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.

Thiocolchicine-podophyllotoxin conjugates: Dynamic libraries based on disulfide exchange reaction

SACCHETTI, ALESSANDRO;
2006

Abstract

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11311/527969
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