Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors |
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| Institution: | 1. Laboratory of Medicinal and Advanced Synthetic Chemistry (Lab MASC), Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, Perugia I-06123, Italy;2. Laboratory of Bioinorganic Chemistry, University of Florence, Via della Lastruccia 3, Sesto Fiorentino (Firenze) I-50019, Italy;3. Neurofarba Dept., Section of Pharmaceutical and Nutriceutical Sciences, University of Florence, Via U. Schiff 6, Sesto Fiorentino (Firenze) I-50019, Italy;1. School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Maudland Building, Preston, Lancashire PR1 2HE, UK;2. Brain Tumour Research Centre, University of Wolverhampton, Wulfruna Street, Wolverhampton WV1 1LY, UK;1. B. Verkin Institute for Low Temperature Physics and Engineering, 47 Lenin Ave., Kharkov 61103, Ukraine;2. Institute of Physics, 46 Science Ave., Kiev 03680, Ukraine;3. Department of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721, USA;1. Drug Design and Medicinal Chemistry Lab, Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Bioinformatics Infrastructure Facility (BIF), Jamia Hamdard, New Delhi 110062, India;2. School of Biochemistry, DAVV, Khandwa Road, Indore, India |
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| Abstract: | A series of secondary and tertiary aryl sulfonamides were synthesized under flow conditions and evaluated for their ability to selectively inhibit tumor-associated carbonic anhydrase isoforms IX and XII. The tested compounds revealed to be highly potent CA IX inhibitors in nanomolar range, and to inhibit CA XII activity with different ranks of potencies. Remarkably, 4-methyl-N-phenyl-benzenesulfonamide was a selective nanomolar CA IX inhibitor with an IC50 of 90 nM. |
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| Keywords: | Carbonic anhydrases Flow synthesis Sulfonamides Docking |
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