Design, Synthesis, and Biological Evaluation of PKD Inhibitors

Protein kinase D (PKD) belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to the lack of a PKD-specific inhibitor. The benzoxoloazepinolone CID755673 was recently reported as the first potent and kinase-selective inhibitor for this enzyme. For structure-activity analysis purposes, a series of analogs was prepared and their in vitro inhibitory potency evaluated.

• Publication year

  2011

• Venue

  Pharmaceutics

• Publication date

  2011-04-21

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.3390/pharmaceutics3020186PMID 22267986PMCID 3261798
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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