Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group

被引：14

作者：

Kendall, Jackie D. ^{[1
,2
]}

Marshall, Andrew J. ^{[1
]}

Giddens, Anna C. ^{[1
]}

Tsang, Kit Yee ^{[1
]}

Boyd, Maruta ^{[1
]}

Frederick, Raphael ^{[1
]}

Lill, Claire L. ^{[3
]}

Lee, Woo-Jeong ^{[3
]}

Kolekar, Sharada ^{[3
]}

Chao, Mindy ^{[3
]}

Malik, Alisha ^{[3
]}

Yu, Shuqiao ^{[3
]}

Chaussade, Claire ^{[2
,3
]}

Buchanan, Christina M. ^{[2
,3
]}

Rewcastle, Gordon W. ^{[1
,2
]}

Baguley, Bruce C. ^{[1
,2
]}

Flanagan, Jack U. ^{[1
,2
]}

Denny, William A. ^{[1
,2
]}

Shepherd, Peter R. ^{[2
,3
]}

机构：

[1] Univ Auckland, Sch Med & Hlth Sci, Auckland Canc Soc Res Ctr, Auckland 1142, New Zealand

[2] Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1142, New Zealand

[3] Univ Auckland, Sch Med & Hlth Sci, Dept Mol Med & Pathol, Auckland 1142, New Zealand

来源：

MEDCHEMCOMM | 2014年 / 5卷 / 01期

关键词：

KINASE-INHIBITORS; PATHWAY INHIBITORS; P110-ALPHA; THIOAMIDES; DISCOVERY; CANCER; DESIGN;

D O I：

10.1039/c3md00221g

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：

As part of our investigation into the pyrazolo[1,5-a] pyridines as novel PI3K inhibitors, we report a range of analogues where the central linker portion of the molecule was varied while retaining the pyrazolo[1,5-a] pyridine and arylsulfonyl or arylcarbonyl groups. Isostere generating software BROOD was used to assist with producing ideas. The isoform selectivity of the compounds varied from pan-PI3K for compound 41 to p110 alpha-selective for compound 58 or p110 delta-selective for compound 57. The latter two compounds varied only in their sulphur oxidation state.

引用

页码：41 / 46

页数：6

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