title: Synthesis and cytotoxic evaluation of some new phthalazinylpiperazine derivatives.
abstract: 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.
authors: Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, China.
authors: Yajing
authors: Y
authors: Liu
authors: Shulan
authors: S
authors: Zhang
authors: Ye
authors: Y
authors: Li
authors: Jianqiang
authors: J
authors: Wang
authors: Yu
authors: Y
authors: Song
authors: Ping
authors: P
authors: Gong
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor / Q000379:methods / Q000706:statistics & numerical data; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010793:Phthalazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D010793:Phthalazines; D010879:Piperazines; D000077489:Piperazine