Citation: Shu Lan Zhang, Ya Jing Liu, Yan Fang Zhao, Qiu Ting Guo, Ping Gong. Synthesis and antitumor activities of novel 1,4-substituted phthalazine derivatives[J]. Chinese Chemical Letters, ;2010, 21(9): 1071-1074. doi: 10.1016/j.cclet.2010.04.004 shu

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

Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China

Received Date: 9 January 2010

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 1 nmol/L to 0.92 μmol/L. A preliminary SAR study of these derivatives was performed.
- 1,4-Substituted phthalazine,
- Synthesis,
- Cytotoxicity
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