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.

引用

页数：10

共 19 条

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