Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand

被引：63
作者：
Pagano, Nicholas
Maksimoska, Jasna
Bregman, Howard
Williams, Douglas S.
Webster, Richard D.
Xue, Feng
Meggers, Eric
机构：
[1] Univ Penn, Dept Chem, Philadelphia, PA 19104 USA
[2] Nanyang Technol Univ, Div Chem & Biol Chem, Singapore 637616, Singapore
[3] Natl Univ Singapore, Dept Chem, Singapore 117543, Singapore
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2007年 / 5卷 / 08期
关键词：
D O I：
10.1039/b700433h
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A general route to ruthenium pyridocarbazole half-sandwich complexes is presented and applied to the synthesis of sixteen new compounds, many of which have modulated protein kinase inhibition properties. For example, the incorporation of a fluorine into the pyridine moiety increases the binding affinity for glycogen synthase kinase 3 by almost one order of magnitude. These data are supplemented with cyclic voltammetry experiments and a protein co-crystallographic study.
引用
收藏
页码：1218 / 1227
页数：10
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