title: Synthesis and biological evaluation of new pyrimidine-4-yl-ethanol derivatives as ROS1 kinase inhibitors.
abstract: As a part of trials to target ROS1 kinase with potential inhibitors, a novel series of pyrimidin-4-yl-ethanol and ethanone derivatives (4a-f, 5a-f, 6a-f and 7a-f) have been designed based on previously discovered lead compounds KIST301072 and KIST301080, and synthesized on 4-5 steps according to compounds. The structures of the newly synthesized compounds have been confirmed on (1)H-NMR, (13)C-NMR and IR. Most of the tested compounds showed ROS1 kinase inhibitory activity in micromolar range.
authors.affiliation: Department of Biological Chemistry, Korea University of Science and Technology , Gwahangno, Yuseong-gu, Daejeon , Republic of Korea and.
authors.forename: Ahmed Z
authors.initials: AZ
authors.lastname: Abdelazem
authors.forename: So Ha
authors.initials: SH
authors.lastname: Lee
mesh_terms: D015195:Drug Design; D009682:Magnetic Resonance Spectroscopy; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011518:Proto-Oncogene Proteins; D011743:Pyrimidines; D011505:Protein-Tyrosine Kinases; C062333:ROS1 protein, human
keywords: Drug; ROS1; non-small cell lung cancer; receptor tyrosine kinase