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.
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MeSH
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 -