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 / B. Danieli, A. Giardini, G. Lesma, D. Passarella, B. Peretto, A. Sacchetti, A. Silvani, G. Pratesi, F. Zunino. - In: JOURNAL OF ORGANIC CHEMISTRY. - ISSN 0022-3263. - 71:7(2006), pp. 2848-2853.
Thiocolchicine-Podophyllotoxin Conjugates: Dynamic Libraries Based on Disulfide Exchange Reaction
B. DanieliPrimo
;A. GiardiniSecondo
;G. Lesma;D. Passarella;B. Peretto;A. Sacchetti;A. Silvani;
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.Pubblicazioni consigliate
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