• Title/Summary/Keyword: Pyrimidine-2,4-diones

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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

  • Kim, Jin-Woong;Cho, Jung-Hyuck;Han, Tae-hee;Lee, Jong-Baek;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.27 no.4
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    • pp.484-488
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    • 2006
  • The solid-phase synthesis of new series of 1,6,8-trisubstituted tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as bicyclic $\beta$-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.