Development of ‘DFG-out’ inhibitors of gatekeeper mutant kinases

Title
Development of ‘DFG-out’ inhibitors of gatekeeper mutant kinases
Authors
최환근Jianming ZhangEllen WeisbergJames D. Griffin심태보Nathanael S. Gray
Keywords
T315I Bcr-Abl; Kinase inhibitor; Gatekeeper mutant; Type II inhibitor; Thiazolo[5,4-b]pyridine
Issue Date
2012-08
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 22, NO 16, 5297-5302
Abstract
HG-7-85-01(22) and HG-7-86-01(26) are thiazolo[5,4-b]pyridine containing type II tyrosine kinase inhibitors with potent cellular activity against both wild-type and ‘gatekeeper’ mutant T315I- Bcr-Abl. Here we report on the ‘hybrid design’ concept and subsequent structure activity guided optimization efforts that resulted in the development of these inhibitors.
URI
http://pubs.kist.re.kr/handle/201004/43078
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE