Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 30, Issue 3, Pages 430-434Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2014.942659
Keywords
Amino acid; carbonic anhydrase inhibitor; sulfonamide; tumor-associated CA XII
Funding
- 7th FP EU grant (METOXIA)
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New benzenesulfonamides incorporating water solubilizing moieties were synthesized using N-alpha-acetyl-L-lysine or gamma-aminobutyric acid as scaffolds followed by the conversion of their terminal amino group to the guanidine one. Their inhibition activity was assessed by determining their K(I)s values against the human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I, II, IX and XII. Some of these compounds were medium potency inhibitors of the cytosolic (CA I, II) and transmembrane (CA IX) isoforms and highly effective, nanomolar inhibitors of the second transmembrane isoform hCA XII. Some of these sulfonamides possessing good selectivity inhibition for the tumor-associated CA XII isoform over the cytosolic and physiologically dominant isoforms CA I and II may be used as tools to develop new anticancer agents.
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