abs

학술발표회초록보기

Inquiry on Abstract abstract@kcsnet.or.kr

Inquiry on Payment member@kcsnet.or.kr

현재 가능한 작업은 아래와 같습니다.
  • 03월 02일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

129th General Meeting of Korean Chemical Society & Exposition Discovery of indolin-2-one analogs as PIM kinase inhibitors

Submission Date :
1 / 20 / 2022 , 16 : 43 : 58
Abstract Number :
129012000458
Presenting Type:
Poster Presentation
Presenting Area :
Medicinal Chemistry
Authors :
Hyeonseong Choo, Jinho Lee*, Victor Sukbong Hong*
Department of Chemistry, Keimyung University, Korea
Assigned Code :
MEDI.P-359 Assigend Code Guideline
Presenting Time :
April 14 (THU) 11:00~13:00
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.