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Issue 4, 2019
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From a MMP2/CK2 multitarget approach to the identification of potent and selective MMP13 inhibitors

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Abstract

In this article, we describe our efforts in the search of MMP2/CK2 dual targeting inhibitors. We have followed a rational drug design approach based on our experience in the selective inhibition of these two enzymes. We have successfully obtained highly active MMP2 (10, IC50 = 70 nM; 11, IC50 = 100 nM) and CK2 (16a, IC50 = 500 nM) inhibitors. However, structural fine tuning of these small molecules to simultaneously target both enzymes turned out to be an unattainable goal. Unexpectedly, we were lucky to identify new and selective MMP13 inhibitors (10, IC50 = 3.7 nM and 11, IC50 = 5.6 nM) with a novel TBB-derived scaffold. These compounds constitute an interesting starting point for further optimization.

Graphical abstract: From a MMP2/CK2 multitarget approach to the identification of potent and selective MMP13 inhibitors

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Publication details

The article was received on 30 Nov 2018, accepted on 18 Dec 2018 and first published on 18 Dec 2018


Article type: Paper
DOI: 10.1039/C8OB02990C
Citation: Org. Biomol. Chem., 2019,17, 916-929

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    From a MMP2/CK2 multitarget approach to the identification of potent and selective MMP13 inhibitors

    M. Pastor, J. M. Zapico, C. Coderch, M. Maslyk, R. Panchuk, B. de Pascual-Teresa and A. Ramos, Org. Biomol. Chem., 2019, 17, 916
    DOI: 10.1039/C8OB02990C

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