A study on the activity of selenocarbamates as a novel chemotype acting as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors is reported. Undergoing CA-mediated hydrolysis, selenocarbamates release selenolates behaving as zinc binding groups and effectively inhibiting CAs. A series of selenocarbamates characterised by high molecular diversity and complexity have been studied against different human CA isoforms such as hCA I, II, IX and XII. Selenocarbamates behave as masked selenols with potential biological applications as prodrugs for CAs inhibition-based strategies. X-ray studies provided insights into the binding mode of this novel class of CA inhibitors.
Selenocarbamates As a Prodrug-Based Approach to Carbonic Anhydrase Inhibition / Angeli A.; Ferraroni M.; Capperucci A.; Tanini D.; Costantino G.; Supuran C.T.. - In: CHEMMEDCHEM. - ISSN 1860-7179. - ELETTRONICO. - 17:(2022), pp. e202200085.e2022000085-e202200085.0. [10.1002/cmdc.202200085]
Selenocarbamates As a Prodrug-Based Approach to Carbonic Anhydrase Inhibition
Angeli A.;Ferraroni M.;Capperucci A.;Tanini D.
;Supuran C. T.
2022
Abstract
A study on the activity of selenocarbamates as a novel chemotype acting as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors is reported. Undergoing CA-mediated hydrolysis, selenocarbamates release selenolates behaving as zinc binding groups and effectively inhibiting CAs. A series of selenocarbamates characterised by high molecular diversity and complexity have been studied against different human CA isoforms such as hCA I, II, IX and XII. Selenocarbamates behave as masked selenols with potential biological applications as prodrugs for CAs inhibition-based strategies. X-ray studies provided insights into the binding mode of this novel class of CA inhibitors.File | Dimensione | Formato | |
---|---|---|---|
ChemMedChem - 2022 - Angeli - Selenocarbamates As a Prodrug‐Based Approach to Carbonic Anhydrase Inhibition.pdf
accesso aperto
Tipologia:
Pdf editoriale (Version of record)
Licenza:
Open Access
Dimensione
1.48 MB
Formato
Adobe PDF
|
1.48 MB | Adobe PDF |
I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.