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

Molecules. 2016 Dec 6;21(12):1674. doi: 10.3390/molecules21121674.

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.

Keywords: 5-bromo-7-azaindolin-2-ones; antitumor activity; synthesis.

MeSH terms

  • A549 Cells
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Aza Compounds / chemical synthesis*
  • Aza Compounds / pharmacology
  • Cell Survival / drug effects
  • Drug Screening Assays, Antitumor
  • Hep G2 Cells
  • Humans
  • Indoles / chemical synthesis*
  • Indoles / pharmacology
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology
  • Sunitinib

Substances

  • Antineoplastic Agents
  • Aza Compounds
  • Indoles
  • Pyrroles
  • Sunitinib