Thiocolchicine-podophyllotoxin conjugates: dynamic libraries based on disulfide exchange reaction |
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Authors: | Danieli Bruno Giardini Alessandra Lesma Giordano Passarella Daniele Peretto Bruno Sacchetti Alessandro Silvani Alessandra Pratesi Graziella Zunino Franco |
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Institution: | Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, 20133 Milan, Italy. |
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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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