Design, Synthesis and in-vitro Screening of New 1H-Pyrazole and 1,2-Isoxazole Derivatives as Potential Inhibitors for ROS and MAPK14 Kinases

Title
Design, Synthesis and in-vitro Screening of New 1H-Pyrazole and 1,2-Isoxazole Derivatives as Potential Inhibitors for ROS and MAPK14 Kinases
Authors
Mohammad M. Al-SaneaIbrahim M. El-deeb이소하
Keywords
1H-pyrazoles; 1,2-Isoxazole; ROS receptor; MARK14; Kinases
Issue Date
2013-02
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 34, NO 2, 437-442
Abstract
A new series of 4-(2-(substituted)pyridin-4-yl)-3-(3-methoxy-5-methylphenyl)-1H-pyrazoles (4a-f) and their 1,2-isoxazole analogues (5a-f) has been rationally designed, synthesized and screened against both ROS and MAPK14 kinases. Compounds 4b, 4c and 4e showed moderate inhibitions against both ROS and MAPK14 kinases. Compound 4e has showed the strongest inhibitions with IC50 values of 1.25 μM and 3.00 μM against ROS and MAPK14 kinases, respectively. A brief structure-activity relationship study and a molecular modeling study were made revealing a group of essential structural features for good kinase inhibitory activity within this new class of kinase inhibitors.
URI
http://pubs.kist.re.kr/handle/201004/44613
ISSN
02532964
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KIST Publication > Article
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