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114th General Meeting of Korean Chemical Society Novel Pyrrolo-Pyrimidine Derivativesas as FGFR4, Tie2/TEK and TrkA Kinase Inhibitors; Design, Synthesis and Biological Evaluation for Anticancer agents

Submission Date :
8 / 28 / 2014 , 15 : 29 : 29
Abstract Number :
Presenting Type:
Poster Presentation
Presenting Area :
Authors :
이주현, 서선희1, 강순방1, 정낙철, 금교창2,*
고려대학교 화학과, Korea
1한국과학기술연구원(KIST) 뇌의약연구단, Korea
2한국과학기술연구원(KIST) 케모인포메틱스연구센터, Korea
Assigned Code :
MEDI.P-968 Assigend Code Guideline
Presenting Time :
10월 15일 (수요일) 16:00~19:00
Development of kinase inhibitors has been extensively progressed as a target of cancer therapy. Among kinase inhibitors, we are interested in the pyrrolo-pyrimidine based inhibitors such as PKI166 (EGFR), CP-690 (JAK3), MPS-1-IN-1 (Mps1) and Meriolins (CDK2). Herein, a series of pyrrolo-pyrimidine derivatives were synthesized, and assessed against cancer cell lines and kinases. Several compounds, in the preliminary screening, displayed high EC50 values less than 4.5 μM against SK-BR-3, MCF-7 and HCT116 in in vitro assay. Among them, KKK5097 and 50101 showed high growth inhibitory effects against 60 cancer cell lines in the NCI-60 DTP screening program. The two compounds displayed high selectivity of FGFR4, Ti2/TEK and TrkA kinases against 59 kinds of kinase by Reaction Biology Corp. In particular, KKK5101 showed high IC50 values of those kinases, 6.71, 6.84 and 2.25 μM, respectively.