Selective inhibition of tumor-associated carbonic anhydrase (CA; EC 188.8.131.52) 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 (Ki= 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.
|Titolo:||Potent and selective carboxylic acid inhibitors of tumor-associated carbonic anhydrases IX and XII|
DREASSI, ELENA (Corresponding)
|Appare nelle tipologie:||1.1 Articolo in rivista|
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