期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 39, 期 1, 页码 5-10出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2003.05.002
关键词
9-anilinothiazolo[5,4-b]quinoline derivatives; antitumoral; DNA intercalation; cytotoxic activity
Five new 9-anilinothiazolo[5,4-b]quinoline derivatives (compounds 5, 7, 9, 10, 11) have been prepared. Some of the compounds were prepared by coupling properly substituted anilines to the novel compound 9-chloro-2-(methylthio)thiazolo[5,4-b]quinoline. Of these, compound 7 (9-anilino-2-[[2-(N,N-diethylamino)ethyl]amino]thiazolo[5,4-b]quinoline) showed the best cytotoxic activity in several cell lines. All compounds demonstrated DNA binding in nanomolar range. Compound 7 inhibited the C-14-thymidine incorporation into DNA. Results indicate that these derivatives deserve more considerations as potential antitumoral drugs. (C) 2003 Elsevier SAS. All rights reserved.
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