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Molecules 2016, 21(12), 1674; doi:10.3390/molecules21121674

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

1
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
2
Zhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Maria Emília de Sousa
Received: 11 November 2016 / Revised: 28 November 2016 / Accepted: 30 November 2016 / Published: 6 December 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [3929 KB, uploaded 6 December 2016]   |  

Abstract

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 μM) was found more potent than Sunitinib (IC50: 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively. View Full-Text
Keywords: 5-bromo-7-azaindolin-2-ones; synthesis; antitumor activity 5-bromo-7-azaindolin-2-ones; synthesis; antitumor activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Zhang, J.; Shen, W.; Li, X.; Chai, Y.; Li, S.; Lv, K.; Guo, H.; Liu, M. Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety. Molecules 2016, 21, 1674.

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