当前期刊：
Journal of Medicinal Chemistry
Go to
current issue
加入关注
本刊介绍/投稿指南
催更
样式： 排序： IF: - GO 导出 标记为已读
Go to
current issue
加入关注
本刊介绍/投稿指南
催更
样式： 排序： IF: - GO 导出 标记为已读
-
Prioritization of Eleven-Nineteen-Leukemia Inhibitors as Orally Available Drug Candidates for Acute Myeloid Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2024-11-12 Xuejiao Shirley Guo, Sandeep Atla, Satyanarayana Nyalata, Yugendar R. Alugubelli, Peng-Hsun Chase Chen, Shiqing Xu, Wenshe Ray Liu
-
Proline Analogues in Drug Design: Current Trends and Future Prospects J. Med. Chem. (IF 6.8) Pub Date : 2024-11-12 Vladimir Kubyshkin, Pavel K. Mykhailiuk
-
Unnatural Amino Acids: Strategies, Designs, and Applications in Medicinal Chemistry and Drug Discovery J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Krishna K. Sharma, Komal Sharma, Kamya Rao, Anku Sharma, Gajanan K. Rathod, Shams Aaghaz, Naina Sehra, Rajesh Parmar, Brett VanVeller, Rahul Jain
-
Synthesis and Pharmacological Characterization of Fluorescent Ligands Targeting the Angiotensin II Receptors Derived from Agonists, β-Arrestin-Biased Agonists, and Antagonists J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Céline Delaitre, Michel Boisbrun, Samir Acherar, André Dias, Alexandra Kleinclauss, Mathilde Achard, Mélissa Colin, Trung Minh Nguyen, Nicolas Humbert, Khawla Chmeis, Karen L. Martinez, Nicolas Gilles, Philippe Robin, Sandra Lecat, François Dupuis
-
Modulatory Role of Pantropic Cell Signaling Pathways in the Antimigratory and Antiproliferative Action of Triazole Chelated Iridium(III) Complexes in Cervical Cancer Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-11-11 Anushka Mondal, Bishnu Das, Souvik Karmakar, Soumili Pani, Shrabani Khan, Parna Gupta, Jayasri Das Sarma
-
Discovery of the First-in-Class Dual-Target ROCK/HDAC Inhibitor with Potent Antitumor Efficacy in Vivo That Trigger Antitumor Immunity J. Med. Chem. (IF 6.8) Pub Date : 2024-11-10 Churu Mao, Jiebin Fang, Shijie Zou, Yun Huang, Xiaoming Chen, Xia Ding, Zhangyun Fang, Ningjing Zhang, Yijie Lou, Zhe Chen, Wanjing Ding, Zhongjun Ma
-
Structure-Guided Design of Affinity/Covalent-Bond Dual-Driven Inhibitors Targeting the AMP Site of FBPase J. Med. Chem. (IF 6.8) Pub Date : 2024-11-09 Hongxuan Cao, Zeyue Huang, Zheng Liu, Xiao Zhang, Yanliang Ren, Muhammad Salman Hameed, Li Rao, Nokwanda P. Makunga, Georgi M. Dobrikov, Jian Wan
-
Discovery of a Novel Macrocyclic Noncovalent CDK7 Inhibitor for Cancer Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-11-09 Hongfu Lu, Yihong Zhang, Jinxin Liu, Tao Jiang, Xiang Yu, Haoyu Zhang, Tao Liang, Jingjing Peng, Xin Cai, Xiaoling Lan, Jinmin Ren, Mei Ge, Jingyang Zhang, Jingjin Shang, Jiaojiao Yu, Hongcan Ren, Qiang Liu, Jinting Gao, Lili Tang, Xiao Ding, Man Zhang, Alex Aliper, Qiang Lu, Fusheng Zhou, Jiong Lan, Feng Ren, Alex Zhavoronkov
-
Discovery of SD-436: A Potent, Highly Selective and Efficacious STAT3 PROTAC Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Renqi Xu, Haibin Zhou, Longchuan Bai, Donna McEachern, Dimin Wu, Ranjan Kumar Acharyya, Mi Wang, Jelena Tošović, Chao-Yie Yang, Krishnapriya Chinnaswamy, Jennifer L. Meagher, Jeanne A. Stuckey, Cai Liu, Meilin Wang, Bo Wen, Duxin Sun, Shaomeng Wang
-
Recent Progress and Future Perspectives on Anti-Hyperuricemic Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Zhiqiang Sun, Xuewen Zhang, Zean Zhao, Xiaoxun Li, Jianxin Pang, Jianjun Chen
-
Closing the Design–Make–Test–Analyze Loop: Interplay between Experiments and Predictions Drives PROTACs Bioavailability J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Zulma Santisteban Valencia, Jennifer Kingston, Filip Miljković, Hannah Rowbottom, Nadia Mann, Sophie Davies, Martin Ekblad, Silvio Di Castro, Karolina Kwapień, Erik Malmerberg, Stig D. Friis, Thomas Lundbäck, Tomas Leek, Johan Wernevik
-
Discovery of Thiazole Carboxamides as Novel Vanin-1 Inhibitors for Inflammatory Bowel Disease Treatment J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Tao Xie, Gao-Yao Cao, Shize Zhang, Meng-Ke Li, Xin Jin, Liu Liu, Guangji Wang, Le Zhen
-
Structure–Activity Relationships and Discovery of (S)-5-(tert-Butyl)-11-(difluoromethoxy)-9-methoxy-2-oxo-1,2,5,6-tetrahydropyrido[2′,1′:2,3]imidazo[4,5-h]quinoline-3-carboxylic Acid (AB-161), a Novel Orally Available and Liver-Centric HBV RNA Destabilizer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Dimitar Gotchev, Shuai Chen, Benjamin Dugan, Bruce D. Dorsey, Xu Wang, Muhammad Sheraz, Rose Kowalski, Fei Liu, Sunny Tang, Tim Chiu, Troy Harasym, Ingrid E. Graves, Emily P. Thi, Jeremy D. Mason, Nathan Overholt, Ravi Dugyala, Angela M. Lam, Andrew G. Cole, Michael J. Sofia
-
A Fast Method to Monitor Tyrosine Kinase Inhibitor Mechanisms J. Med. Chem. (IF 6.8) Pub Date : 2024-11-08 Alejandro Fernández, Margarida Gairí, María Teresa González, Miquel Pons
-
Discovery of CHD1 Antagonists for PTEN-Deficient Prostate Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Rebecca L. Johnson, Amanda L. Graboski, Fengling Li, Jacqueline L. Norris-Drouin, William G. Walton, Cheryl H. Arrowsmith, Matthew R. Redinbo, Stephen V. Frye, Lindsey I. James
-
Discovery of SZJK-0421: A Novel Potent, Low Toxicity, Selective Second Generation of CRM1 Inhibitor for the Treatment of Both Hematological and Solid Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Hang Miao, Yanru Qin, DingLu Shao, Qinghua Chen, Yupeng Pan, Meng Lei, Ruokun Wu, Xinran Ye, Xueyuan Wang, Yongqiang Zhu
-
Development of N-(4-(1H-Imidazol-1-yl)phenyl)-4-chlorobenzenesulfonamide, a Novel Potent Inhibitor of β-Catenin with Enhanced Antitumor Activity and Metabolic Stability J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Michela Puxeddu, Lele Ling, Silvia Ripa, Michele D’Ambrosio, Marianna Nalli, Anastasia Parisi, Pietro Sciò, Antonio Coluccia, Arianna Granese, Martina Santelli, Domiziana Masci, Petra Cuřínová, Chiara Naro, Claudio Sette, Arianna Pastore, Mariano Stornaiuolo, Chiara Bigogno, Giulio Dondio, Laura Di Magno, Gianluca Canettieri, Te Liu, Romano Silvestri, Giuseppe La Regina
-
Discovery of 5-Nitro-N-(3-(trifluoromethyl)phenyl) Pyridin-2-amine as a Novel Pure Androgen Receptor Antagonist against Antiandrogen Resistance J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Huating Wang, Xuwen Wang, Haiyang Zhong, Lvtao Cai, Weitao Fu, Xin Chai, Jianing Liao, Rong Sheng, Luhu Shan, Xiaohong Xu, Lei Xu, Peichen Pan, Tingjun Hou, Dan Li
-
Small-Molecule Modulators Targeting Coactivator-Associated Arginine Methyltransferase 1 (CARM1) as Therapeutic Agents for Cancer Treatment: Current Medicinal Chemistry Insights and Emerging Opportunities J. Med. Chem. (IF 6.8) Pub Date : 2024-11-07 Shuqing Li, Wanyi Pan, Chengpeng Tao, Zhihao Hu, Binbin Cheng, Jianjun Chen, Xiaopeng Peng
-
Antiplasmodial and Insecticidal Activities of Third-Generation Ivermectin Hybrids J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Parth, Sofia Santana, Catarina Rôla, Carla Bastos Oliveira, Miguel Prudêncio, Kamaljit Singh, Diana Fontinha
-
Single Amine or Guanidine Modification on Norvancomycin and Vancomycin to Overcome Multidrug-Resistance through Augmented Lipid II Binding and Increased Membrane Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Xiaolei Bian, Zhifu Chen, Fang Li, Yuanyuan Xie, Yi Li, Youhong Luo, Xiangman Zou, Hui Wang, Jingwen Zhang, Xiaowen Wang, Jinyong Zhang, Dongliang Guan
-
Medicinal Chemistry Education: Emphasize Fundamentals and Skillfully Integrate Knowledge J. Med. Chem. (IF 6.8) Pub Date : 2024-11-06 Shaoqing Du, Xueping Hu, Craig W. Lindsley, Peng Zhan
Medicinal chemistry is an interdisciplinary field that aims to discover innovative drugs and synthesize drug molecules at the intersection of chemistry and biology. In the field of medicinal chemistry education, it is essential to establish a robust foundation by emphasizing fundamental principles of chemistry and biology. This strategy not only imparts students with a comprehensive understanding of
-
Inhibition of Human Salivary and Pancreatic α-Amylase by Resveratrol Oligomers J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Rizliya Visvanathan, Dang Truong Le, Sushil Dhital, Topul Rali, Rohan A. Davis, Gary Williamson
-
Optimization of Antiproliferative Properties of Triimine Copper(II) Complexes J. Med. Chem. (IF 6.8) Pub Date : 2024-11-04 Katarzyna Choroba, Bartosz Zowiślok, Sławomir Kula, Barbara Machura, Anna M. Maroń, Karol Erfurt, Cristiana Marques, Sandra Cordeiro, Pedro V. Baptista, Alexandra R. Fernandes
-
Discovery of Highly Selective Inhibitors of Microtubule-Associated Serine/Threonine Kinase-like (MASTL) J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Rebecca A. Gallego, Stephanie Scales, Chad Toledo, Marin Auth, Louise Bernier, Madeline Berry, Sonja Brun, Loanne Chung, Carl Davis, Wade Diehl, Klaus Dress, Koleen Eisele, Jeff Elleraas, Jason Ewanicki, Yvette Fobian, Samantha Greasley, Eric C. Greenwald, Ted W. Johnson, Penney Khamphavong, Jennifer Lafontaine, Jian Li, Angelica Linton, Michael Maestre, Nichol Miller, Anwar Murtaza, Ryan L. Patman
-
Structure-Based Design of Covalent SARS-CoV-2 Papain-like Protease Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Bin Tan, Xueying Liang, Ahmadullah Ansari, Prakash Jadhav, Haozhou Tan, Kan Li, Francesc Xavier Ruiz, Eddy Arnold, Xufang Deng, Jun Wang
-
Target Ligand Separation and Identification of Isoforsythiaside as a Histone Lysine-Specific Demethylase 1 Covalent Inhibitor Against Breast Cancer Metastasis J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Mengzhen Gu, Xiaoqing Xu, Xiaoping Wang, Yun Wang, Yu Zhao, Xiaoxian Hu, Lu Zhu, Zhenzhong Deng, Chao Han
-
Expanding the Solvent/Protein Region Occupation of the Non-Nucleoside Reverse Transcriptase Inhibitor Binding Pocket for Improved Broad-Spectrum Anti-HIV-1 Efficacy: from Rigid Phenyl-Diarylpyrimidines to Flexible Hydrophilic Piperidine-Diarylpyrimidines J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Wen-Juan Huang, Christophe Pannecouque, Erik De Clercq, Angela Corona, Stefania Maloccu, Enzo Tramontano, Shuai Wang, Fen-Er Chen
-
Medicinal Chemistry Education and Training J. Med. Chem. (IF 6.8) Pub Date : 2024-11-05 Craig W. Lindsley
I decided to weigh in on the ongoing discussion about medicinal chemistry education and training with my thoughts on the matter, as I began my career in industry (Parke-Davis, Eli Lilly and Merck) and later moved into academia (Vanderbilt University/Warren Center for Neuroscience Drug Discovery). First and foremost, training in synthetic organic chemistry is essential. A deep understanding of mechanistic
-
Identification of Oral Bioavailable Coumarin Derivatives as Potential AR Antagonists Targeting Prostate Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-04 Jinbiao Liao, Jianing Liao, Minkui Zhang, Yanzhen Yu, Lvtao Cai, Kaixin Le, Weitao Fu, Yiyang Qin, Tingjun Hou, Dan Li, Rong Sheng
-
A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins J. Med. Chem. (IF 6.8) Pub Date : 2024-11-04 Suzanne Ackloo, Fengling Li, Magda Szewczyk, Almagul Seitova, Peter Loppnau, Hong Zeng, Jin Xu, Shabbir Ahmad, Yelena A Arnautova, A. J. Baghaie, Serap Beldar, Albina Bolotokova, Paolo A. Centrella, Irene Chau, Matthew A. Clark, John W. Cuozzo, Saba Dehghani-Tafti, Jeremy S. Disch, Aiping Dong, Antoine Dumas, Jianwen A. Feng, Pegah Ghiabi, Elisa Gibson, Justin Gilmer, Brian Goldman, Stuart R Green
-
Pan-Transcriptional Enhanced Associated Domain Palmitoylation Pocket Covalent Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-11-02 Jinhyuk Kim, Hadong Kim, Jongwan Kim, Seon Yeon Cho, Sungho Moon, Youngki Yoo, Hanseong Kim, Jin Kwan Kim, Hyejin Jeon, Wan Namkung, Gyoonhee Han, Kyoung Tai No
-
Palladium-Mediated Bioorthogonal System for Prodrug Activation of N-Benzylbenzamide-Containing Tubulin Polymerization Inhibitors for the Treatment of Solid Tumors J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Jinlong Li, Tong Zhang, Di Wu, Chen He, Haoxiang Weng, Tiandong Zheng, Jie Liu, Hong Yao, Jichao Chen, Yansong Ren, Zheying Zhu, Jinyi Xu, Shengtao Xu
-
Azobenzene-Tagged Photopeptides Exhibiting Excellent Selectivity and Light-Induced Cytotoxicity in MCF-7 Cells over HeLa and A549 J. Med. Chem. (IF 6.8) Pub Date : 2024-11-02 Sambit Pradhan, Surajit Sarker, Pakkirisamy Thilagar
-
Discovery of ERD-1233 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader for the Treatment of ER+ Human Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Ranjan Kumar Acharyya, Rohan Kalyan Rej, Biao Hu, Zhixiang Chen, Dimin Wu, Jianfeng Lu, Hoda Metwally, Donna McEachern, Yu Wang, Wei Jiang, Longchuan Bai, Jelena Tošović, Christina L. Gersch, Guozhang Xu, Weihong Zhang, WenXue Wu, E. Scott Priestley, Zhihua Sui, Farzad Sarkari, Bo Wen, Duxin Sun, James M. Rae, Shaomeng Wang
-
Perspective for Drug Discovery Targeting SARS Coronavirus Methyltransferases: Function, Structure and Inhibition J. Med. Chem. (IF 6.8) Pub Date : 2024-10-31 Xin Li, Yongcheng Song
-
Synthesis and Biological Evaluation of New Chalcogen Semicarbazone (S, Se) and Their Azole Derivatives against Chagas Disease J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Mercedes Rubio-Hernández, Verónica Alcolea, Elany Barbosa da Silva, Miriam A. Giardini, Thaís H. M Fernandes, Nuria Martínez-Sáez, Anthony J. O’Donoghue, Jair L. Siqueira-Neto, Silvia Pérez-Silanes
-
Targeting Periplakin of Novel Benzenesulfonamides as Highly Selective Agonists for the Treatment of Vitiligo J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Hui Zhong, Panpan Li, Qiuming Yan, Yu Xia, Xin Zhang, Yifan Lai, Liqiang Li, Feifei Wang, Jing Shang, Xiaoming Zha
-
Discovery of Anthranilic Acid Derivatives as Antagonists of the Pro-Inflammatory Orphan G Protein-Coupled Receptor GPR17 J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Nader M. Boshta, Michael Lewash, Meryem Köse, Vigneshwaran Namasivayam, Soumya Sarkar, Jan H. Voss, Andy J. Liedtke, Anna Junker, Maoqun Tian, Anne Stößel, Mahmoud Rashed, Ahmed Mahal, Nicole Merten, Cécile Pegurier, Jörg Hockemeyer, Evi Kostenis, Christa E. Müller
-
Development of α-Helical Antimicrobial Peptides with Imperfect Amphipathicity for Superior Activity and Selectivity J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Zhongxiang Wu, Ying Cai, Yajun Han, Yunhan Su, Tianyu Zhang, Xingyu Wang, An Yan, Liunan Wang, Sijing Wu, Gan Wang, Zhiye Zhang
-
Preliminary Study of Radionuclide-Labeled MerTK-Targeting PET Imaging Agents for the Diagnosis of Melanoma J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Changjiang Wang, Hao Liu, Yunyi Yang, Qinghong Sun, Liping Yin, Liping Yang, Xiaodong Wang, Weiling Zhao, Qiang Wan, Guangfu Liu, Yue Chen, Zibo Li, Li Wang
-
Designing Quasi-Intrinsic Photosensitizers with Dual Function of Fluorescence Imaging and Photodynamic Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-11-01 Xixi Cui, Jianzhong Fan, Yang Gao, Xucong Zhou, Changzhe Zhang, Qingtian Meng
-
A Prostate-Specific Membrane Antigen-Targeting Small Molecule–Drug Conjugate Strategy to Overcome the Hematological Toxicity of Olaparib J. Med. Chem. (IF 6.8) Pub Date : 2024-10-31 Qi Chen, Zhenying Wu, Haiying Zhu, Xi Zhang, Yongping Yu, Wenteng Chen
-
Discovery of MD-265: A Potent MDM2 Degrader That Achieves Complete Tumor Regression and Improves Long-Term Survival of Mice with Leukemia J. Med. Chem. (IF 6.8) Pub Date : 2024-10-31 Angelo Aguilar, Jiuling Yang, Yangbing Li, Donna McEachern, Liyue Huang, Stevenchoukry Razzouk, Shaomeng Wang
-
Achieving High Affinity for a Bacterial Lectin with Reversible Covalent Ligands J. Med. Chem. (IF 6.8) Pub Date : 2024-10-31 Giulia Antonini, Anna Bernardi, Emilie Gillon, Alberto Dal Corso, Monica Civera, Laura Belvisi, Annabelle Varrot, Sarah Mazzotta
-
Structural Modification and Pharmacological Evaluation of (Thiadiazol-2-yl)pyrazines as Novel Piezo1 Agonists for the Intervention of Disuse Osteoporosis J. Med. Chem. (IF 6.8) Pub Date : 2024-10-27 Hairong Tang, Ruihan Hao, Ding Ma, Yujia Yao, Chunyong Ding, Xiaoling Zhang, Ao Zhang
-
Developing Stapled Aptamers with a Constrained Conformation for Osteogenesis Imperfect Therapeutics J. Med. Chem. (IF 6.8) Pub Date : 2024-10-29 Gubu Amu, Ge Zhang, Nannan Jing, Yuan Ma
-
Discovery of BAY 2413555, First Selective Positive Allosteric Modulator of the M2 Receptor to Restore Cardiac Autonomic Balance J. Med. Chem. (IF 6.8) Pub Date : 2024-10-28 Alexandros Vakalopoulos, Daniel Basting, Markus Brechmann, Henrik Teller, Melissa Boultadakis Arapinis, Alexander Straub, Joachim Mittendorf, Mark Meininghaus, Thomas Müller, Katrin Nowak-Reppel, Martina Schäfer, Matthias Wittwer, Maximilian Kullmann, Carsten Terjung, Dieter Lang, Thorsten Poethko, Tobias Marquardt, Till Freudenberger, Thomas Mondritzki, Jörg Hüser, Michael Heckmann, Hanna Tinel
-
Rational Exploration of 2,4-Diaminopyrimidines as DHFR Inhibitors Active against Mycobacterium abscessus and Mycobacterium avium, Two Emerging Human Pathogens J. Med. Chem. (IF 6.8) Pub Date : 2024-10-28 Matheus Andrade Meirelles, Vitor M. Almeida, Jaryd R. Sullivan, Ian de Toledo, Caio Vinicius dos Reis, Micael Rodrigues Cunha, Rachel Zigweid, Abraham Shim, Banumathi Sankaran, Elijah L. Woodward, Steve Seibold, Lijun Liu, Mohammad Rasel Mian, Kevin P. Battaile, Jennifer Riley, Christina Duncan, Frederick R. C. Simeons, Liam Ferguson, Halimatu Joji, Kevin D. Read, Scott Lovell, Bart L. Staker, Marcel
-
Discovery and Characterization of BAY-184: A New Potent and Selective Acylsulfonamide-Benzofuran In Vivo-Active KAT6AB Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-10-25 Antonius ter Laak, Roman C. Hillig, Steven J. Ferrara, Daniel Korr, Naomi Barak, Philip Lienau, Simon Herbert, Amaury Ernesto Fernández-Montalván, Roland Neuhaus, Mátyás Gorjánácz, Vera Puetter, Volker Badock, Wilhelm Bone, Craig Strathdee, Franziska Siegel, Christoph Schatz, Katrin Nowak-Reppel, Olaf Doehr, Stefan Gradl, Ingo V. Hartung, Matthew Meyerson, Léa Bouché
-
Chromatographic Determination of Permeability-Relevant Lipophilicity Facilitates Rapid Analysis of Macrocyclic Peptide Scaffolds J. Med. Chem. (IF 6.8) Pub Date : 2024-10-25 Grant Koch, Alexander Engstrom, Jaru Taechalertpaisarn, Justin Faris, Satoshi Ono, Matthew R. Naylor, R. Scott Lokey
-
Rational Design of Macrocyclic Noncovalent Inhibitors of SARS-CoV-2 Mpro from a DNA-Encoded Chemical Library Screening Hit That Demonstrate Potent Inhibition against Pan-Coronavirus Homologues and Nirmatrelvir-Resistant Variants J. Med. Chem. (IF 6.8) Pub Date : 2024-10-25 Xu Wang, Dimitar Gotchev, Kristi Yi Fan, Marvin M. Vega, Nagraj Mani, Kayleigh McGovern-Gooch, Andrea Cuconati, Breanna Tercero, Xiaohe Wang, Philip Carpino, Klaus Maskos, Paolo A. Centrella, Andreas Schmitt, Franziska Preuss, Archna Prasad, Chia-yi Chen, Matthew A. Clark, John P. Guilinger, Shawn Johnstone, Konstanze von König, Anthony D. Keefe, Jenny Liu, Stéphane Turcotte, Ying Zhang, Debora L.
-
Design, Synthesis, and Activity Evaluation of BRD4 PROTAC Based on Alkenyl Oxindole-DCAF11 Pair J. Med. Chem. (IF 6.8) Pub Date : 2024-10-30 Man Zhao, Wenjing Ma, Jinyi Liang, Yubao Xie, Tianzi Wei, Ming Zhang, Jiajie Qin, Lingyin Lao, Ruilin Tian, Haiqiang Wu, Jin Cheng, Min Li, Yuyang Liu, Liang Hong, Guofeng Li
-
Antibacterial, Antibiofilm, and Anti-inflammatory Effects of a Novel Thrombin-Derived Peptide in Sepsis Models: Insights into Underlying Mechanisms J. Med. Chem. (IF 6.8) Pub Date : 2024-10-30 S. Dinesh Kumar, Jin Kyeong Lee, Naveen Kumar Radhakrishnan, Jeong Kyu Bang, Byeongkwon Kim, Shubhash Chandra Chaudhary, Ajish Chelladurai, Byambasuren Ganbaatar, Eun Young Kim, Chul Won Lee, Sungtae Yang, Yangmee Kim, Song Yub Shin
-
NGT: Generative AI with Synthesizability Guarantees Discovers MC2R Inhibitors from a Tera-Scale Virtual Screen J. Med. Chem. (IF 6.8) Pub Date : 2024-10-29 Saulo H. P de Oliveira, Aryan Pedawi, Victor Kenyon, Henry van den Bedem
-
DBPR116, a Prodrug of BPRMU191, in Combination with Naltrexone as a Safer Opioid Analgesic Than Morphine via Peripheral Administration J. Med. Chem. (IF 6.8) Pub Date : 2024-10-29 Shu-Yu Lin, Yung-Chiao Chang, Ya-Wen Tien, Yu-Hsien Kuo, Hsiao-Fu Chang, Li-Chin Ou, Ya-Ping Chen, Kuei-Hua Chang, Ying-Ting Hsu, Yu-Chen Huang, Chen-Ming Yang, Ping-Yee Law, Jing-Hua Xi, Pao-Luh Tao, Horace H. Loh, Teng-Kuang Yeh, Hong Zhuang, Hsing-Pang Hsieh, Chuan Shih, Chiung-Tong Chen, Shiu-Hwa Yeh, Shau-Hua Ueng
-
Inhibition of Pseudomonas aeruginosa Carbonic Anhydrases, Exploring Ciprofloxacin Functionalization Toward New Antibacterial Agents: An In-Depth Multidisciplinary Study J. Med. Chem. (IF 6.8) Pub Date : 2024-10-25 Beatrice Marinacci, Ilaria D’Agostino, Andrea Angeli, Simone Carradori, Francesco Melfi, Rossella Grande, Micol Corsiani, Marta Ferraroni, Mariangela Agamennone, Anna Rita Tondo, Susi Zara, Valentina Puca, Benedetta Pellegrini, Chiara Vagaggini, Elena Dreassi, Marianna A. Patrauchan, Clemente Capasso, Orazio Nicolotti, Fabrizio Carta, Claudiu T. Supuran
-
Discovery of Novel PROTAC-Based HPK1 Degraders with High Potency and Selectivity for Cancer Immunotherapy J. Med. Chem. (IF 6.8) Pub Date : 2024-10-24 Zhimin Zhang, Liubin Guo, Mengting Zhao, Hao Pan, Zhao Dong, Ling Wang, Xi Yang, Zhiping Zhang, Mengqiang Wu, Yujie Chang, Yacheng Yang, Linan Sun, Sirui Liu, Rongyao Zhu, Haowen Zheng, Xinyu Dai, Xiaohua Zhang, Chunhua Jiang, Zhuangzhi Zhu, Yuchen Zhang, Dongzhou Liu
-
Development of an Intravenously Stable Disulfide-Rich Peptide for the Treatment of Chemotherapy-Induced Neuropathic Pain J. Med. Chem. (IF 6.8) Pub Date : 2024-10-24 Tianmiao Li, Han-Shen Tae, Shen Chen, Xiao Li, Jiazhen Liang, Teng Pan, Zixuan Zhang, Tao Jiang, David J. Adams, Rilei Yu
-
Immune Checkpoint-Modulating Photosensitizer That Targets BRD4 for Cancer Photoimmunotherapy J. Med. Chem. (IF 6.8) Pub Date : 2024-10-24 Peixia Li, Yayin Du, Jingru Qiu, Qiaoyun Jiang, Weijia Chen, Xinke Zhang, Guiling Li, Donghai Li, Gang Shan
更新日期：2024-11-08
京公网安备 11010802027423号