通过拟环设计进入一类新型蛋白激酶抑制剂。
Entry into a new class of protein kinase inhibitors by pseudo ring design.
作者信息
Furet Pascal, Caravatti Giorgio, Guagnano Vito, Lang Marc, Meyer Thomas, Schoepfer Joseph
机构信息
Novartis Institutes for BioMedical Research, WKL-136.P.12, CH-4002 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2008 Feb 1;18(3):897-900. doi: 10.1016/j.bmcl.2007.12.041. Epub 2008 Jan 14.
PMID:18248988
Abstract
A pyrimidin-4-yl-urea motif forming a pseudo ring by intramolecular hydrogen bonding has been designed to mimic the pyrido[2,3-d]pyrimidin-7-one core structure of a well-established class of protein kinase inhibitors. Potent inhibition of a number of protein kinases was obtained with the first prototype compound synthesized to probe the design concept.
摘要
通过分子内氢键形成假环的嘧啶-4-基脲基序已被设计用于模拟一类成熟的蛋白激酶抑制剂的吡啶并[2,3-d]嘧啶-7-酮核心结构。用合成的首个原型化合物来探究该设计理念，获得了对多种蛋白激酶的强效抑制作用。
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