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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2+3 |
| Time |
10월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-308 |
| Subject |
Synthesis and biological evaluation of new pyrimidine derivatives for kinase inhibitor
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| Authors |
Tae Young Kim, Eslam M. H. Ali1, Jae Yeol Lee*, So Ha LEE2,*
Department of Chemistry, Kyung Hee University, Korea
1Department of Biological Chemistry, University of Science and Technology, Egypt
2Chemical Kinomics Research Center, Korea Institute of Science and Technology, Korea
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| Abstract |
Cancer cells grow by the signal transduction pathway like normal cells and there are various protein kinases in the cell that play an important role in the signaling pathway. Until recently, it has been known that among the various kinases, SIK kinase has three types of SIK1, SIK2, and SIK3. SIK2 kinase (salt-inducible kinase 2) is a serine / threonine protein kinase belonging to the AMP-activating protein kinase (AMPK) family and is overexpressed in 30% of ovarian cancer patients. Prostate cancer is generally a cancer that can be treated surgically, but about 10-15% of patients have difficulty with surgery and require medication. SIK2 kinase may be a target for cancer treatment. It is also reported to be involved in triple-negative breast cancer (TNBC), a difficult breast cancer to treat. SIK2 receptor kinase has been shown to occur at very high frequency in ovarian, prostate, and breast cancer cells, and has recently been suggested as a new target for kinase inhibitors. Therefore, inhibition of SIK2 can be an effective therapeutic strategy in these cancers. For developing SIK2 inhibitors, we synthesized new pyrimidine derivatives based on the hit scaffolds. Among the synthesized compounds, KIST301613 was identified as a lead SIK2 inhibitor. The optimization of novel SIK2 inhibitors to further enhance potency and physicochemical properties is now in progress.
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| E-mail |
tykim373@kist.re.kr |
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120th General Meeting of the KCS