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

SL Zhang, YJ Liu, YF Zhao, QT Guo, P Gong

Index: Zhang, Shu Lan; Liu, Ya Jing; Zhao, Yan Fang; Guo, Qiu Ting; Gong, Ping Chinese Chemical Letters, 2010 , vol. 21, # 9 p. 1071 - 1074

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Citation Number: 11

Abstract

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 IC50 values from 1nmol/L to 0.92 μmol/L. A preliminary SAR study of these derivatives was performed.