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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)benzene-sulphonamides. 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 KI 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. [ABSTRACT FROM AUTHOR]

Sulfated zirconia is a very strong solid acid catalyst which can be utilized for various reactions. The present study focuses on synthesis of zirconia-based catalyst with high acidity and high surface area, particularly for isomerization reaction. Sulfated zirconia has been obtained by sulfation of zirconia prepared by hydrothermal route. The catalyst was developed by impregnating tungstophosphoric acid on sulfated zirconia by wet incipient method. The catalyst was characterized through Brunauer–Emmett–Teller (BET) surface area, temperature-programmed desorption of ammonia, temperature program reduction of hydrogen, Fourier transmission infrared spectroscopy, and thermogravimetric analysis. The results revealed that the catalyst is crystalline in nature with surface area 190–225 m2 g−1 and acidity 0.135–0.558 mmol g−1. Twenty-five percent conversion was obtained (as confirmed by gas chromatography) at 225°C using n-hexane as model hydrocarbon in fixed-bed microreactor. [ABSTRACT FROM AUTHOR]