Synthesis of d-ring modified acid hydrazide derivatives of podophyllotoxin and their anticancer studies as Tubulin inhibiting agents

Abstract

A new series (except compound 3a) of d-ring modified acid hydrazides of podophyllotoxin were synthesized by cleaving of its d-ring with various hydrazines. Furthermore, the synthesized compounds were screened for their anticancer activity against human tumor cell lines i.e., MCF-7, HeLa and A-549 and among the synthesized compounds 3c and 3f have shown significant anticancer activity almost similar to that of standard drug etoposide. Molecular modelling studies were also conducted for active compounds and found that the free energies obtained were in good agreement with the observed IC₅₀ values.

Keywords: Acid hydrazides; Anti-cancer studies; Podophyllotoxin; Tubulin inhibiting agents; d-Ring modification.