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Abstract
A series of polymethoxylated-pyrazoline benzene sulfonamides were synthesized, investigated for their cytotoxic activities on tumor and non-tumor cell lines and inhibitory effects on carbonic anhydrase isoenzymes (hCA I and hCA II). Although tumor selectivity (TS) of the compounds were less than the reference compounds 5-Fluorouracil and Melphalan, trimethoxy derivatives 4, 5, and 6 were more selective than dimethoxy derivatives 2 and 3 as judged by the cytotoxicity assay with the cells both types originated from the gingival tissue. The compound 6 (4-[3-(4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl] benzene sulfonamide) showed the highest TS values and can be considered as a lead molecule of the series for further investigations. All compounds synthesized showed superior CA inhibitory activity than the reference compound acetazolamide on hCA I, and II isoenzymes, with inhibition constants in the range of 26.5–55.5 nM against hCA I and of 18.9–28.8 nM against hCA II, respectively.
Acknowledgements
The authors thank Dr. Y. Ozkay (Anadolu University, Eskisehir, Turkey) and Dr. M. K. Sukuroglu (Gazi University, Ankara, Turkey) for HRMS analysis.
Declaration of interest
The authors report no conflict of interest and are responsible for the contents and writing of the paper. This study was supported by the Research Foundation of Ataturk University, Turkey. Grant Number: 2015/078 and 2015/322.
Supplementary material available online