Kim, Jin-Woong Cho, Jung-Hyuck Han, Taehee Lee, JongBaek Oh, Chang-Hyun 2024-01-21T03:05:42Z 2024-01-21T03:05:42Z 2021-09-01 2006-04-20 0253-2964 https://pubs.kist.re.kr/handle/201004/135571 The solid-phase synthesis of new series of 1,6,8-trisubstituted tetrahydro-2H-pyrazino[1,2-alpha]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. English WILEY-V C H VERLAG GMBH KAPPA-B CONFORMATIONAL-ANALYSIS MAJOR CULPRIT MIMETICS RECEPTOR CANCER INFLAMMATION ACTIVATION SCAFFOLDS DESIGN 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 Article 1 BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.27, no.4, pp.484 - 488 BULLETIN OF THE KOREAN CHEMICAL SOCIETY 27 4 484 488 scie scopus kci ART001008578 000237498900006 2-s2.0-33646592257 Chemistry, Multidisciplinary Chemistry Article KAPPA-B CONFORMATIONAL-ANALYSIS MAJOR CULPRIT MIMETICS RECEPTOR CANCER INFLAMMATION ACTIVATION SCAFFOLDS DESIGN bicyclic beta-turn mimetics NF-kB inhibitor solid phase