医学
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Exploring the role of conformational restriction in 5-alkyl-6-benzyl-2-{[(methylthio)methyl]thio}pyrimidin-4(3H)-ones: Effects in HIV-1 infected cells and reverse transcriptase enzymes
作者Egor Degtyarenko; Gebremedhin Solomon Hailu; Emanuele Fabbrizi; Anastasia Golovina; Andrey Voronkov; Roberta Astolfi; Lidia Giuliani; Andrea Mancini; Maxim B. Nawrozkij; Vladimir Chernyshov; Clarissa Pupillo; Roberto Cirilli; Laura Bavagnoli; Rino Ragno; José A. Esté; Emmanuele Crespan; Francesco Fiorentino; Roman Ivanov; Antonello Mai; Dante Rotili
作者单位Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow Region, 142432, Russia; Department of Science, Roma Tre University, Rome, 00146, Italy; Department of Drug Chemistry and Technologies, Sapienza University of Rome, Rome, 00185, Italy; Medicinal Biotechnology Department, Sirius University of Science and Technology, Olimpiyskiy Ave. 1, Sirius, Krasnodar Region, 354340, Russia; Institute of Biophysics of the Future, Institutsky lane, 9, Building 7, Dolgoprudny, Moscow region, 141701, Russia; Department of Chemistry, Sapienza University of Rome, Pale Aldo Moro 5, Rome, Italy; Centro Nazionale per il Controllo e la Valutazione dei Farmaci, Istituto Superiore di Sanità, Viale Regina Elena 299, Roma, 00161, Italy; Istituto di Genetica Molecolare IGM-CNR, via Abbiategrasso 207, Pavia, 27100, Italy; Universitat Internacional de Catalunya, C/ Josep Trueta s/n., Barcelona, 08195, Spain; Department of Biochemical Sciences, Sapienza University of Rome, Rome, 00185, Italy; Biostructures and Biosystems National Institute (INBB), Rome, 00165, Italy
Targeting the myeloid immune checkpoint ILT3 (LILRB4) with small molecules enables reprogramming of suppressive tumor immunity
作者Somaya A. Abdel-Rahman; Antonio Monari; Tom Miclot; Florent Barbault; Moustafa T. Gabr
作者单位Department of Radiology, Columbia University Irving Medical Center, New York, NY, 10032, USA; Department of Radiology, Weill Cornell Medicine, New York, NY, 10065, USA; Université Paris Cité, CNRS, ITODYS, Paris, F-75013, France
Discovery of a highly selective FLT3-ITD inhibitor with potent antileukemic activity based on 4-(2-fluorophenoxy)pyridine scaffold
作者Zhongyuan Wang; Yiwei Zhang; Lin Li; Yunfeng Wang; Dan Yang; Qingmei Song; Qingqing Fu; Dongsheng Zhao; Lei Tang; Weiwei Ouyang; Yue'e Chai; Weike Liao
作者单位Department of Pharmacy, Guizhou Provincial People's Hospital, Guiyang, 550002, China; State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Guizhou Medical University, Guiyang, 550004, China; Department of Oncology, Affiliated Hospital of Guizhou Medical University and Affiliated Cancer Hospital of Guizhou Medical University, Guiyang, 550001, China; Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China
Discovery and characterization of PGC-01: An effective GSDMD-targeting PROTAC
作者Qian-qian Wang; Rong-ying Hou; Yi-xuan Shua; Ya-fei Xu; Wen-jing Bian; Wen Xiao; Yu-qing Chen; Bing-yu Zhou; Yue Gao; Li Liu; Yu-hang Wang; Yi-bei Xiao; Cheng Jiang
作者单位School of Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Nanjing, 211198, China; Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China; Center of Drug Metabolism and Pharmacokinetics, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China
In silico identification and biological evaluation of newly synthetic hinokiflavone derivatives as multi-kinase inhibitors with preferential Aurora A activity for ovarian cancer therapy
作者Ke Wang; Guan-Yu Chen; Pei‐Yi Chu; Yi-Cheng Pan; Wei-Yu Hsu; Yun-Hao Dai; Yu-Liang Yang; Yeong-Jiunn Jang; Yang-Chang Wu
作者单位School of Pharmaceutical Sciences, Jiangsu Provincial University Key Laboratory of Green Biomanufacturing for Pharmaceuticals, Nanjing Tech University, Nanjing, 211816, China; Chinese Medicine Research and Development Center, China Medical University Hospital, Taichung, 404327, Taiwan; Master Program of Pharmaceutical Manufacture, College of Pharmacy, China Medical University, Taichung, Taiwan; Agricultural Biotechnology Research Center, Academia Sinica, Taipei, 11529, Taiwan; Graduate Institute of Integrated Medicine, College of Chinese Medicine, China Medical University, Taichung, 404333, Taiwan; Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung, Taiwan
Structure-based virtual screening leads to the discovery of a 4,5-dihydropyrazole derivative as the first dual inhibitor of West Nile virus NS3 helicase and protease
作者Antonio Lupia; Roberta Emmolo; Giulia Atzeni; Erica Sanna; Salvatore Nieddu; Alessia Onali; Laura Demuru; Annalaura Paulis; Simona Distinto; Angela Corona; Francesca Esposito; Rita Meleddu; Filippo Cottiglia; Sharon D. Bryant; Elias Maccioni; Enzo Tramontano
作者单位Department of Life and Environmental Sciences, University of Cagliari, Drug Sciences Section, Laboratories of Synthesis and CADD, A Building, University Campus, S.P. 8, Monserrato, CA, 09042, Italy; Department of Life and Environmental Sciences, University of Cagliari, Biomedical Section, Laboratory of Molecular Virology, E Building, University Campus, S.P. 8, Monserrato, CA, 09042, Italy; Inte: Ligand GmbH, Mariahilfer Straβe 74B/11, Vienna, 1070, Austria
Development of potent and selective ENPP1 inhibitors based on imidazo[1,2-a]pyrazine and pyrazine scaffolds for cancer immunotherapy
作者Zhiyue He; Yingying Zhang; Shiping Zhan; Tian Cao; Wanru Bai; Bozhi Zhou; Jie Yu; Huiying Zeng; Jingyi Zhou; Fuyun Tian; Xiaoyan Chen; Sulin Zhang; Mingyue Zheng; Xiaowei Wu
作者单位Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan, 528400, China; School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou, 511436, China; School of Life Sciences, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230026, China; The First Affiliated Hospital of USTC (Anhui Provincial Hospital), Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, China; University of Chinese Academy of Sciences, Beijing, 100049, China; College of Pharmacy, Guangdong Pharmaceutical University, Guangdong, 510006, China; School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China; School of Pharmaceutical Science and Technology, Hangzhou Institute of Advanced Study, UCAS, Hangzhou, 310024, China
Discovery and characterization of a sophoridine-derived TNIK inhibitor with antitumor activity in hepatocellular carcinoma
作者Yongquan Wei; Ziyi Wang; Die Sun; Zexu Xing; Haixia Yu; Lisheng Wang
作者单位School of Chemistry and Chemical Engineering, Guangxi University, Nanning, 530004, China; School of Chemical Engineering, Jilin Vocational College of Industry and Technology, Jilin, 132000, China; Guangxi Key Laboratory of Special Biomedicine, School of Medicine, Guangxi University, Nanning, 530004, China
Synthesis and biological evaluation of novel gemcitabine-dexamethasone hybrid as potent antitumor agents against esophageal cancer
作者Ruoxin Liu; Na Liu; Yimeng Wang; Jingyu Yang; Yuxin Chen; Xingjia Ma; Weijin Sheng; Kai Lv; Xiujun Liu
作者单位State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 100050, China
Discovery of a novel anti-ischemic acute kidney injury candidate from pestaphilones, a new subtype of azaphilones derived from marine fungus
作者Jianglian She; Jian Cai; Chuanliang Wei; Xiaoqiang He; Rongxiang Qiu; Xin Qi; Xinlong Li; Tanwei Gu; Xi Zhang; Zhihao Zeng; Xinqi Chen; Yuanxin Tian; Wei Xu; Yonghong Liu; Xuefeng Zhou; Lan Tang
作者单位Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China; State Key Laboratory of Tropical Oceanography, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, 510301, China; University of Chinese Academy of Sciences, Beijing, 100049, China; Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China; Guangxi Key Laboratory of Marine Drugs, Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning, 530200, China
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