Identification of amides derived from 1H-pyrazolo [3, 4-b] pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)

…, T Baumeister, KK Bowman, AJ Buckmelter…

文献索引：Zheng, Xiaozhang; Bair, Kenneth W.; Bauer, Paul; Baumeister, Timm; Bowman, Krista K.; Buckmelter, Alexandre J.; Caligiuri, Maureen; Clodfelter, Karl H.; Feng, Yezhen; Han, Bingsong; Ho, Yen-Ching; Kley, Nikolai; Li, Hong; Liang, Xiaorong; Liederer, Bianca M.; Lin, Jian; Ly, Justin; O'Brien, Thomas; Oeh, Jason; Oh, Angela; Reynolds, Dominic J.; Sampath, Deepak; Sharma, Geeta; Skelton, Nicholas; Smith, Chase C.; Tremayne, Jarrod; Wang, Leslie; Wang, Weiru; Wang, Zhongguo; Wu, Hongxing; Wu, Jiansheng; Xiao, Yang; Yang, Guangxing; Yuen, Po-Wai; Zak, Mark; Dragovich, Peter S. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 20 p. 5488 - 5497

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被引用次数: 18

摘要

Abstract Potent, 1H-pyrazolo [3, 4-b] pyridine-containing inhibitors of the human nicotinamide phosphoribosyltransferase (NAMPT) enzyme were identified using structure- based design techniques. Many of these compounds exhibited nanomolar antiproliferation activities against human tumor lines in in vitro cell culture experiments, and a representative example (compound 26) demonstrated encouraging in vivo efficacy in a mouse xenograft ...