New C 4-and C 1-derivatives of furo [3, 4-c] pyridine-3-ones and related compounds: Evidence for site-specific inhibition of the constitutive proteasome and its …

…, M Reboud-Ravaux, M Bouvier-Durand

Index: Hovhannisyan, Anna; Pham, The Hien; Bouvier, Dominique; Piroyan, Alexander; Dufau, Laure; Qin, Lixian; Cheng, Yan; Melikyan, Gagik; Reboud-Ravaux, Michele; Bouvier-Durand, Michelle Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 6 p. 1571 - 1580

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Citation Number: 4

Abstract

Abstract A set of 18 new C 4 and C 1 derivatives of nor-cerpegin (1, 1-dimethyl furo [3, 4-c] pyridine-3-one), 6 model compounds (γ-and δ-lactones) and 20 furo-or thieno [2, 3-d]- pyrimidine-4-one related compounds were designed and synthesized. Each compound was assayed for inhibition of CT-L, TL and PA proteolytic activities of 20S constitutive proteasome (c20S). Most performant compounds were also assayed on 20S ...