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Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5
Institution:1. Key Laboratory of Natural Resources of Changbai Mountain and Functional Molecules, Ministry of Education, Molecular Medicine Research Center, College of Pharmacy, Yanbian University, Yanji 133002, PR China;2. The School of Public Health, Jilin Medical University, Jilin 132013, PR China;3. Pharmacy Intravenous Admixture Services, Yanbian University Hospital, Yanji 133000, PR China;1. Faculty of Arts and Science, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan;2. Faculty of Pharmacy and Pharmaceutical Science, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan;3. Department of Hospital Pharmacy, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan;4. Graduate School of Science and Engineering, University of Toyama, 3190 Gofuku, Toyama 930-8555, Japan;1. School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, Yunnan, China;2. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, Yunnan, China;3. Department of Respiratory Medicine, The Second Affiliated Hospital of Kunming Medical University, Kunming 650031, Yunnan, China;1. Department of Chemistry and Biochemistry and the Viral Information Institute, San Diego State University, San Diego, CA 92182, USA;2. Department of Chemistry and Biochemistry, San Diego State University, San Diego, CA 92182, USA;3. Department of Chemistry, Southwestern College, Chula Vista, CA 92120, USA;1. Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development & Shanghai Key Laboratory of Green Chemistry and Chemical Processes, SCME, East China Normal University, Shanghai 200062, China;2. Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai 200241, China;1. Department of Chemistry, Bristol-Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA;2. BBRC, Special Economic Zone, Biocon Park, Jigani Link Road, Bangalore, India;3. Molecular Structure & Design, Bristol-Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA;4. Immuno-Oncology Small Molecule Biology, Bristol-Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA;5. Lead Discovery & Optimization, Bristol-Myers Squibb Company, P.O. Box 4000, Princeton, NJ, USA
Abstract:
Keywords:TGF-β  ALK5 inhibitor  HIF-1α  Apoptosis  Docking
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