Synthesis and antitumor activity of 1-deoxybaccatin III analogs from 1-deoxybaccatin VI

Abstract

Several new 1-deoxybaccatin III analogs were conveniently synthesized from 1-deoxybaccatin VI with the aim of having modified ester groups at C-2 and C-4. The antitumor activity of these compounds was evaluated. The preliminary SAR analysis showed that the electronic properties of the terminal group in the substituent on C4, C9, and C10 constituted important factors to the cytotoxic activities against A 549 and MCF-7 cell lines. The present studies provide a new synthetic basis for development of new 1-deoxypaclitaxel analogs. .