N-β-Glycosyl sulfamides are selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Rodriguez, Oscar M.¹  Maresca, Alfonso²  Tempera, Carlos A.¹  Bravo, Rodolfo D.¹  Colinas, Pedro A.¹  Supuran, Claudiu T.² 

[1] Natl Univ La Plata, Fac Ciencias Exactas, Dept Quim, LADECOR, RA-1900 La Plata, Argentina

[2] Univ Florence, Lab Chim Bioinorgan, I-50019 Florence, Italy

关键词: Glycosyl sulfamides;    Carbonic anhydrase;    Targeted therapies;    Cancer;   

DOI  :  10.1016/j.bmcl.2011.06.031

来源: Elsevier

【 摘 要 】

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-beta-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 KIs in the low nanomolar range. (C) 2011 Elsevier Ltd. All rights reserved.

【 授权许可】

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