Issue 1, 2015
From the journal:

Organic & Biomolecular Chemistry

Design and synthesis of potent hydroxamate inhibitors with increased selectivity within the gelatinase family†

José María Zapico,a   Anna Puckowska,ab   Kamila Filipiak,ac   Claire Coderch,a   Beatriz de Pascual-Teresa*a  and  Ana Ramos*a  

* Corresponding authors

a Departamento de Química y Bioquímica, Facultad de Farmacia, Universidad CEU San Pablo, Urbanización Monteprincipe, 28668 Madrid, Spain
E-mail: bpaster@ceu.es, aramgon@ceu.es
Fax: (+34) 913510496
Tel: (+34) 913724724, (+34) 913724796

b Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Bialystok, Poland

c Department of Molecular Biology, Faculty of Biotechnology and Natural Sciences, The John Paul II Catholic University of Lublin, 20-718 Lublin, Poland

Abstract

MMP-2 is a validated target for the development of anticancer agents. Herein we describe the synthesis of a new series of potent phenylalanine derived hydroxamates, with increased MMP-2/MMP-9 selectivity compared to analogous hydroxamates described previously. Docking and molecular dynamics experiments have been used to account for this selectivity, and to clarify the role of the triazole ring in the binding process.

Graphical abstract: Design and synthesis of potent hydroxamate inhibitors with increased selectivity within the gelatinase family

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Article information

DOI
https://doi.org/10.1039/C4OB01516A
Article type
Paper
Submitted
18 Jul 2014
Accepted
01 Oct 2014
First published
01 Oct 2014

Org. Biomol. Chem., 2015,13, 142-156

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Design and synthesis of potent hydroxamate inhibitors with increased selectivity within the gelatinase family

J. M. Zapico, A. Puckowska, K. Filipiak, C. Coderch, B. de Pascual-Teresa and A. Ramos, Org. Biomol. Chem., 2015, 13, 142 DOI: 10.1039/C4OB01516A

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