6-Arylamino-7-chloro-quinazoline-5,8-diones as novel cytotoxic and DNA topoisomerase inhibitory agents

  • Bioorg Med Chem Lett. 2004 Jul 5;14(13):3385-8. doi: 10.1016/j.bmcl.2004.04.094.
Hyen Joo Park  1 ,  Young-Shin Kim ,  Jin Sung Kim ,  Eun-Jin Lee ,  You-Jin Yi ,  Hye Jin Hwang ,  Myung-Eun Suh ,  Chung-Kyu Ryu ,  Sang Kook Lee
Affiliations
  • 1. College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-ku, Seoul 120-750, South Korea.
PMID: 15177438 DOI: 10.1016/j.bmcl.2004.04.094
Abstract

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.