Development of 'DFG-out' inhibitors of gatekeeper mutant kinases
- Authors
- Choi, Hwan Geun; Zhang, Jianming; Weisberg, Ellen; Griffin, James D.; Sim, Taebo; Gray, Nathanael S.
- Issue Date
- 2012-08-15
- Publisher
- Pergamon Press Ltd.
- Citation
- Bioorganic & Medicinal Chemistry Letters, v.22, no.16, pp.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. (C) 2012 Elsevier Ltd. All rights reserved.
- Keywords
- CHRONIC MYELOID-LEUKEMIA; ABL TYROSINE KINASE; BCR-ABL; SELECTIVE INHIBITOR; RESISTANCE; DISCOVERY; IMATINIB; SRC; AMN107; CELLS; CHRONIC MYELOID-LEUKEMIA; ABL TYROSINE KINASE; BCR-ABL; SELECTIVE INHIBITOR; RESISTANCE; DISCOVERY; IMATINIB; SRC; AMN107; CELLS; T315I Bcr-Abl; Kinase inhibitor; Gatekeeper mutant; Type II inhibitor; Thiazolo[5,4-b]pyridine
- ISSN
- 0960-894X
- Appears in Collections:
- KIST Article > 2012
- Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.
KIST 리포지터리는 국립중앙도서관 OAK 보급사업으로 구축되었습니다.