Cytotoxic activities of 6-arylamino-7-halo-5,8-quinolinediones against human tumor cell lines.
6-Arylamino-7-halo-5,8-quinolinediones (4a-4k, 5a-5b) were tested for in vitro cytotoxicity against human solid tumor cell lines such as A 549 (non-small cell lung), SK-OV-3 (ovarian), SK-MEL-2 (melanoma), HCT-15 (colon) and XF 498 (CNS) by SRB assay. The arylamino-7-chloro-5,8-quinolinediones 4 were also evaluated for cyclin-dependent kinase (CDK2 and CDK4) inhibitory effect. Among them, the 5,8-quinolinediones 4a and 5a with 7-(4-fluorophenyl)amino group were found to be potent cytotoxic against HCT 15, SKOV-3 and XF 498, and the compounds 4f and 4i showed inhibitory activities for the CDK4.
Ryu
C K
CK
College of Pharmacy, Ewha Womans University, Seoul, Korea. ckryu@mm.ewha.ac.kr
Kang
H Y
HY
Yi
Y J
YJ
Lee
C O
CO
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors; D006801:Humans; D011804:Quinolines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D011804:Quinolines; D018844:Cyclin-Dependent Kinases