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Dual Carbonic anhydrase/matrix Metalloproteinase Inhibitors Incorporating Bisphosphonic Acid Moieties Targeting Bone Tumors

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

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2617-20.

PMID: 24813742

Abstract:

A set of bisphosphonate matrix metalloproteinase (MMP) inhibitors was investigated for inhibitory activity against several carbonic anhydrase (CA, EC 4.2.1.1) isozymes, some of which are overexpressed in hypoxic tumors. Some of the bisphosphonate revealed to be very potent inhibitors (in the low nanomolar range) of the cytosolic isoform CA II and the membrane-bound CA IX, XII and XIV isozymes, a feature useful for considering them as interesting compounds for bone resorption inhibition applications. We suggest here that it is possible to develop dual enzyme inhibitors bearing bisphosphonate moieties that may target both MMPs and CAs, two families of enzymes involved in tumor formation, growth, and metastasis.

Chemicals Related in the Paper:

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