Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors

被引：44
|
作者：
Caldarelli, Marina [1 ]
Angiolini, Mauro [1 ]
Disingrini, Teresa [1 ]
Donati, Daniele [1 ]
Guanci, Marco [1 ]
Nuvoloni, Stefano [1 ]
Posteri, Helena [1 ]
Quartieri, Francesca [1 ]
Silvagni, Marco [1 ]
Colombo, Riccardo [1 ]
机构：
[1] Nerviano Med Sci Srl, Business Unit Oncol, I-20014 Nerviano, MI, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 15期
关键词：
MPS1; TTK; Anticancer; Kinase selectivity; SAR; SPINDLE CHECKPOINT; MITOSIS; ANAPHASE;
D O I：
10.1016/j.bmcl.2011.05.122
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and SAR of a series of novel pyrazolo-quinazolines as potent and selective MPS1 inhibitors are reported. We describe the optimization of the initial hit, identified by screening the internal library collection, into an orally available, potent and selective MPS1 inhibitor. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4507 / 4511
页数：5
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