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

Affiliation

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).

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