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Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors.
Said MA, Eldehna WM, Nocentini A, Bonardi A, Fahim SH, Bua S, Soliman DH, Abdel-Aziz HA, Gratteri P, Abou-Seri SM, Supuran CT. Said MA, et al. Eur J Med Chem. 2020 Jan 1;185:111843. doi: 10.1016/j.ejmech.2019.111843. Epub 2019 Nov 2. Eur J Med Chem. 2020. PMID: 31718943
The four examined isoforms were inhibited by the prepared sulfonamides (9a-d, 11a-h, 13a-c, 15a,b, 17a,b and 21a-g) in variable degrees with K(I)s ranges: 94.4-4953.5 nM for hCA I, 6.9-837.6 nM for hCA II, 3.3-85.0 nM for hCA XI, and 4.4-105.0 nM for hCA XII. ...
The four examined isoforms were inhibited by the prepared sulfonamides (9a-d, 11a-h, 13a-c, 15a,b, 17a,b and 21a-g) in variable degrees with …
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.
Said MA, Eldehna WM, Nocentini A, Fahim SH, Bonardi A, Elgazar AA, Kryštof V, Soliman DH, Abdel-Aziz HA, Gratteri P, Abou-Seri SM, Supuran CT. Said MA, et al. Eur J Med Chem. 2020 Mar 1;189:112019. doi: 10.1016/j.ejmech.2019.112019. Epub 2020 Jan 2. Eur J Med Chem. 2020. PMID: 31972394
The target tumor-associated isoforms hCA IX and XII were effectively inhibited with K(I)s ranges 6-67.6 and 10.1-88.6 nM, respectively. Furthermore, all compounds were evaluated for their potential CDK2 and 9 inhibitory activities. ...
The target tumor-associated isoforms hCA IX and XII were effectively inhibited with K(I)s ranges 6-67.6 and 10.1-88.6 nM, resp …