Park, Byung Sun El-Deeb, Ibrahim M. Yoo, Kyung Ho Han, Dong Keun Tae, Jin Sung Lee, So Ha 2024-01-20T13:34:22Z 2024-01-20T13:34:22Z 2021-09-04 2012-11 0253-2964 https://pubs.kist.re.kr/handle/201004/128734 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 mu M. 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. English WILEY-V C H VERLAG GMBH Synthesis and Biological Activity of New 4-(Pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles Derivatives as ROS Receptor Tyrosine Kinase Inhibitors Article 10.5012/bkcs.2012.33.11.3629 1 BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.33, no.11, pp.3629 - 3634 BULLETIN OF THE KOREAN CHEMICAL SOCIETY 33 11 3629 3634 N scie scopus kci ART001711839 000311816000019 2-s2.0-84870012206 Chemistry, Multidisciplinary Chemistry Article GENE 1H-pyrazoles ROS receptor Tyrosine kinase inhibitor Cancer