Synthesis and antitumor activities of novel 1,4-substituted phthalazine derivatives

A series of 1,4-substituted phthalazine derivatives were designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549, HT-29 and MDA-MB-231 cell lines in vitro. Among them, compounds 7a-7h showed excellent selectivity for MDA-MB-231 cell line with IC(50) values from 1 nmol/L to 0.92 mu mol/L. A preliminary SAR study of these derivatives was performed. (C) 2010 Ping Gong. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.