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Amino- and glycoconjugates of pyrido[4,3,2- kl]acridine. Synthesis, antitumor activity, and DNA binding

A series of amino- and glycoconjugates of pyrido[4,3,2- kl]acridine and pyrido[4,3,2- kl]acridin-4-one have been prepared. The most active molecules, the amino conjugates 7 and 11, display a cytostatic activity against HT-29 cancer cells at micromolar concentration. This activity correlates well wit...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2006-11, Vol.14 (22), p.7520-7530
Main Authors: Bouffier, Laurent, Baldeyrou, Brigitte, Hildebrand, Marie-Paule, Lansiaux, Amélie, David-Cordonnier, Marie-Hélène, Carrez, Danièle, Croisy, Alain, Renaudet, Olivier, Dumy, Pascal, Demeunynck, Martine
Format: Article
Language:English
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Summary:A series of amino- and glycoconjugates of pyrido[4,3,2- kl]acridine and pyrido[4,3,2- kl]acridin-4-one have been prepared. The most active molecules, the amino conjugates 7 and 11, display a cytostatic activity against HT-29 cancer cells at micromolar concentration. This activity correlates well with a strong DNA binding. The molecules, amino or glycoconjugates, bind DNA by intercalation, the amino or glyco substituent being located in one groove. None of the molecules inhibits topoisomerase activity.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2006.07.010