Epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors

…, G Sbardella, F De Bellis, M Miceli…

Index: Mai, Antonello; Rotili, Dante; Tarantino, Domenico; Ornaghi, Prisca; Tosi, Federica; Vicidomini, Caterina; Sbardella, Gianluca; Nebbioso, Angela; Miceli, Marco; Altucci, Lucia; Filetici, Patrizia Journal of Medicinal Chemistry, 2006 , vol. 49, # 23 p. 6897 - 6907

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Citation Number: 117

Abstract

A number of new compounds bearing two ortho-bromo-and ortho, ortho-dibromophenol moieties linked through a saturated/unsaturated, linear/(poly) cyclic spacer (compounds 1– 9) were prepared as simplified analogues of AMI-5 (eosin), a recently reported inhibitor of both protein arginine and histone lysine methyltransferases (PRMTs and HKMTs). Such compounds were tested against a panel of PRMTs (RmtA, PRMT1, and CARM1) and ...

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