Synthesis and evaluation of 9-anilinothiazolo[5,4-b]quinoline derivatives as potential antitumorals |
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Authors: | Rodríguez-Loaiza Pilar Quintero Angelina Rodríguez-Sotres Rogelio Solano José D Lira-Rocha Alfonso |
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Institution: | Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Cd. Universitaria, Coyoacán 04510, México. |
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Abstract: | Five new 9-anilinothiazolo5,4-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)thiazolo5,4-b]quinoline. Of these, compound 7 (9-anilino-2-2-(N,N-diethylamino)ethyl]amino]thiazolo5,4-b]quinoline) showed the best cytotoxic activity in several cell lines. All compounds demonstrated DNA binding in nanomolar range. Compound 7 inhibited the (14)C-thymidine incorporation into DNA. Results indicate that these derivatives deserve more considerations as potential antitumoral drugs. |
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