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Abdelazem, Ahmed Z.,Lee, So Ha Informa UK Ltd. 2015 Journal of enzyme inhibition and medicinal chemist Vol.30 No.2
<P>As a part of trials to target ROS1 kinase with potential inhibitors, a novel series of pyrimidin-4-yl-ethanol and ethanone derivatives (<B>4a</B>-<B>f</B>, <B>5a</B>-<B>f</B>, <B>6a</B>-<B>f</B> and <B>7a</B>-<B>f</B>) 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 <SUP>1</SUP>H-NMR, <SUP>13</SUP>C-NMR and IR. Most of the tested compounds showed ROS1 kinase inhibitory activity in micromolar range.</P>
Mohammad M. Al-Sanea,박병선,Ahmed Z. Abdelazem,Khalid B. Selim,유경호,심태보,태진성,이소하 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.1
A series of rationally designed ROS1 tyrosine kinase inhibitors 6a–9b with bipyridinyl pyrazole scaffold was synthesized and screened. The scaffold itself has showed an exclusive selectivity profile over ROS1 closely related kinases,ALKand c-Met. The aim of this study was to further explore the structure–activity relationships (SAR) of the bipyridinyl pyrazole core structure, and to improve its ROS1 inhibitory potency. The rational of this study was to explore the nature of the proposed binding site for the pyrazoleNHsubstituents. Careful selections of pyrazoleNHsubstituent groups along with their regioisomers were considered. The compounds exhibited high degree of potency, IC50 values of 21–159 nM. A detailed SAR of bipyridinyl pyrazole scaffold has been finally well established and the virtual screening strategy, through molecular docking, has been performed for this type of ROS1 kinase inhibitors and the docked poses along with the activity data have gone in consistent with SAR specifications.