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J Enzyme Inhib Med Chem. 2015 Apr;30(2):290-8. doi: 10.3109/14756366.2014.920838. Epub 2014 Jun 18.

Synthesis and biological evaluation of new pyrimidine-4-yl-ethanol derivatives as ROS1 kinase inhibitors.

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1
Department of Biological Chemistry, Korea University of Science and Technology , Gwahangno, Yuseong-gu, Daejeon , Republic of Korea and.

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.

KEYWORDS:

Drug; ROS1; non-small cell lung cancer; receptor tyrosine kinase

PMID:
24939104
DOI:
10.3109/14756366.2014.920838
[Indexed for MEDLINE]
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