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Efficient PNA double-duplex invasion using preQ1•G-clamp as a pseudo-complementary G•C base pair
作者Yuga Shibuya; Yosuke Demizu; Toru Sugiyama
作者单位Faculty of Pharmaceutical Sciences, Teikyo University, Itabashi-ku, Tokyo 173-8605, Japan; Division of Organic Chemistry, National Institute of Health Sciences, Ministry of Health and Welfare, 3-25-26 Tonomachi, Kawasaki-ku, Kawasaki-shi, Kanagawa 210-9501, Japan
Reactivation of an inert 15-mer antimicrobial peptide by truncation-directed i, i + 7 lactam cyclization
作者Jinhua Zhang; Zhiyi Jiang; Mingli Jiang; Zhuoqiong Guo; Ruifang Li; Guancheng Liu
作者单位School of Biological Engineering, Henan Provincial Key Laboratory of Grain Resource Conversion and Utilization, Henan University of Technology, Zhengzhou 450001, China
Semi-synthesis and activity study of α-mangostin ether derivatives bearing N-heterocyclic side chains as multitarget-directed ligands against AD
作者Bokai Zhang; Yu Li; Xiaoli Qiao; Boyong Zhang; Xinying Liu; Xiang Li; Zhenzhen Liu; Zitong Li; Gang Wang; Yizhe Wang; Xiaokun Yang
作者单位First Teaching Hospital of Tianjin University of Traditional Chinese Medicine, Tianjin 300381, China; National Clinical Research Center for Chinese Medicine, Tianjin 300381, China; Tianjin Nankai Hospital, Tianjin 300100, China; School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Caffeic acid phenethyl ester derivatives inhibit glyoxalase I activity and induce cell death in cultured cancer cell lines
作者Shuji Ishizaki; Aya Nishida; Kanako Nakamine; Kana Yamaji; Natsuki Miyazaki; Mio Takahashi; Ryohei Sato; Kouji Kuramochi; Atsushi Yoshimori; Ryoko Takasawa
作者单位Faculty of Pharmaceutical Sciences, Tokyo University of Science, 6-3-1 Niijuku, Katsushika-ku, Tokyo 125-8585, Japan; Department of Applied Biological Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan; Institute for Theoretical Medicine, Inc., 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-0012, Japan
Synthesis, computational and in vitro anti-tubercular activity studies of thiadiazole-linked pyridazinone derivatives
作者Neeru Bhanwala; Niranjana Sri Sundaramoorthy; Nimbark Yash Dhirajlal; Ramandeep Singh; Gopal L. Khatik
作者单位Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Raebareli—Transit Campus, Lucknow 226002, Uttar Pradesh, India; Centre for Tuberculosis Research, Tuberculosis Research Laboratory, BRIC–Translational Health Science and Technology Institute (THSTI), Faridabad 121001, Haryana, India
Design, synthesis, and evaluation of novel 5-aminolevulinic acid and 3-hydroxypyridinone conjugates for enhanced photodynamic therapy in triple-negative breast cancer
作者Jinhui Ren; Jingqi Zhang; Yan Liu; Yikai Shen; Keren Wang; Changjun Zhang; Yuanyuan Xie
作者单位College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, PR China; Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, Hangzhou 310014, PR China; State Key Laboratory of Green Chemical Synthesis and Conversion, Zhejiang Key Laboratory of Green Manufacturing Technology for Chemical Drugs, Hangzhou 310014, China
Synthesis and antimalarial activity of novel C30-aminated betulin derivatives
作者Christopher Bérubé; Catherine Bergeron; Dominic Gagnon; Mathieu Gagné-Boulet; Sébastien Fortin; Simon Côté; Fernando Albericio; Dave Richard; Eric Biron
作者单位Faculté de pharmacie, Université Laval, Québec (QC) G1V 0A6, Canada; Centre de recherche du CHU de Québec-Université Laval, Québec (QC) G1V 4G2, Canada; Peptide Science Laboratory, School of Chemistry and Physics, University of KwaZulu-Natal, Durban, KwaZulu-Natal 4001, South Africa; Department of Inorganic and Organic Chemistry, University of Barcelona, Barcelona 08028, Spain; Matrix Innovation Inc., Québec (QC) G2C 1S9, Canada; Département de microbiologie-infectiologie et d'immunologie, Université Laval, Québec (QC) G1V 0A6, Canada
Discovery of orally available benzimidazole-based STING antagonists with in vivo activity
作者Takao Kiyoi; Hirokazu Matsumoto; Shiori Takamatsu; Haruka Taniguchi; Kanako Ishihara; Tomohiko Taguchi; Masaaki Sawa
作者单位Drug Discovery Unit, Carna Biosciences, Inc., 1-5-5 Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo 650-0047, Japan; Laboratory of Organelle Pathophysiology, Department of Integrative Life Sciences, Graduate School of Life Sciences, Tohoku University, Aobayama, Aoba-ku, Sendai, Miyagi 980-8578, Japan
Novel salicylamido sulfonamides as CD73 immune checkpoint inhibitors: Synthesis and in vitro biological evaluation
作者Dinesh Krishna Narukulla; Shrilekha Chilvery; Chandraiah Godugu; Avvaru Subha Jahnavi; Amol G. Dikundwar; Venkata Rao Kaki
作者单位Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER)-Hyderabad, Balanagar, Hyderabad 500037, Telangana, India.; Department of Biological Sciences, National Institute of Pharmaceutical Education and Research (NIPER)-Hyderabad, Balanagar, Hyderabad 500037, Telangana, India.; Department of Pharmaceutical Analysis, National Institute of Pharmaceutical Education and Research (NIPER)-Hyderabad, Balanagar, Hyderabad 500037, Telangana, India.
Design and synthesis of dual-target CDK9-EZH2 inhibitors using a pharmacophore fusion strategy
作者Yixue Han; Ruiqi Wang; Lina Tian; Jian Xiao; Aihuan Wei; Jian Ding; Yi Chen; Youhong Hu; Yanfen Fang; Xin Li
作者单位School of Pharmacy, Anhui University of Chinese Medicine, Hefei, 230012, China; Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong, 264117, China; State Key Laboratory of Chemical Biology, Division of Anti-tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; State Key Laboratory of Drug Research, Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 ZuChongZhi Road, Shanghai, 201203, China; University of Chinese Academy of Sciences, 19 Yuquan Road, Beijing, 110039, China; School of Medicine, Hangzhou City University, Hangzhou 310015, China
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