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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-304 |
| Subject |
Design, Synthesis of N-(5-methyl-2-(phenylamino)thiazolo[5,4-d]pyrimidin-7-yl)benzenesulfonamide derivatives as an inhibitor of cyclin-dependent kinases(CDKs) |
| Authors |
HYEJIN KWON, eunsil Lee1, Young Dae Gong*
Department of Chemistry, Dongguk University, Korea
1Medicinal Chemistry Laboratory, Dongguk University, Korea
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| Abstract |
Roscovitine, also called Seliciclib, is biologically well used inhibitor which is targeting cyclin-dependent kinases(CDKs). CDKs(CDK1, CDK2, CDK5 and CDK7), drug targets of Roscovitine, are involved in cell cycle including mRNA process, transcription and the cellular differentiation. Roscovitine regulates abnormal cell cycle by binding to ATP binding site. Therefore, it is currently evaluated as a potential drug of cancers, neurodegenerative diseases, inflammation, viral infections, polycystic kidney disease etc. In this context, we’ve tried to design a new drug targeting CDKs by referring to the structure of Roscovitine. We’ve synthesized Thiazolopyrimidine-based compound By replacing the imidazole which is part of purine, the main structure of Roscovitine, with thiazole. Also, various substituents were introduced at carbons(2,6,8) of thiazolopyrimidine to increase the structural diversity. Starting from 4,6-dichloro-2-methylpyrimidin-5-amine, we have synthesized about 100 kinds of compound by substituting 8 kinds of benzenesulfonamide at carbon 6 in thiazolopyrimidine which were synthesized by cyclization of 4,6-dichloro-2-N-pyrimidin-5-amine using 20 kinds of isothiocyanate. |
| E-mail |
khgin@hanmail.net |
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120th General Meeting of the KCS