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Issue 1, 2015
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Design and synthesis of potent hydroxamate inhibitors with increased selectivity within the gelatinase family

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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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Publication details

The article was received on 18 Jul 2014, accepted on 01 Oct 2014 and first published on 01 Oct 2014


Article type: Paper
DOI: 10.1039/C4OB01516A
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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