Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor

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• 作者：Hojong Yoon^a ; ¹ ; Injae Shin^b ; ¹ ; Yunju Nam^b ; Nam Doo Kim^c ; Kyung-Bok Lee^d ; Taebo Sim^a ; ^b ; ^{tbsim@kist.re.kr}
• 关键词：RET kinase ; Metabolic stability ; Specific inhibitor ; 5-Aminopyrazole-4-carboxamide
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：1145-1155
• 全文大小：2054 K
• 卷排序：125

文摘

Novel 5-aminopyrazole-4-carboxamide derivatives were synthesized as RET inhibitors. Compound 15 l is potent on V804M-RET as well as on wt-RET. Compound 15 l is metabolically stable. Compound 15 l displays exceptional kinase selectivity. Compound 15 l suppresses growth of wt-RET-Ba/F3 and V804M-RET-Ba/F3 cells.