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제129회 대한화학회 학술발표회, 총회 및 기기전시회 Discovery of indolin-2-one analogs as PIM kinase inhibitors

2022년 1월 20일 16시 43분 58초
MEDI.P-359 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
4월 14일 (목요일) 11:00~13:00
Medicinal Chemistry
저자 및
Hyeonseong Choo, Jinho Lee*, Victor Sukbong Hong*
Department of Chemistry, Keimyung University, Korea
Proviral Integration Moloney murine leukemia virus (PIM) kinase, which is involved in the regulation of cellular processes such as survival, proliferation, cell cycle regulation, is overexpressed in hematological and solid cancers. It is a serine/threonine kinase with three homologous isomers of PIM-1, PIM-2, and PIM-3. PIM-1 kinase characteristically has a proline residue (Pro123) in the hinge region of the ATP binding site, and show high selectivity over other kinase inhibitors. In this study, using an indolin-2-one scaffold a series of novel compounds were designed and synthesized for PIM kinase inhibitor. Multiple substituents were introduced to the scaffold to make effective interaction not only with the carboxyl groups of Asp128 and Glu121, but also with the amino group of Lys67 of PIM-1 kinase. As a result of structure-activity relationship (SAR) study, the most potent inhibitor yielded IC50 values of 5.6 nM and 6.9 nM for PIM-1 and PIM-3, respectively.