Design and Synthesis of 2-substituted [1,2,4]Triazolo[1,5-a]pyrimidines Tethered with Umbelliferone as Selective Carbonic Anhydrase IX and XII Inhibitors

In this study, we have identified compound 3d as a selective inhibitor of the isoforms hCA IX and XII, showing minimal inhibition over hCA I, II, and IV isoenzymes (selectivity indices > 100). Its moderate inhibitory effects on hCA IX and XII at submicromolar levels were paralleled by significant antiproliferative activity against HD-MB03 cells. These findings underscore the potential of compound 3d as a promising candidate for further therapeutic development, especially in combination with clinically used chemotherapeutic agents.

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Publication Details

Journal
Anti-Cancer Agents in Medicinal Chemistry
Published
2025-03-28
DOI
https://doi.org/10.2174/0118715206373602250318062414
Primary Topic
Enzyme function and inhibition
Type
article
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article

Design and Synthesis of 2-substituted [1,2,4]Triazolo[1,5-a]pyrimidines Tethered with Umbelliferone as Selective Carbonic Anhydrase IX and XII Inhibitors

Roberta Bortolozzi, Alessio Nocentini, Lorenzo Manfreda, Claudiu T. Supuran et al.
Anti-Cancer Agents in Medicinal Chemistry
Enzyme function and inhibition
article

Design and Synthesis of 2-substituted [1,2,4]Triazolo[1,5-a]pyrimidines Tethered with Umbelliferone as Selective Carbonic Anhydrase IX and XII Inhibitors

Roberta Bortolozzi, Alessio Nocentini, Lorenzo Manfreda, Claudiu T. Supuran, Romeo Romagnoli, Giampietro Viola, Andrea Brancale, Elena Romagnoli, Arianna Zanolli
article en

Abstract

In this study, we have identified compound 3d as a selective inhibitor of the isoforms hCA IX and XII, showing minimal inhibition over hCA I, II, and IV isoenzymes (selectivity indices > 100). Its moderate inhibitory effects on hCA IX and XII at submicromolar levels were paralleled by significant antiproliferative activity against HD-MB03 cells. These findings underscore the potential of compound 3d as a promising candidate for further therapeutic development, especially in combination with clinically used chemotherapeutic agents.

Anti-Cancer Agents in Medicinal ChemistryVol. 25(18)
Marche Polytechnic University (IT), University of Padua (IT), University of Ferrara (IT), Città della Speranza Foundation (IT), University of Florence (IT), University of Chemistry and Technology, Prague (CZ)
Clean water and sanitation
Openalex Percentile: Top 95%
Enzyme function and inhibition
DOISourceOpenAlex
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Design and Synthesis of 2-substituted [1,2,4]Triazolo[1,5-a]pyrimidines Tethered with Umbelliferone as Selective Carbonic Anhydrase IX and XII Inhibitors — Roberta Bortolozzi, Alessio Nocentini, et al. · Anti-Cancer Agents in Medicinal Chemistry (2025) | TGRS Research Map | TGRS