophil-Mediated Antifungal Immunotherapy J. Med. Chem. (IF 7.3) Pub Date : 2024-03-25 Xiangran Lu, Rongrong Wang, Yao Yu, Jinlian Wei, Yixiang Xu, Luoyifan Zhou, Fei Mao, Jian Li, Xiaokang Li, Xinming Jia
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Recent Advances on Small-Molecule Inhibitors of Lipocalin-like Proteins J. Med. Chem. (IF 7.3) Pub Date : 2024-03-25 Siliang Chen, Zhaoping Pan, Mingxia Liu, Linghong Guo, Xian Jiang, Gu He
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Cycloplatinated (II) Complex Based on Isoquinoline Alkaloid Elicits Ferritinophagy-Dependent Ferroptosis in Triple-Negative Breast Cancer Cells J. Med. Chem. (IF 7.3) Pub Date : 2024-03-25 Feng-Yang Wang, Liang-Mei Yang, Shan-Shan Wang, Hui Lu, Xu-Sheng Wang, Yuan Lu, Wen-Xiu Ni, Hong Liang, Ke-Bin Huang
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Correction to “Rational Design of Bioorthogonally Activatable PROTAC for Tumor-Targeted Protein Degradation” J. Med. Chem. (IF 7.3) Pub Date : 2024-03-22 Tao Bi, Pan Liang, Yanan Zhou, Hong Wang, Rui Huang, Qin Sun, Hongping Shen, Sijin Yang, Wei Ren, Zengjin Liu
We noticed that the WB graphic of GAPDH band in “MZ1” and “BT-PROTAC+BODIPY-TZ” group was overlapped in Figure 4c. After carefully checking our raw data, we found that the WB graphic of GAPDH band in “BT-PROTAC+BODIPY-TZ” group was uploaded by mis-operation. Thus, the graphic in Figure 4c needs to be corrected, but the results and conclusions in the published Article are not changed. The corrected
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Inhibition of NF-κB-Mediated Proinflammatory Transcription by Ru(II) Complexes of Anti-Angiogenic Ligands in Triple-Negative Breast Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-03-23 Ayan Chakraborty, Shilpendu Ghosh, Manas Pratim Chakraborty, Sujato Mukherjee, Shantanu Saha Roy, Rahul Das, Moulinath Acharya, Arindam Mukherjee
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Discovery of Novel 5,6-Dihydro-4H-pyrido[2,3,4-de]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases J. Med. Chem. (IF 7.3) Pub Date : 2024-03-22 Leifu Yang, Yaxin Li, Yunling Du, Yan Guo, Zhenke Guo, Baoxiu Liu, Jianglin Liu, Yanfei Liu, Hongdan Niu, Yueming Sun, Henglin Yan, Yajuan Yang, Shannan Yu, Yifan Zhang, Yuan Zhang, Kun Zheng, Nanqiao Zheng, Xiaoqing Zhang, Qiang Zhang, Liming Hu
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Copper(II) Complexes with 2,2′:6′,2″-Terpyridine Derivatives Displaying Dimeric Dichloro−μ–Bridged Crystal Structure: Biological Activities from 2D and 3D Tumor Spheroids to In Vivo Models J. Med. Chem. (IF 7.3) Pub Date : 2024-03-22 Katarzyna Choroba, Barbara Machura, Karol Erfurt, Ana Rita Casimiro, Sandra Cordeiro, Pedro V. Baptista, Alexandra R. Fernandes
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Discovery of Novel 11-Membered Templates as Squalene Synthase Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-03-22 Noriyasu Haginoya, Masanori Suzuki, Makoto Suzuki, Yutaka Ishigai, Koji Terayama, Akira Kanda, Kazuyuki Sugita
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CBP/p300 Degrader: A Promising Therapeutic Strategy for Treatment of Prostate Cancer and Beyond J. Med. Chem. (IF 7.3) Pub Date : 2024-03-22 Jiankang Hu, Yong Xu
Transcriptional coactivators CBP/p300 have emerged as potential targets for cancer therapeutics. This Viewpoint discusses recent results that demonstrate an exceptionally potent and orally efficacious CBP/p300 degrader for the treatment of prostate cancer. This degrader stands out as a promising new candidate for cancer therapy and deserves further research.
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Chimeric NOD2 Mincle Agonists as Vaccine Adjuvants J. Med. Chem. (IF 7.3) Pub Date : 2024-03-20 Emma M. Dangerfield, Shigenari Ishizuka, Kristel Kodar, Sho Yamasaki, Mattie S. M. Timmer, Bridget L. Stocker
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Novel PET Imaging Probe for Quantitative Detection of Senescence In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-03-20 Xin Xiang, Chuning Dong, Lianbo Zhou, Jun Liu, Zachary M. Rabinowitz, Yuzhao Zhang, Honghui Guo, Feng He, Xingdou Chen, Yunhua Wang, Lina Cui, Xiaowei Ma
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Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders J. Med. Chem. (IF 7.3) Pub Date : 2024-03-21 Simon C. C. Lucas, Afshan Ahmed, S. Neha Ashraf, Argyrides Argyrou, Matthias R. Bauer, Gian Marco De Donatis, Sylvain Demanze, Frederik Eisele, Lucia Fusani, Andreas Hock, Ganesh Kadamur, Shuyou Li, Abigail Macmillan-Jones, Iacovos N. Michaelides, Christopher Phillips, Marie Rehnström, Magdalena Richter, Monica C. Rodrigo-Brenni, Fiona Shilliday, Peng Wang, R. Ian Storer
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Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-03-21 Maoxu Xiao, Si Ha, Jiacheng Zhu, Wenxiang Tao, Zixuan Fu, Hanlin Wei, Qiangqiang Hou, Guoshun Luo, Hua Xiang
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Novel TLR4-Activating Vaccine Adjuvant Enhances the Production of Enterococcus faecium-binding Antibodies J. Med. Chem. (IF 7.3) Pub Date : 2024-03-21 Ana Rita Franco, Océane Sadones, Alessio Romerio, Valentina Artusa, Mohammed Monsoor Shaik, Samuel T. Pasco, Alice Italia, Simona D’Amato, Juan Anguita, Johannes Huebner, Felipe Romero-Saavedra, Francesco Peri
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Discovery of DNL343: A Potent, Selective, and Brain-Penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative Diseases J. Med. Chem. (IF 7.3) Pub Date : 2024-03-21 Robert A. Craig, II, Javier De Vicente, Anthony A. Estrada, Jianwen A. Feng, Katrina W. Lexa, Mark J. Canet, William E. Dowdle, Rebecca I. Erickson, Brittany N. Flores, Patrick C. G. Haddick, Lesley A. Kane, Joseph W. Lewcock, Nathan J. Moerke, Suresh B. Poda, Zachary Sweeney, Ryan H. Takahashi, Vincent Tong, Jing Wang, Ernie Yulyaningsih, Hilda Solanoy, Kimberly Scearce-Levie, Pascal E. Sanchez, Liwei
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Thermal Proteome Profiling Strategy Identifies CNPY3 as a Cellular Target of Gambogic Acid for Inducing Prostate Cancer Pyroptosis J. Med. Chem. (IF 7.3) Pub Date : 2024-03-21 Xiao-Wen Zhang, Ling Li, Min Liao, Dan Liu, Asma Rehman, Yang Liu, Zheng-Ping Liu, Peng-Fei Tu, Ke-Wu Zeng
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Prevention of Metastasis by Suppression of Stemness Genes Using a Combination of microRNAs J. Med. Chem. (IF 7.3) Pub Date : 2024-03-20 Kseniya V. Nevskaya, Alexandra G. Pershina, Ekaterina S. Hmelevskaya, Lina V. Efimova, Marina K. Ibragimova, Darya S. Dolgasheva, Irina A. Tsydenova, Alexander A. Ufandeev, Evgeny E. Buyko, Ekaterina A. Perina, Ksenia A. Gaptulbarova, Ekaterina A. Kravtsova, Sergei V. Krivoshchekov, Vladimir V. Ivanov, Artem M. Guriev, Elena V. Udut, Nikolai V. Litviakov
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Design of Novel 2-Phenylquinazolin-4-amines as Selective CYP1B1 Inhibitors for Overcoming Paclitaxel Resistance in A549 Cells J. Med. Chem. (IF 7.3) Pub Date : 2024-03-20 Meixian Yang, Fengyuan Yang, Xinyue Huang, Jiajing Cai, Yuxin Zhang, Jianhua Jia, Dachuan Qiu
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Long-Residence Time Peptide Antagonist for the Vasopressin V2 Receptor to Treat Autosomal Dominant Polycystic Kidney Disease J. Med. Chem. (IF 7.3) Pub Date : 2024-03-20 Xiaochun Xiong, Naiyuan Wang, Yixiao Zhang, Wenchao Zhao, Ningning Pang, Kequan Fu, Nan Zhou, Xueyan Zhou, Dong Guo
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Amphiphilic α-Peptoid-deoxynojirimycin Conjugate-based Multivalent Glycosidase Inhibitor for Hypoglycemic Effect and Fluorescence Imaging J. Med. Chem. (IF 7.3) Pub Date : 2024-03-19 Guang-Yuan Wang, Dong-Xiao Yan, Rui-Xue Rong, Bing-Ye Shi, Gao-Juan Lin, Fangqian Yin, Wen-Tong Wei, Xiao-Liu Li, Ke-Rang Wang
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Design and Synthesis of Cyclolipopeptide Mimics of Dysoxylactam A and Evaluation of the Reversing Potencies against P-Glycoprotein-Mediated Multidrug Resistance J. Med. Chem. (IF 7.3) Pub Date : 2024-03-19 Guan-Zhou Yang, Lei Wang, Kun Gao, Xi Zhu, Li-Guang Lou, Jian-Min Yue
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Identification of Novel Series of Potent and Selective Relaxin Family Peptide Receptor 1 (RXFP1) Agonists J. Med. Chem. (IF 7.3) Pub Date : 2024-03-19 Kenneth L. Granberg, Shigeki Sakamaki, Ryuichi Fuchigami, Yasuki Niwa, Masakazu Fujio, Harutoshi Kato, Fredrik Bergström, Niklas Larsson, Mikael Persson, Inmaculada C. Villar, Takuya Fujita, Emiko Sugikawa, Magnus Althage, Naoko Yano, Yoshito Yokoyama, Junpei Kimura, Mark Lal, Hideki Mochida
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Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure J. Med. Chem. (IF 7.3) Pub Date : 2024-03-19 Kenneth L. Granberg, Shigeki Sakamaki, Niklas Larsson, Fredrik Bergström, Ryuichi Fuchigami, Yasuki Niwa, Erik Ryberg, Anna Backmark, Harutoshi Kato, Shiki Miyazaki, Kaori Iguchi, Toshiaki Sakamoto, Mikael Persson, Akiko Idei, Luna Prieto Garcia, Inmaculada C. Villar, Henrik Gradén, Giulia Bergonzini, Torbjörn Arvidsson, Takuya Fujita, Magnus Althage, Johan Ulander, Junpei Kimura, Hikaru Yoneda, Ola
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Impact of Halogen Bonds on Protein–Peptide Binding and Protein Structural Stability Revealed by Computational Approaches J. Med. Chem. (IF 7.3) Pub Date : 2024-03-19 Jintian Li, Liping Zhou, Zijian Han, Leyun Wu, Jianfang Zhang, Weiliang Zhu, Zhijian Xu
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RNA–Small-Molecule Interaction: Challenging the “Undruggable” Tag J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Jaskirat Kaur, Akanksha Sharma, Poonam Mundlia, Vikas Sood, Ankur Pandey, Gurpal Singh, Ravi Pratap Barnwal
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Structure-Guided Discovery of Potent and Selective CLK2 Inhibitors for the Treatment of Knee Osteoarthritis J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Yongqiang Sun, Tianxing Hu, Mengdi Zhang, Jiaxing Song, Zhen Qin, Mai Liu, Jinliang Ji, Zhiyu Li, Zhixia Qiu, Jinlei Bian
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Design and Synthesis of 3-(2H-Chromen-3-yl)-5-aryl-1,2,4-oxadiazole Derivatives as Novel Toll-like Receptor 2/1 Agonists That Inhibit Lung Cancer In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Yijie Wang, Xu Cheng, Xinru Liu, Jing Xu, Lin Wang, Shouguo Zhang, Shuchen Liu, Tao Peng
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Discovery of Conformationally Constrained ALK2 Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Héctor González-Álvarez, Deeba Ensan, Tao Xin, Jong Fu Wong, Carlos A. Zepeda-Velázquez, Julien Cros, Laurent Hoffer, Taira Kiyota, Brian J. Wilson, Ahmed Aman, Owen Roberts, Methvin B. Isaac, Alex N. Bullock, David Smil, Rima Al-awar
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Beyond Rule of Five and PROTACs in Modern Drug Discovery: Polarity Reducers, Chameleonicity, and the Evolving Physicochemical Landscape J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Edward Price, Manuel Weinheimer, Alexey Rivkin, Gary Jenkins, Marjoleen Nijsen, Philip B. Cox, David DeGoey
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A Selective-Tumor-Penetrating Strategy via Unidirectional Direct Transfer for Intravesical Therapy of Bladder Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Xiaowen Qin, Heng Wang, Wentao Xu, Bin Zheng, Haibao Zhang, Qi Zhang, Yang Liu, Zhenghong Liu, Li Sun, Yixuan Mou, Cenchao Yao, Wei Zheng, Yiyang Chen, Chenkai Wang, Xuanyi Zhou, Youqing Shen, Pu Zhang, Dahong Zhang
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Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Chenming Gu, Jiayuan Liu, Fei Qian, Wenchao Yu, Doudou Huang, Jingshan Shen, Chenguo Feng, Kaixian Chen, Yiming Li, Xiangrui Jiang, Yechun Xu, Liuqiang Zhang
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Development of Membrane-Targeting Fluorescent 2-Phenyl-1H-phenanthro[9,10-d]imidazole-Antimicrobial Peptide Mimic Conjugates against Methicillin-Resistant Staphylococcus aureus J. Med. Chem. (IF 7.3) Pub Date : 2024-03-16 Ting Xu, Xiaoting Yan, Ayue Kang, Longhua Yang, Xinhui Li, Yue Tian, Ruige Yang, Shangshang Qin, Yong Guo
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Discovery of New Tricyclic Oxime Sampangine Derivatives as Potent Antifungal Agents for the Treatment of Cryptococcosis and Candidiasis J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Wanzhen Yang, Ruxiong Liu, Zhuang Li, Jie Tu, Dongjian Xu, Na Liu, Chunquan Sheng
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Cyclic Peptide Keap1–Nrf2 Protein–Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Jihua Zou, Jianyu Yan, Yifei Lu, Zhou Yu, Kai Zhang, Qianyu Han, Dan Han, Conghao Gai, Xiaoyun Chai, Qingjie Zhao, Chunlin Zhuang, Yan Zou
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Covalent Fragment Screening and Optimization Identifies the Chloroacetohydrazide Scaffold as Inhibitors for Ubiquitin C-terminal Hydrolase L1 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Ryan D. Imhoff, Rishi Patel, Muhammad Hassan Safdar, Hannah B. L. Jones, Adan Pinto-Fernandez, Iolanda Vendrell, Hao Chen, Christine S. Muli, Aaron D. Krabill, Benedikt M. Kessler, Michael K. Wendt, Chittaranjan Das, Daniel P. Flaherty
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Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Ye Zhong, Jing Xu, Ruochen Zhou, Li Tang, Shaoyue Ding, Zhaohui Ren, Ning Song, Baichun Hu, Huali Yang, Yili Sun, Maosheng Cheng, Jia Li, Yang Liu
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Synthetic Approaches to the New Drugs Approved During 2022 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Scott P. France, Erick A. Lindsey, Emma L. McInturff, Simon Berritt, Daniel W. Carney, Jacob C. DeForest, Sarah J. Fink, Andrew C. Flick, Tony S. Gibson, Kaitlyn Gray, Amber M. Johnson, Carolyn A. Leverett, Yiyang Liu, Subham Mahapatra, Rebecca B. Watson
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Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Zi-Xuan Wang, Qing-Qing Li, Jiao Cai, Jia-Zhen Wu, Jing-Jing Wang, Meng-Yuan Zhang, Qing-Xin Wang, Zhen-Jiang Tong, Jin Yang, Tian-Hua Wei, Yun Zhou, Wei-Chen Dai, Ning Ding, Xue-Jiao Leng, Shan-Liang Sun, Xin Xue, Yan-Cheng Yu, Ye Yang, Nian-Guang Li, Zhi-Hao Shi
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Subtle Structural Changes across the Boundary between A2AR/A2BR Dual Antagonism and A2BR Antagonism: A Novel Class of 2-Aminopyrimidine-Based Derivatives J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Haojie Wang, Xinyu Yang, Yan Li, Shuyin Ze, Bo Feng, Yuan Weng, Aoqi Gao, Gaojie Song, Mingyao Liu, Qiong Xie, Yonghui Wang, Weiqiang Lu
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Arginine-Selective Bioconjugation Reagent for Effective 18F-labeling of Native Proteins J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Pragalath Sadasivam, Shivashankar Khanapur, Siddesh V. Hartimath, Boominathan Ramasamy, Peter Cheng, Chin Zan Feng, David Green, Christopher Davis, Julian L. Goggi, Edward G. Robins, Ran Yan
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Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Lara Dötsch, Caitlin Davies, Elisabeth Hennes, Julia Schönfeld, Adarsh Kumar, Celine Da Cruz Lopes Guita, Johanna H.M. Ehrler, Kerstin Hiesinger, Sasikala Thavam, Petra Janning, Sonja Sievers, Stefan Knapp, Ewgenij Proschak, Slava Ziegler, Herbert Waldmann
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Correction to “Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer’s Disease” J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Min Jae Lee, Deepak Bhattarai, Hyeryung Jang, Ahreum Baek, In Jun Yeo, Seongsoo Lee, Zachary Miller, Sukyeong Lee, Jin Tae Hong, Dong-Eun Kim, Wooin Lee, Kyung Bo Kim
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DNA Interaction and Cleavage Modes of Anthraquinone-Fused Enediynes: A Study on Tiancimycins, Yangpumicins, and Their Semisynthetic Analogues J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Zhongqing Wen, Zhoukang Zhuang, Huiming Liu, Zilong Wang, Xueqiong Feng, Xiangcheng Zhu, Xiaohui Yan, Yanwen Duan, Yong Huang
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Discovery of a Novel Thienopyrimidine Compound as a Urate Transporter 1 and Glucose Transporter 9 Dual Inhibitor with Improved Efficacy and Favorable Druggability J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Xiaoyu Shi, Tong Zhao, Shuo Wang, Shujing Xu, Hui Liao, Shenghua Gao, Zhen Gao, Jian Zhang, Danhui Qi, Zhijiao Zhang, Fengxin Zheng, Youzhao Wang, Zhenqian Wang, Mingyu Yang, Qian Yang, Fan Yi, Jianxin Pang, Xinyong Liu, Peng Zhan
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Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Rishi R. Shah, Elena De Vita, Preethi S. Sathyamurthi, Daniel Conole, Xinyue Zhang, Elliot Fellows, Eleanor R. Dickinson, Carlos M. Fleites, Markus A. Queisser, John D. Harling, Edward W. Tate
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Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Zeren Sun, Lanjie Li, Bingxin Zhai, Mengxuan Hu, Lei Huang, Shihui Huang, Liu Ye, Xiangying Kong, Jie Xu, Jie Bai, Jingjie Yan, Qichen Zhou, Zheqi Hu, Yuchen Zhang, Yuhan Jiang, Yan Zhang, Zhou Qiao, Yi Zou, Yungen Xu, Qihua Zhu
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Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 John M. Ketcham, Stephen J. Harwood, Ruth Aranda, Athenea N. Aloiau, Briana M. Bobek, David M. Briere, Aaron C. Burns, Kersti Caddell Haatveit, Andrew Calinisan, Jeffery Clarine, Adam Elliott, Lars D. Engstrom, Robin J. Gunn, Anthony Ivetac, Benjamin Jones, Jon Kuehler, J. David Lawson, Natalie Nguyen, Cody Parker, Kelly E. Pearson, Lisa Rahbaek, Barbara Saechao, Xiaolun Wang, Anna Waters, Laura Waters
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Retro-Inverso Collagen Modulator Peptide Derived from Serpin A1 with Enhanced Stability and Activity In Vitro J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Fosca Errante, Marco Pallecchi, Gianluca Bartolucci, Elena Frediani, Francesca Margheri, Lisa Giovannelli, Anna M. Papini, Paolo Rovero
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Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Zhixiang Chen, Mi Wang, Dimin Wu, Longchuan Bai, Tianfeng Xu, Hoda Metwally, Yu Wang, Donna McEachern, Lijie Zhao, Ruiting Li, John Takyi-Williams, Meilin Wang, Lu Wang, Qiuxia Li, Bo Wen, Duxin Sun, Shaomeng Wang
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Mechanism-Based Macrocyclic Inhibitors of Serine Proteases J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Vishnu C. Damalanka, Victoria Banas, Paolo De Bona, Maithri M. Kashipathy, Kevin Battaile, Scott Lovell, James W. Janetka
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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 : 2024-03-13 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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Synthesis of Sorafenib−Ruthenium Complexes, Investigation of Biological Activities and Applications in Drug Delivery Systems as an Anticancer Agent J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Belma Zengin Kurt, Dilek Öztürk Civelek, Elmas Begüm Çakmak, Yakup Kolcuoğlu, Halil Şenol, Begüm Nurpelin Sağlık Özkan, Aydan Dag, Kadriye Benkli
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Searching for Conjugates as New Structures for Antifungal Therapies J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Izabela Muszalska-Kolos, Piotr Mariusz Dwiecki
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Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Ruth Dorel, Dawei Sun, Nicholas Carruthers, Georgette M. Castanedo, Peter M.-U. Ung, Daniel C. Factor, Tianbo Li, Hannah Baumann, Danielle Janota, Jodie Pang, Laurent Salphati, Robert Meklemburg, Allison J. Korman, Halie E. Harper, Samantha Stubblefield, Jian Payandeh, Daniel McHugh, Bradley T. Lang, Paul J. Tesar, Edward Dere, Matthieu Masureel, Drew J. Adams, Matthew Volgraf, Marie-Gabrielle Braun