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| Type |
Poster Presentation |
| Area |
의약화학 |
| Room No. |
포스터발표장 |
| Time |
4월 20일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-439 |
| Subject |
Design and synthesis of novel triazolo[3,4-d]pyridazin-3-yl pyridine-2-amine derivatives as novel Bruton’s tyrosine kinase inhibitors |
| Authors |
김덕운, 정현석, 황종연1, 김필호1, 류도현, 조성윤2,*
성균관대학교 화학과, Korea
1한국화학연구원 의약화학연구센터, Korea
2한국화학연구원 난치성질환치료제연구센터, Korea
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| Abstract |
Bruton’s tyrosine kinase (BTK), a non-receptor tyrosine kinase, plays an important role in the B cell receptor signal transduction pathways regulating activation, survival, proliferation, and differentiation of B-lineage lymphoid cells. Mutations in gene encoding human BTK lead to X-linked agammaglobulinemia (XLA) in humans and X-linked immunodeficiency (Xid) in mice. Aberrant activation of Btk is implicated with the pathogenesis of B cell lymphoma because B cells play a central role in the pathogenesis of several autoimmune diseases and B cell malignancies. BTK inhibitors are anticipitated to be important clinical options for treatin rheumatoid arthritis and lupus. Indeed, inhibition of BTK has been considered as an effective and attractive therapeutic target for B cell related malignancies. In this report, we synthesized a series of novel triazolo[3,4-d]pyridazin-3-yl pyridine-2-amine derivatives that were substituted with diphenyl moieties and evaluated BTK kinase inhibitory activity and cell based proliferation assay. Some of the compounds displayed excellent activity in vitro enzyme and cell-based assay.
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| E-mail |
godejrwk@naver.com |
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119th General Meeting of the KCS