Al-Sanea, Mohammad M. Elkamhawy, Ahmed Paik, Sora Bua, Silvia Lee, So Ha Abdelgawad, Mohamed A. Roh, Eun Joo Eldehna, Wagdy M. Supuran, Claudiu T. 2024-01-19T21:02:34Z 2024-01-19T21:02:34Z 2021-09-04 2019-01-01 1475-6366 https://pubs.kist.re.kr/handle/201004/120488 Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes that are involved in diverse bioprocesses. We report the synthesis and biological evaluation of novel series of benzenesulfonamides incorporating un/substituted ethyl quinoline-3-carboxylate moieties. The newly synthesised compounds were in vitro evaluated as inhibitors of the cytosolic human (h) isoforms hCA I and II. Both isoforms hCA I and II were inhibited by the quinolines reported here in variable degrees: hCA I was inhibited with K(I)s in the range of 0.966-9.091 mu M, whereas hCA II in the range of 0.083-3.594 mu M. The primary 7-chloro-6-flouro substituted sulphfonamide derivative 6e (K-I = 0.083 mu M) proved to be the most active quinoline in inhibiting hCA II, whereas, its secondary sulfonamide analog failed to inhibit the hCA II up to 10 mu M, confirming the crucial role of the primary sulphfonamide group, as a zinc-binding group for CA inhibitory activity. English TAYLOR & FRANCIS LTD DRUG DISCOVERY THERAPEUTIC APPLICATIONS SELECTIVE INHIBITORS ISOZYME-II SULFONAMIDES QUINOLINE DERIVATIVES POTENT PATENT VII Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors Article 10.1080/14756366.2019.1652282 1 JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, v.34, no.1, pp.1457 - 1464 JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 34 1 1457 1464 scie scopus 000480723600001 2-s2.0-85071025700 Biochemistry & Molecular Biology Chemistry, Medicinal Biochemistry & Molecular Biology Pharmacology & Pharmacy Article DRUG DISCOVERY THERAPEUTIC APPLICATIONS SELECTIVE INHIBITORS ISOZYME-II SULFONAMIDES QUINOLINE DERIVATIVES POTENT PATENT VII Benzenesulfonamides carbonic anhydrase quinolines synthesis cytosolic isoforms hCA I and II