Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety

被引：7
作者：
Zhang, Jun [1 ,2 ,3 ]
Shen, Weiyi [3 ]
Li, Xiaoning [1 ,2 ]
Chai, Yun [1 ,2 ]
Li, Senjun [3 ]
Lv, Kai [1 ,2 ]
Guo, Huiyuan [1 ,2 ]
Liu, Mingliang [1 ,2 ]
机构：
[1] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China
[2] Peking Union Med Coll, Beijing 100050, Peoples R China
[3] Zhejiang Starry Pharmaceut Co Ltd, Xianju 317300, Peoples R China
来源：
MOLECULES | 2016年 / 21卷 / 12期
关键词：
5-bromo-7-azaindolin-2-ones; synthesis; antitumor activity; KINASE-1; PDK1; INHIBITORS; ANTIBACTERIAL ACTIVITY; GROWTH; DESIGN;
D O I：
10.3390/molecules21121674
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC50: 2.357-3.012 mu M) was found more potent than Sunitinib (IC50: 31.594-49.036 mu M) against HepG2, A549 and Skov-3, respectively.
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页数：10
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