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

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 (IC50 = 1.0 μM, MDA-MB-231). The compound 5k exhibited selective cytotoxicity against breast cancer cell line MCF7 (IC50 = 3.1 μM).