Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII |
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| Institution: | 1. Department of Chemistry, Allama Iqbal Open University, Islamabad 44000, Pakistan;2. Department of Transdisciplinary Studies, Graduate School of Convergence Science and Technology, Seoul National University, Seoul 08826, South Korea;3. School of Chemistry and Materials Engineering, Huizhou University, Huizhou, Guangdong 516007, China;4. Food and Feed Immunology Group, Laboratory of Animal Food Function, Graduate School of Agricultural Science, Tohoku University, Sendai 980-8572, Japan;5. Department of Chemistry, School of Natural Sciences (SNS), National University of Science and Technology (NUST), H-12, Islamabad 46000, Pakistan;6. Department of Physiology, University of Sindh, Jamshoro, Pakistan;7. Institute of molecular biology and biotechnology, The University of Lahore, Lahore, Pakistan;8. Department of Chemistry, Balochistan University of Information Technology, Engineering and Management Sciences, Quetta, Pakistan;9. Department of Chemistry Division of Science and Technology, University of Education Lahore, Pakistan |
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| Abstract: | Four novel scaffolds consisting of total 24 compounds (1a–1o, 2a–2c, 3a–3c and 4a–4c) bearing aromatic sulfonamide and coumarin moieties connected through various linkers were synthesized in order to synergize the inhibition potential of both the moieties against four selected human carbonic anhydrase isoforms (hCA I, II, IX & XII). All compounds were found to be potent inhibitors of tumor associated hCA IX & XII while at the same time required large amounts to inhibit off-targeted housekeeping hCA I & II. Selectivity was more pronounced against hCA II over I, and hCA XII over IX. Results were compared with antitumor drug acetazolamide. One derivative 2b of series 2 was found to be a better selective inhibitor of hCA IX and XII. |
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| Keywords: | Sulfonamide Coumarin Human carbonic anhydrase isoforms I II IX XII Acetazolamide Synergistic inhibition |
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