아쉬라프 카림 Kim Hyun Ji Nocentini, Alessio Seo, Seon Hee Eldehna, Wagdy M. Bang, Eun-Kyoung Supuran, Claudiu T. Keum, Gyochang 2024-01-12T02:32:18Z 2024-01-12T02:32:18Z 2023-02-18 2023-02 1475-6366 https://pubs.kist.re.kr/handle/201004/75806 A series of 6-ureido/amidocoumarins (5a？p and 7a？c) has been designed and synthesised to develop potent and isoform- selective carbonic anhydrase hCA XI and XII inhibitors. All coumarin derivatives were investigated for their CA inhibitory effect against hCA I, II, IX, and XII. Interestingly, target coumarins potently inhibited both tumour-related isoforms hCA IX (KIs: 14.7？82.4？nM) and hCA XII (KIs: 5.9？95.1？nM), whereas the cytosolic off-target hCA I and II isoforms have not inhibited by all tested coumarins up to 100？μM. These findings granted the target coumarins an excellent selectivity profile towards both hCA IX and hCA XII isoforms, supporting their development as promising anticancer candidates. Moreover, all target molecules were evaluated for their anticancer activities against HCT-116 and MCF-7 cancer cells. The 3,5-bis-trifluoromethylphenyl ureidocoumarin 5i, exerted the best anticancer activity. Overall, ureidocoumarins, particularly compound 5i, could serve as a promising prototype for the development of potent anticancer CAIs. English Taylor & Francis Discovery of new 6-ureido/amidocoumarins as highly potent and selective inhibitors for the tumour-relevant carbonic anhydrases IX and XII Article 10.1080/14756366.2022.2154603 1 Journal of Enzyme Inhibition and Medicinal Chemistry, v.38, no.1 Journal of Enzyme Inhibition and Medicinal Chemistry 38 1 Y scie scopus 000924325900001 Biochemistry & Molecular Biology Chemistry, Medicinal Biochemistry & Molecular Biology Pharmacology & Pharmacy Article DESIGN COUMARINS UREIDO SULFONAMIDES HYBRIDS Ureidocoumarins carbonic anhydrase IX carbonic anhydrase XII SLC-0111 anticancer activity