Carbamate Prodrug Concept for Hydroxamate HDAC Inhibitors | Zendy

Schlimme Sonja | Zendy; Hauser AlexanderThomas | Zendy; Carafa Vincenzo | Zendy; Heinke Ralf | Zendy; Kannan Srinivasaraghavan | Zendy; Stolfa Diana A. | Zendy; Cellamare Saverio | Zendy; Carotti Angelo | Zendy; Altucci Lucia | Zendy; Jung Manfred | Zendy; Sippl Wolfgang | Zendy

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Carbamate Prodrug Concept for Hydroxamate HDAC Inhibitors

Author(s) -

Schlimme Sonja,

Hauser AlexanderThomas,

Carafa Vincenzo,

Heinke Ralf,

Kannan Srinivasaraghavan,

Stolfa Diana A.,

Cellamare Saverio,

Carotti Angelo,

Altucci Lucia,

Jung Manfred,

Sippl Wolfgang

Publication year - 2011

Publication title -

chemmedchem

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.817

H-Index - 100

eISSN - 1860-7187

pISSN - 1860-7179

DOI - 10.1002/cmdc.201100007

Subject(s) - prodrug , carbamate , hydroxamic acid , hdac6 , chemistry , selectivity , biochemistry , combinatorial chemistry , stereochemistry , pharmacology , histone deacetylase , biology , catalysis , histone , gene

Virtual screening efforts have identified several novel HDAC6 inhibitors with cellular isoform selectivity. In particular, a carbamate‐protected hydroxamic acid exhibited improved effects with respect to protein hyperacetylation compared with the parent hydroxamate, possibly because of improved cell permeability. The carbamate structure therefore represents a potential prodrug concept for hydroxamic acid‐containing HDAC inhibitors.

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