Design, synthesis and cytotoxicity of novel 2-arylvinyl-4-aminoquinoline derivatives.
With an aim to develop promising anti-tumor agents, a novel series of 2-arylvinyl-4-aminoquinoline derivatives were designed, synthesized and evaluated for their cytotoxicity against H-460, HT-29, HepG2 and SGC-7901 cell lines in vitro. The pharmacological results indicated that most compounds were more potent than the positive controls, especially compounds 8, 14 and 16 with IC(50) values ranging from 0.05 to 0.85 µM against all tested cell lines respectively, which were 5.7- to 112-fold better than Iressa. The most active compound 14 (IC(50) values of 0.05, 0.25, 0.16, 0.68 µM), bearing 4-fluorostyryl at C-2 position and 3-(dimethylamino)-1-propylamino at C-4 position, showed great promise as a lead for the development of more effective quinoline analogues.
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, P. R. China.
Nan
N
Jiang
Xin
X
Zhai
Zhichao
Z
Chen
Chuang
C
Liang
Chao
C
Sun
Jing
J
Han
Ping
P
Gong
D000634:Aminoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D000077156:Gefitinib; D019073:HT29 Cells; D056945:Hep G2 Cells; D006801:Humans; D011799:Quinazolines / Q000737:chemistry / Q000633:toxicity; D013329:Structure-Activity Relationship
D000634:Aminoquinolines; D000970:Antineoplastic Agents; D011799:Quinazolines; D000077156:Gefitinib