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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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Published in: | Bioorganic & medicinal chemistry 2006-11, Vol.14 (22), p.7520-7530 |
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Main Authors: | , , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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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. |
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ISSN: | 0968-0896 1464-3391 |
DOI: | 10.1016/j.bmc.2006.07.010 |