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

ㆍ 저자명: Al-Sanea. Mohammad M.,El-Deeb. Ibrahim M.,Lee. So Ha
ㆍ 간행물명: Bulletin of the Korean Chemical Society
ㆍ 권/호정보: 2013년|34권 2호|pp.437-442 (6 pages)
ㆍ 발행정보: 대한화학회
ㆍ 파일정보: 정기간행물|ENG|
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ㆍ 주제분야: 기타

이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.

서지반출

기타언어초록

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 ${mu}M$ and 3.00 ${mu}M$ 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.

키워드

1H-Pyrazoles 1 2-Isoxazole ROS receptor MARK14 Kinases

다운URL