Design and Synthesis of N??Substituted Indazole??3??Carboxamides as Poly (ADP??ribose) polymerase??1 (PARP??1) Inhibitors†

…, KG Pandya, CA Lau??Cam, S Singh…

文献索引：Patel, Maulik R.; Pandya, Kashyap G.; Lau-Cam, Cesar A.; Singh, Satyakam; Pino, Maria A.; Billack, Blase; Degenhardt, Kurt; Talele, Tanaji T. Chemical Biology and Drug Design, 2012 , vol. 79, # 4 p. 488 - 496

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被引用次数: 4

摘要

A group of novel N-1-substituted indazole-3-carboxamide derivatives were synthesized and evaluated as inhibitors of poly (ADP-ribose) polymerase-1 (PARP-1). A structure-based design strategy was applied to a weakly active unsubstituted 1H-indazole-3-carboxamide 2, by introducing a three carbon linker between 1H-indazole-3-carboxamide and different heterocycles, and led to compounds 4 [1-(3-(piperidine-1-yl) propyl)-1H-indazole-3- ...