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

被引：58

作者：

Danieli, B

Giardini, A

Lesma, G

Passarella, D

Peretto, B

Sacchetti, A

Silvani, A

Pratesi, G

Zunino, F

机构：

[1] Univ Milan, Dipartimento Chim Organ & Ind, Milan, Italy

[2] Ist Nazl Tumori, I-20133 Milan, Italy

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2006年 / 71卷 / 07期

关键词：

D O I：

10.1021/jo052677g

中图分类号：

O62 [有机化学];

学科分类号：

070303 [有机化学]; 081704 [应用化学];

摘要：

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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页码：2848 / 2853

页数：6

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