Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors

被引：53

作者：

Mai, Antonello

Valente, Sergio

Cheng, Donghang

Perrone, Andrea

Ragno, Rino

Simeoni, Silvia

Sbardella, Gianluca

Brosch, Gerald

Nebbioso, Angela

Conte, Mariarosaria

Altucci, Lucia

Bedford, Mark T.

机构：

[1] Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Università degli Studi di Roma La Sapienza, 00185 Roma

[2] University of Texas, M.D. Anderson Cancer Center, Science Park-Research Division, Smithville

[3] Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, 84084 Fisciano (SA), via Ponte Don Melillo

[4] Division of Molecular Biology, Biocenter, Innsbruck Medical University, 6020 Innsbruck

[5] Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, 80138 Napoli

来源：

CHEMMEDCHEM | 2007年 / 2卷 / 07期

关键词：

D O I：

10.1002/cmdc.200700023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(Chemical Equation Presented) Coding control: Protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) are epigenetic enzymes involved in regulation of gene expression and cellular processes. A new series of histone/protein methyltransferase inhibitors based on the 1,5-diphenyl-1,4-pentadien-3-one scaffold is reported. The described compounds showed various degrees of selectivity against the tested PRMTs (PRMT1 and CARM1) and HKMT (SET7). © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：987 / 991

页数：5

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