Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors

被引：27

作者：

Sleebs, Brad E. ^{[1
,2
,3
]}

Levit, Alla ^{[1
,2
,3
]}

Street, Ian P. ^{[1
,2
,3
]}

Falk, Hendrik ^{[1
,2
,3
]}

Hammonds, Tim ^{[4
]}

Wong, Al Ching ^{[4
]}

Charles, Mark D. ^{[4
]}

Olson, Michael F. ^{[5
]}

Baell, Jonathan B. ^{[1
,2
,3
]}

机构：

[1] Walter & Eliza Hall Inst Med Res, Parkville, Vic 3052, Australia

[2] Canc Therapeut CRC PIL, Bundoora, Vic 3086, Australia

[3] Univ Melbourne, Dept Med Biol, Parkville, Vic 3010, Australia

[4] Canc Res Technol Ltd, London WC1E 6BT, England

[5] Beatson Inst Canc Res, Glasgow G61 1BD, Lanark, Scotland

来源：

MEDCHEMCOMM | 2011年 / 2卷 / 10期

基金：

澳大利亚国家健康与医学研究理事会;

关键词：

ACTIN DYNAMICS; KINASE;

D O I：

10.1039/c1md00137j

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A high throughput chemical screening campaign has led to the identification of 3-aminobenzo[b]thiophene-2-carboxamides as LIMK I inhibitors. Evolution of bicyclic hits to the tricyclic 4-aminobenzothieno[3,2-d]pyrimidine, using a traditional medicinal chemistry SAR guided approach, resulted in a significant increase in potency. Further elaboration has seen the 7-phenyl-4-aminobenzothieno[3,2-d]pyrimidine emerge as a LIMK I inhibitor lead candidate.

引用

页码：977 / 981

页数：5

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