6-Arylamino-7-chloro-quinazoline-5,8-diones as novel cytotoxic and DNA topoisomerase inhibitory agents.
A series of 6-arylamino-7-chloro-quinazoline-5,8-diones were prepared and evaluated for their in vitro cytotoxicity in cultured human cancer cell lines A549 (lung cancer), Col2 (colon cancer), and SNU-638 (stomach cancer). The preliminary structure-activity relationship has been described for providing further development of potent antitumor agents. To further investigate the cytotoxic mechanism, the effects of test compounds on DNA topoisomerase I and II activities have been assessed.
Park
Hyen Joo
HJ
College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-ku, Seoul 120-750, South Korea.
Kim
Young-Shin
YS
Kim
Jin Sung
JS
Lee
Eun-Jin
EJ
Yi
You-Jin
YJ
Hwang
Hye Jin
HJ
Suh
Myung-Eun
ME
Ryu
Chung-Kyu
CK
Lee
Sang Kook
SK
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D026942:DNA Topoisomerases / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011799:Quinazolines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D059003:Topoisomerase Inhibitors
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011799:Quinazolines; D059003:Topoisomerase Inhibitors; D026942:DNA Topoisomerases