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N-β-glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII.
Bioorg Med Chem Lett. 2011 Aug 01; 21(15):4447-50.BM

Abstract

The transmembrane isoforms of carbonic anhydrase (CA IX and XII) have been shown to be linked to carcinogenesis and their inhibition to arrest primary tumor and metastases growth. In this Letter, we present a series of peracetylated and deprotected N-β-glycosyl sulfamides that were tested for the inhibition of 4 carbonic anhydrase isoforms: the cytosolic hCA I and hCA II and transmembrane tumor-associated IX and XII. Compounds 1-4 and 6-8 selectively target cancer-associated CAs (IX and XII) with K(I)s in the low nanomolar range.

Authors+Show Affiliations

LADECOR, Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, La Plata, Argentina.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21723123

Citation

Rodríguez, Oscar M., et al. "N-β-glycosyl Sulfamides Are Selective Inhibitors of the Cancer Associated Carbonic Anhydrase Isoforms IX and XII." Bioorganic & Medicinal Chemistry Letters, vol. 21, no. 15, 2011, pp. 4447-50.
Rodríguez OM, Maresca A, Témpera CA, et al. N-β-glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII. Bioorg Med Chem Lett. 2011;21(15):4447-50.
Rodríguez, O. M., Maresca, A., Témpera, C. A., Bravo, R. D., Colinas, P. A., & Supuran, C. T. (2011). N-β-glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII. Bioorganic & Medicinal Chemistry Letters, 21(15), 4447-50. https://doi.org/10.1016/j.bmcl.2011.06.031
Rodríguez OM, et al. N-β-glycosyl Sulfamides Are Selective Inhibitors of the Cancer Associated Carbonic Anhydrase Isoforms IX and XII. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4447-50. PubMed PMID: 21723123.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - N-β-glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII. AU - Rodríguez,Oscar M, AU - Maresca,Alfonso, AU - Témpera,Carlos A, AU - Bravo,Rodolfo D, AU - Colinas,Pedro A, AU - Supuran,Claudiu T, Y1 - 2011/06/16/ PY - 2011/04/29/received PY - 2011/06/02/revised PY - 2011/06/06/accepted PY - 2011/7/5/entrez PY - 2011/7/5/pubmed PY - 2011/12/13/medline SP - 4447 EP - 50 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 21 IS - 15 N2 - The transmembrane isoforms of carbonic anhydrase (CA IX and XII) have been shown to be linked to carcinogenesis and their inhibition to arrest primary tumor and metastases growth. In this Letter, we present a series of peracetylated and deprotected N-β-glycosyl sulfamides that were tested for the inhibition of 4 carbonic anhydrase isoforms: the cytosolic hCA I and hCA II and transmembrane tumor-associated IX and XII. Compounds 1-4 and 6-8 selectively target cancer-associated CAs (IX and XII) with K(I)s in the low nanomolar range. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/21723123/N_β_glycosyl_sulfamides_are_selective_inhibitors_of_the_cancer_associated_carbonic_anhydrase_isoforms_IX_and_XII_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(11)00814-6 DB - PRIME DP - Unbound Medicine ER -