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Arylamino Bisphosphonates: Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrase XII

Arylamino Bisphosphonates: Potent and Selective Inhibitors of the Tumor-Associated Carbonic Anhydrase XII

Marilena Tauro, Fulvio Loiodice, Mariangela Ceruso, Claudiu T Supuran, Paolo Tortorella

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1941-3.

PMID: 24650641

Abstract:

A set of matrix metalloproteinases (MMPs) inhibitors, containing a bisphosphonate moiety (BP), has been evaluated for the inhibitory activity of carbonic anhydrases (CAs, EC 4.2.1.1). Human (h) isoforms hCA I, II, IX, XII and XIV were included in the study due to their involvement in crucial physiologic and pathologic processes. Some of these molecules selectively inhibited CA XII in the nanomolar range, showing an attractive dual mechanism (anti-MMP and anti-CA) of action as potential antitumor agents. The BP inhibitors investigated in this study are also excellent leads for obtaining even more effective compounds able to selectively target membrane-bound CA XII and having the potential to be used as tools for understanding physiologic processes regulated by this isoform.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP203915597	MMP Inhibitor II - CAS 203915-59-7		203915-59-7	Price

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