{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T04:57:40Z","timestamp":1787029060878,"version":"build-2736575974"},"reference-count":44,"publisher":"MDPI AG","issue":"19","license":[{"start":{"date-parts":[[2019,10,4]],"date-time":"2019-10-04T00:00:00Z","timestamp":1570147200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the fundamental reaction of CO2 hydration in all living organisms and are actively involved in the regulation of a plethora of pathological and physiological conditions. A set of new coumarin\/ dihydrocoumarin derivatives was here synthesized, characterized, and tested as human CA inhibitors. Their inhibitory activity was evaluated against the cytosolic human isoforms hCA I and II and the transmembrane hCA IX and hCA XII. Two compounds showed potent inhibitory activity against hCA IX, being more active or equipotent with the reference drug acetazolamide. Computational procedures were used to investigate the binding mode of this class of compounds within the active site of hCA IX and XII that are validated as anti-tumor targets.<\/jats:p>","DOI":"10.3390\/molecules24193580","type":"journal-article","created":{"date-parts":[[2019,10,4]],"date-time":"2019-10-04T10:54:58Z","timestamp":1570186498000},"page":"3580","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Extending the Inhibition Profiles of Coumarin-Based Compounds Against Human Carbonic Anhydrases: Synthesis, Biological, and In Silico Evaluation"],"prefix":"10.3390","volume":"24","author":[{"given":"Victor","family":"Kartsev","sequence":"first","affiliation":[{"name":"InterBioscreen, 119019 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Athina","family":"Geronikaki","sequence":"additional","affiliation":[{"name":"School of Health, Department of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0107-2682","authenticated-orcid":false,"given":"Silvia","family":"Bua","sequence":"additional","affiliation":[{"name":"Dipartimento Neurofarba, Sezione Di Scienze Farmaceutiche e Nutraceutiche, Universita\u2019 Degli Studi Di Firenze, Sesto Fiorentino, 50019 Florence, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3342-702X","authenticated-orcid":false,"given":"Alessio","family":"Nocentini","sequence":"additional","affiliation":[{"name":"Dipartimento Neurofarba, Sezione Di Scienze Farmaceutiche e Nutraceutiche, Universita\u2019 Degli Studi Di Firenze, Sesto Fiorentino, 50019 Florence, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8587-2710","authenticated-orcid":false,"given":"Anthi","family":"Petrou","sequence":"additional","affiliation":[{"name":"School of Health, Department of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9615-4519","authenticated-orcid":false,"given":"Boris","family":"Lichitsky","sequence":"additional","affiliation":[{"name":"Zelinsky Institute of Organic Chemistry, Leninsky prospect, 119991 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3133-601X","authenticated-orcid":false,"given":"Mykhaylo","family":"Frasinyuk","sequence":"additional","affiliation":[{"name":"Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Science of Ukraine, 02094 Kiev, Ukraine"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Janis","family":"Leitans","sequence":"additional","affiliation":[{"name":"Latvian Biomedical Research and Study Center, Ratsupites 1, Riga LV-1067, Latvia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Andris","family":"Kazaks","sequence":"additional","affiliation":[{"name":"Latvian Biomedical Research and Study Center, Ratsupites 1, Riga LV-1067, Latvia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kaspars","family":"Tars","sequence":"additional","affiliation":[{"name":"Latvian Biomedical Research and Study Center, Ratsupites 1, Riga LV-1067, Latvia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4262-0323","authenticated-orcid":false,"given":"Claudiu T.","family":"Supuran","sequence":"additional","affiliation":[{"name":"Dipartimento Neurofarba, Sezione Di Scienze Farmaceutiche e Nutraceutiche, Universita\u2019 Degli Studi Di Firenze, Sesto Fiorentino, 50019 Florence, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2019,10,4]]},"reference":[{"key":"ref_1","first-page":"236","article-title":"Coumarin: Chemical and Pharmacological Profile","volume":"2","author":"Jain","year":"2012","journal-title":"J. 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