鉴定 5,6-取代的 4-氨基噻吩并[2,3-d]嘧啶类化合物作为 LIMK1 抑制剂。
Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors.
机构信息
The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia.
出版信息
Bioorg Med Chem Lett. 2011 Oct 1;21(19):5992-4. doi: 10.1016/j.bmcl.2011.07.050. Epub 2011 Jul 23.
PMID:21852129
Abstract
4-Aminobenzothieno[3,2-d]pyrimidines were previously identified in a high throughput screening campaign as LIMK1 inhibitors. Scaffold reversal led to the identification of a series of simple 5,6-substituted 4-aminothieno[2,3-d]pyrimidines with low micromolar inhibition of LIMK1.
摘要
4-氨基苯并噻吩并[3,2-d]嘧啶类化合物曾在高通量筛选中被鉴定为 LIMK1 抑制剂。骨架反转导致了一系列简单的 5,6-取代的 4-氨基噻吩并[2,3-d]嘧啶类化合物的发现，它们对 LIMK1 的抑制作用为低微摩尔级。
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