A new series of N 5 derivatives of the 1, 1, 5-trimethyl furo [3, 4-c] pyridine-3, 4-dione (cerpegin) selectively inhibits the post-acid activity of mammalian 20S …

…, L Tian, M Reboud-Ravaux, G Melikyan…

Index: Pham, The Hien; Hovhannisyan, Anna; Bouvier, Dominique; Tian, Lei; Reboud-Ravaux, Michele; Melikyan, Gagik; Bouvier-Durand, Michelle Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3822 - 3827

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Citation Number: 11

Abstract

A large set of N5-derivatives of cerpegin (1, 1, 5-trimethyl furo [3, 4-c] pyridine-3, 4-dione) was designed and synthesized in high yields by a simple and handy method using various primary amines for a pyridine cycle synthesis. The effects of 29 derivatives on the three types of catalytic sites of purified mammalian 20S proteasomes (CT-L, TL and PA) were measured. Most of the new compounds specifically inhibited the PA activity, in the micromolar range. ...

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