Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3)

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• 作者：Fei Ma^a ; Peng Liu^a ; Min Lei^a ; Jian Liu^b ; ^{liujian623@njucm.edu.cn} ; Hongtao Wang^c ; Shaohua Zhao^c ; Lihong Hu^a ; ^b ; ^{lhhu@simm.ac.cn}
• 关键词：Indolin-2-one derivatives ; FLT3 inhibitors ; Structure-activity relationships (SARs) ; Acute myeloid leukemia (AML) ; In vivo study
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：72-86
• 全文大小：1580 K
• 卷排序：127

文摘

Bioisosterism strategy was used to modify the carboxamide bond of sunitinib. All the derivatives were evaluated in FLT3-dependent human AML cell line MV4-11. The kinase and cellular inhibition assay experiments were also conducted.