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Discovery of 5-methyl-N-(2-arylquinazolin-7-yl)isoxazole-4-carboxamide analogues as highly selective FLT3 inhibitorsopen access
- Issue Date
- Jan-2020
- Publisher
- Taylor & Francis
- Keywords
- FLT3; FLT3-ITD; FLT3-TKD; quinazoline; selectivity
- Citation
- Journal of Enzyme Inhibition and Medicinal Chemistry, v.35, no.1, pp 1110 - 1115
- Pages
- 6
- Indexed
- SCIE
SCOPUS
- Journal Title
- Journal of Enzyme Inhibition and Medicinal Chemistry
- Volume
- 35
- Number
- 1
- Start Page
- 1110
- End Page
- 1115
- ISSN
- 1475-6366
1475-6374
- Abstract
- A series of 4-arylamido 5-methylisoxazole derivatives with quinazoline core was designed and synthesised based on conformational rigidification of a previous type II FMS inhibitor. Most of quinazoline analogues displayed activity against FLT3 and FLT3-ITD. Compound 7d, 5-methyl-N-(2-(3-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)phenyl)quinazolin-7-yl)isoxazole-4-carboxamide, exhibited the most potent inhibitory activity against FLT3 (IC50= 106 nM) with excellent selectivity profiles over 36 other protein kinases including cKit and FMS kinase. Compound 7d was also active in FLT-ITD, with an IC50 value of 301 nM, and other FLT3 mutants showing potential as an AML therapeutics.
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Related Researcher
- Hah, Jung Mi
- COLLEGE OF PHARMACY (DEPARTMENT OF PHARMACY)