Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure
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DOI：
10.1016/j.bmcl.2006.07.026
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发表时间：
2006-10-01
影响因子：
2.7
通讯作者：
Hirai, Hiroshi
中科院分区：
文献类型：
--
作者：
Kawanishi, Nobuhiko;Sugimoto, Tetsuya;Hirai, Hiroshi
设计了一系列新的细胞周期蛋白依赖性激酶（CDK）抑制剂，其中含有一个大环喹啉-2- 1。基于结构的药物设计和优化，从我们之前报道的中度CDK1,2,4,6抑制剂diylurea 2开始[J]。医学杂志。化学，2001,276,27548]，导致发现有效的CDK1,2,4,6抑制剂，适合静脉给药的体内研究。(c) 2006 Elsevier Ltd.版权所有。
The design of a novel series of cyclin-dependent kinase (CDK) inhibitors containing a macrocyclic quinoxaline-2-one is reported. Structure-based drug design and optimization from the starting point of diarylurea 2, which we previously reported as a moderate CDK1,2,4,6 inhibitor [J. Biol. Chem. 2001, 276, 27548], led to the discovery of potent CDK1,2,4,6 inhibitor that were suitable for iv administration for in vivo study. (c) 2006 Elsevier Ltd. All rights reserved.