发现一类新型的 2-氨基嘧啶作为 CDK1 和 CDK2 的抑制剂。
Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors.
机构信息
Department of Chemistry, Keimyung University, Daegu 704-701, South Korea.
出版信息
Bioorg Med Chem Lett. 2011 Jul 15;21(14):4203-5. doi: 10.1016/j.bmcl.2011.05.081. Epub 2011 May 27.
PMID:21684737
Abstract
A series of new 2-(2-aminopyrimidin-4-yl)phenol derivatives were synthesized as potential antitumor compounds. Substitution with pyrrolidine-3,4-diol at the 4-position of phenol provided potent inhibitory activity against CDK1 and CDK2. X-ray crystal structural studies were performed to account for the effect of the substituent on both the enzymatic and cell growth inhibitory activities.
摘要
一系列新型 2-(2-氨基嘧啶-4-基)苯酚衍生物被合成出来作为潜在的抗肿瘤化合物。在苯酚的 4-位用吡咯烷-3,4-二醇取代提供了对 CDK1 和 CDK2 的强大抑制活性。进行了 X 射线晶体结构研究，以解释取代基对酶和细胞生长抑制活性的影响。
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