Synthesis and Biological Activity of New 4-(Pyridin-4-yl)-(3-methoxy-5-methylphenyl)- 1H-pyrazoles Derivatives as ROS Receptor Tyrosine Kinase Inhibitors

Bulletin of the Korean chemical society

Dong Keun Han¹  Byung Sun Park¹  So Ha Lee¹  Ibrahim M. El-deeb¹  Kyung Ho Yoo¹  Jin Sung Tae¹ 

关键词: 1H-pyrazoles;    ROS receptor;    Tyrosine kinase inhibitor;    Cancer;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A series of new 4-(pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles (6a-k & 7a-l) has been rationally designed based on the structure of the lead compound KIST301080, a selective ROS receptor tyrosine kinase inhibitor, in order to study the activity of ROS of this new class of inhibitors. The compounds were synthesized and screened against ROS kinase, where compound 6h showed moderate inhibitory activity with an IC50 value of 6.25 μM. The study emphasized the importance of the acetonitrile group at the pyrazole ring and also the importance of having a hydrogen bond donor on the distal phenyl ring linked to the pyridine moiety.

【 授权许可】

Unknown