3,1-benzothiazines, 1,4-benzodioxines and 1,4-benzoxazines as inhibitors of matriptase-2: Outcome of a focused screening approach

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Abstract

© 2016 by the authors; licensee MDPI, Basel, Switzerland. The liver enzyme matriptase-2 is a multi-domain, transmembrane serine protease with an extracellular, C-terminal catalytic domain. Synthetic low-molecular weight inhibitors of matriptase-2 have potential as therapeutics to treat iron overload syndromes, in particular in patients with β-thalassemia. A sub-library of 64 compounds was screened for matriptase-2 inhibition and several active compounds were identified. (S)-Ethyl 2-(benzyl(3-((4-carbamidoylphenoxy)methyl)-2,3-dihydrobenzo[b][1,4] dioxin-6-yl)amino)-2-oxoacetate ((S)-12) showed an IC50 value of less than 10 µM. Structure-activity relationships were discussed and proposals to design new matriptase-2 inhibitors were made.

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Roydeva, P. G., Beckmann, A. M., Stirnberg, M., Cesar, J., Kikelj, D., Ilaš, J., & Gütschow, M. (2016). 3,1-benzothiazines, 1,4-benzodioxines and 1,4-benzoxazines as inhibitors of matriptase-2: Outcome of a focused screening approach. Pharmaceuticals, 9(1). https://doi.org/10.3390/ph9010002

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