Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 37, Issue 1, Pages 1454-1463Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2022.2077333
Keywords
Carbonic anhydrase inhibitors; hCA isoforms; benzenesulphonamide; triazole; apoptosis
Funding
- Council of Scientific and Industrial Research, New Delhi, India
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In this study, two subsets of novel benzenesulphonamide compounds were designed and synthesized, which showed good inhibition activity against tumour-associated carbonic anhydrase IX. Some of these compounds also demonstrated interesting potential for inducing apoptosis in vitro.
In search of selective carbonic anhydrase (CA) IX inhibitors endowed with apoptotic inducing properties, we designed and synthesised two subsets of 4- and 3-(5-aryl-(4-phenylsulphonyl)-1H-1,2,3-triazol-1-yl)benzenesulphonamides. All compounds were assayed for human carbonic anhydrase (hCA) isoforms I, II, IV, and IX inhibition. Isoforms hCA I and hCA IV were weakly inhibited by most of the synthesised compounds. Many four-substituted benzenesulphonamides displayed low nanomolar inhibition against isoform hCA II, unlike the three-substituted analogues. All target compounds exhibited good inhibition profile with K-I values ranging from 16.4 to 66.0 nM against tumour-associated isoform hCA IX. Some selective and potent inhibitors of hCA IX were assayed for in vitro apoptotic induction in goat testicular cells. Compounds 10d and 10h showed interesting apoptotic induction potential. The present study may provide insights into a strategy for the design of novel anticancer agents based on hCA inhibitors endowed with apoptotic interference.
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