Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides

  • Bioorg Med Chem Lett. 2015 Jul 15;25(14):2782-7. doi: 10.1016/j.bmcl.2015.05.017.
Minghua Wang  1 ,  Cheng Ye  1 ,  Mingliang Liu  2 ,  Zhaoyang Wu  3 ,  Linhu Li  1 ,  Chunlan Wang  1 ,  Xiujun Liu  1 ,  Huiyuan Guo  1
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
  • 2. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. Electronic address: [email protected].
  • 3. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
PMID: 26009164 DOI: 10.1016/j.bmcl.2015.05.017
Abstract

We report herein the design and synthesis of a series of novel 5-halogenated-7-azaindolin-2-one derivatives containing a 2,4-dimethylpyrrole moiety. Nine target compounds with ⩾70% inhibition against MCF-7 at 30 μM were further evaluated for their in vitro antitumor activity against seven human Cancer cell lines by SRB assay. Results reveal that some compounds have potent antitumor activity, and the most active 13c7 (IC50s: 4.49-15.39 μM) was found to be more active than Sunitinib (IC50s: 4.70->30 μM) against all of the tested Cancer cell lines.

Keywords
7-Azaindolin-2-ones; Antitumor activity; Synthesis.