Solid-phase Synthesis and Preliminary Evaluation of 1,6,8-Trisubstituted Tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as a NF-kB Inhibitor

Bulletin of the Korean chemical society

Jin-Woong Kim¹  Jung-Hyuck Cho¹  Taehee Han¹  JongBaek Lee¹  Chang-Hyun Oh¹ 

关键词: Bicyclic ¥â-turn mimetics;    NF-kB inhibitor;    Solid phase;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

The solid-phase synthesis of new series of 1,6,8-trisubstituted tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as bicyclic �?-turn mimetics is described. Their NF-kB inhibition activities were tested and the effect of substituents on bicyclic ring was investigated. Among the prepared compounds, the fluorobenzyl and methoxybenzyl group substituted compounds 26 and 27 at C-1 and C-8 position showed more inhibitory activities than the others. Tested at a concentration of 10 uM, these two compounds showed a 60% inhibition against the target NF kB 549.

【 授权许可】

Unknown