Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474

被引：14
|
作者：
Gamage, Swarna A. [1 ]
Giddens, Anna C. [1 ]
Tsang, Kit Y. [1 ]
Flanagan, Jack U. [1 ,2 ]
Kendall, Jackie D. [1 ,2 ]
Lee, Woo-Jeong [3 ]
Baguley, Bruce C. [1 ,2 ]
Buchanan, Christina M. [2 ,3 ]
Jamieson, Stephen M. F. [1 ,2 ]
Shepherd, Peter R. [1 ,2 ,3 ]
Denny, William A. [1 ,2 ]
Rewcastle, Gordon W. [1 ,2 ]
机构：
[1] Univ Auckland, Fac Med & Hlth Sci, Auckland Canc Soc, Res Ctr, Private Bag 92019, Auckland 1142, New Zealand
[2] Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Private Bag 92019, Auckland 1142, New Zealand
[3] Univ Auckland, Fac Med & Hlth Sci, Dept Mol Med & Pathol, Private Bag 92019, Auckland 1142, New Zealand
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2017年 / 25卷 / 20期
关键词：
Phosphatidylinositol; 3-kinase; PI3K; p110; alpha; ZSTK474; PHOSPHOINOSITIDE; 3-KINASE; CLASS-I; PI3K INHIBITOR; ISOFORM SELECTIVITY; BREAST-CANCER; PIK3CA GENE; DISCOVERY; PATHWAY; KINASE; MECHANISMS;
D O I：
10.1016/j.bmc.2017.09.025
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：
Replacement of one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 (1) with sulfonamide containing substituents produced a new class of active and potent PI3K alpha inhibitors. Solubility issues prevented all but the 6-amino derivative 17 from being evaluated in vivo, but the clear activity of this compound demonstrated that this class of PI3K inhibitor shows great promise. (C) 2017 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5859 / 5874
页数：16
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