{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,22]],"date-time":"2026-09-22T17:32:38Z","timestamp":1790098358666,"version":"4.0.1"},"reference-count":47,"publisher":"Wiley","issue":"3","license":[{"start":{"date-parts":[[2023,11,27]],"date-time":"2023-11-27T00:00:00Z","timestamp":1701043200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2024,3]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>\n                    Herein, we report the design and synthesis of a library of 28 new 1,2,3\u2010triazole derivatives bearing carboxylic acid and ester moieties as dual inhibitors of carbonic anhydrase (CA) and cathepsin B enzymes. The synthesised compounds were assayed in vitro for their inhibition potential against four human CA (hCA) isoforms, I, II, IX and XII. The carboxylic acid derivatives displayed low micromolar inhibition against hCA II, IX and XII in contrast to the ester derivatives. Most of the target compounds showed poor inhibition against the hCA I isoform. 4\u2010Fluorophenyl appended carboxylic acid derivative\n                    <jats:bold>6c<\/jats:bold>\n                    was found to be the most potent inhibitor of hCA IX and hCA XII with a\n                    <jats:italic>K<\/jats:italic>\n                    <jats:sub>I<\/jats:sub>\n                    value of 0.7\u2009\u03bcM for both the isoforms. The newly synthesised compounds showed dual inhibition towards CA as well as cathepsin B. The ester derivatives exhibited higher % inhibition at 10\n                    <jats:sup>\u22127<\/jats:sup>\n                    \u2009M concentration as compared with the corresponding carboxylic acid derivatives against cathepsin B. The results from in silico studies of the target compounds with the active site of cathepsin B were found in good correlation with the in vitro results. Moreover, two compounds,\n                    <jats:bold>5i<\/jats:bold>\n                    and\n                    <jats:bold>6c<\/jats:bold>\n                    , showed cytotoxic activity against A549 lung cancer cells, with IC\n                    <jats:sub>50<\/jats:sub>\n                    values lower than 100\u2009\u03bcM.\n                  <\/jats:p>","DOI":"10.1002\/ardp.202300372","type":"journal-article","created":{"date-parts":[[2023,11,27]],"date-time":"2023-11-27T23:15:19Z","timestamp":1701126919000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["1,2,3\u2010Triazole\u2010based esters and carboxylic acids as nonclassical carbonic anhydrase inhibitors capable of cathepsin B inhibition"],"prefix":"10.1002","volume":"357","author":[{"given":"Kiran","family":"Siwach","sequence":"first","affiliation":[{"name":"Department of Chemistry Kurukshetra University  Kurukshetra Haryana 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