Targeting tumor associated carbonic anhydrase IX and XII: Highly isozyme selective coumarin and psoralen inhibitors
Melis, Claudia;Distinto, Simona
;Bianco, Giulia;Meleddu, Rita;Cottiglia, Filippo;Fois, Benedetta;Maccioni, Elias
2018-01-01
Abstract
A small library of psoralen carboxylic acids and their corresponding benzenesulfonamide derivatives were designed and synthetized to evaluate their activity and selectivity toward tumor associated human Carbonic Anhydrase (hCA) isoforms IX and XII. Both psoralen acids and sulfonamides exhibited potent inhibition of IX and XII isozymes in the nanomolar concentration range. However, psoralen acids resulted as the most selective in comparison with the corresponding benzenesulfonamide derivatives. Our data indicate that the psoralen scaffold is a promising starting point for the design of highly selective tumor associated hCA inhibitors.File | Size | Format | |
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ACSMedChemLett-Manuscript-Targeting tumor associated carbonic anhydrase IX and XII-accepted.pdf open access
Type: versione pre-print
Size 511.25 kB
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File caricatoACS2018.pdf Solo gestori archivio
Type: versione editoriale
Size 3.22 MB
Format Adobe PDF
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3.22 MB | Adobe PDF | & nbsp; View / Open Request a copy |
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