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Thiocolchicine−Podophyllotoxin Conjugates: Dynamic Libraries Based on Disulfide Exchange Reaction
Ist Teil von
Journal of organic chemistry, 2006-03, Vol.71 (7), p.2848-2853
Ort / Verlag
Washington, DC: American Chemical Society
Erscheinungsjahr
2006
Link zum Volltext
Quelle
MEDLINE
Beschreibungen/Notizen
A dynamic combinatorial library of thiocolchicine−podophyllotoxin derivatives based on the disulfide bond exchange reaction is described. The influence of a biological target on the composition of the reaction mixture has been demonstrated. Use of high-resolution ESI mass spectrometry to evaluate the composition of the mixture shows promise for the design of new large libraries. The biological evaluation demonstrates that formation of a divalent compound affords a new chemical entity whose biological activity is not merely the sum of the single ligands activities, thus reflecting a different interaction with the biological target.