Novel bis(indolyl)hydrazide-hydrazones as potent cytotoxic agents

  • Bioorg Med Chem Lett. 2012 Jan 1;22(1):212-5. doi: 10.1016/j.bmcl.2011.11.031.
Dalip Kumar  1 ,  N Maruthi Kumar ,  Soumitra Ghosh ,  Kavita Shah
Affiliations
  • 1. Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India. [email protected]
PMID: 22123320 DOI: 10.1016/j.bmcl.2011.11.031
Abstract

A series of bis(indolyl) hydrazide-hydrazones 5a-n were synthesized and evaluated for their cytotoxicity against selected human Cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 in presence of catalytic amount of acetic acid afforded 5a-n in good yields. Among the synthesized bis(indolyl)hydrazide-hydrazones, the compound 5b with N-(p-chlorobenzyl) and bromo substituents was found to be the most potent against multiple Cancer cell lines (IC(50)=1.0 μM, MDA-MB-231). The compound 5k exhibited selective cytotoxicity against breast Cancer cell line MCF7 (IC(50)=3.1 μM).