Design, Synthesis and in-vitro Screening of New 1H-Pyrazole and 1,2-Isoxazole Derivatives as Potential Inhibitors for ROS and MAPK14 Kinases
- Design, Synthesis and in-vitro Screening of New 1H-Pyrazole and 1,2-Isoxazole Derivatives as Potential Inhibitors for ROS and MAPK14 Kinases
- Mohammad M. Al-Sanea; Ibrahim M. El-deeb; 이소하
- 1H-pyrazoles; 1,2-Isoxazole; ROS receptor; MARK14; Kinases
- Issue Date
- Bulletin of the Korean Chemical Society
- VOL 34, NO 2, 437-442
- 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.
- Appears in Collections:
- KIST Publication > Article
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.