Potent And Selective Carboxylic Acid Inhibitors Of Tumor-Associated Carbonic Anhydrases Ix And Xii
MOLECULES(2018)
Abstract
Selective inhibition of tumor-associated carbonic anhydrase (CA; EC 4.2.1.1) isoforms IX and XII is a crucial prerequisite to develop successful anticancer therapeutics. Herein, we confirmed the efficacy of the 3-nitrobenzoic acid substructure in the design of potent and selective carboxylic acid derivatives as CAs inhibitors. Compound 10 emerged as the most potent inhibitor of the tumor-associated hCA IX and XII (K-i = 16 and 82.1 nM, respectively) with a significant selectivity with respect to the wide spread hCA II. Other 3-nitrobenzoic acid derivatives showed a peculiar CA inhibition profile with a notable potency towards hCA IX.
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Key words
carbonic anhydrase inhibitors (CAIs),carboxylic acid,tumor-associated isoforms,isoform selectivity,molecular modeling
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