Thiocolchicine-podophyllotoxin conjugates: dynamic libraries based on disulfide exchange reaction.


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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@article{Danieli2006ThiocolchicinepodophyllotoxinCD, title={Thiocolchicine-podophyllotoxin conjugates: dynamic libraries based on disulfide exchange reaction.}, author={Bruno Danieli and Alessandra Giardini and Giordano Lesma and Daniele Passarella and Bruno Peretto and Alessandro Sacchetti and Alessandra Silvani and Graziella Pratesi and Franco Zunino}, journal={The Journal of organic chemistry}, year={2006}, volume={71 7}, pages={2848-53} }