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

被引：55
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 ; 081704 ;
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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