European Journal of Medicinal Chemistry p. 521 - 530 (2017)
Update date:2022-08-31
Topics:
Eldehna, Wagdy M.
Al-Ansary, Ghada H.
Bua, Silvia
Nocentini, Alessio
Gratteri, Paola
Altoukhy, Ayman
Ghabbour, Hazem
Ahmed, Hanaa Y.
Supuran, Claudiu T.
Herein we present the design, synthesis, and biological evaluation of three different series of novel sulfonamides (3a-f, 6a-f and 9a-f) incorporating substituted indolin-2-one moieties (as tails) linked to benzenesulfonamide (as zinc anchoring moieties) through aminoethyl or (4-oxothiazolidin-2-ylidene)aminoethyl linkers. The synthesized sulfonamides were evaluated in?vitro for their inhibitory activity against the following human (h) carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, hCA I, II, IV and VII. All these isoforms were inhibited by the sulfonamides reported here in variable degrees. hCA I was inhibited with KIs in the range of 42–8550.9?nM, hCA II in the range of 5.9–761?nM; hCA IV in the range of 4.0–2069.5?nM, whereas hCA VII in the range of 13.2–694?nM. Molecular docking studies were carried out for some of the tested compounds within the hCA II active site, allowed us to rationalize the obtained inhibition results.
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