English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Plus monthly

Global: Zendy Tools annual

Global: Zendy Tools monthly

Global: Zendy Free Plan

A novel series of 8-substituted coumarin-based compounds, characterized by the presence of alkylpiperazine and arylpiperazine chains, were synthesized and tested for their inhibitory activity against four human carbonic anhydrase ( h CA) isoforms. All compounds displayed nanomolar potency against the cancer-related h CA IX and h CA XII; moreover, they were shown to be devoid of any inhibitory activity toward the cytosolic h CA I and h CA II up to 10 µM concentration in the assay system. Therefore, the synthesized coumarin ligands demonstrated to be potent and selective h CA IX/XII inhibitors, and were shown to be as potent as the reference inhibitor acetazolamide against h CA XII, with single-digit nanomolar K  i values. Molecular modeling studies provided a rationale for explaining the selectivity profile of these non-classic h CA inhibitors and their interactions with the enzymes, according to their specific mechanism of action, thus paving the way for future structure-based lead optimization studies.

Novel 8-Substituted Coumarins That Selectively Inhibit Human Carbonic Anhydrase IX and XII