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Synthesis and Cytotoxic Evaluation of Some New Phthalazinylpiperazine Derivatives
Author(s) -
Liu Yajing,
Zhang Shulan,
Li Ye,
Wang Jianqiang,
Song Yu,
Gong Ping
Publication year - 2012
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201100250
Subject(s) - chemistry , cytotoxic t cell , stereochemistry , selectivity , cytotoxicity , in vitro , combinatorial chemistry , cancer cell lines , cell culture , cancer cell , cancer , biochemistry , biology , genetics , catalysis
A new series of 1,4‐disubstituted phthalazinylpiperazine derivatives 7a–f , 12a–f and 20a–f were designed and synthesized in order to develop potent and selective antitumor agents. The target compounds were screened for their cytotoxic activities against A549, HT‐29 and MDA‐MB‐231 cancer cell lines in vitro . Among them, compounds 7a–f exhibited excellent selectivity for MDA‐MB‐231 with IC 50 values ranging from 0.013 µM to 0.079 µM. The most promising compound, 7e (IC 50 = 2.19 µM, 2.19 µM, 0.013 µM), was 9.3, 10, and 4.9 × 10 3 times more active than vatalanib (IC 50 = 20.27 µM, 21.96 µM, 63.90 µM), respectively.