Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition

被引：137

作者：

Fancelli, D ^{[1
]}

Berta, D ^{[1
]}

Bindi, S ^{[1
]}

Cameron, A ^{[1
]}

Cappella, P ^{[1
]}

Carpinelli, P ^{[1
]}

Catana, C ^{[1
]}

Forte, B ^{[1
]}

Giordano, P ^{[1
]}

Giorgini, ML ^{[1
]}

Mantegani, S ^{[1
]}

Marsiglio, A ^{[1
]}

Meroni, M ^{[1
]}

Moll, J ^{[1
]}

Pittalà, V ^{[1
]}

Roletto, F ^{[1
]}

Severino, D ^{[1
]}

Soncini, C ^{[1
]}

Storici, P ^{[1
]}

Tonani, R ^{[1
]}

Varasi, M ^{[1
]}

Vulpetti, A ^{[1
]}

Vianello, P ^{[1
]}

机构：

[1] Nerviano Med Sci Oncol, I-20014 Milan, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 08期

关键词：

D O I：

10.1021/jm049076m

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potent and selective Aurora kinase inhibitors were identified from the combinatorial expansion of the 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole bi-cycle, a novel and versatile scaffold designed to target the ATP pocket of protein kinases. The most potent compound reported in this study had an IC50 of 0.027 mu M in the enzymatic assay for Aur-A inhibition and IC(50)s between 0.05 mu M and 0.5 mu M for the inhibition of proliferation of different tumor cell lines.

引用

页码：3080 / 3084

页数：5

共 14 条

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