2. Academic Validation
  3. Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases

Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases

  • Bioorg Med Chem Lett. 2010 Nov 15;20(22):6657-60. doi: 10.1016/j.bmcl.2010.09.016.
Alastair D G Donald 1,  Vanessa L Clark,  Sanjay Patel,  Francesca A Day,  Martin G Rowlands,  Judata Wibata,  Lindsay Stimson,  Anthea Hardcastle,  Sue A Eccles,  Deborah McNamara,  Lindsey A Needham,  Florence I Raynaud,  Wynne Aherne,  David F Moffat
Affiliations

Affiliation

  • 1 Chroma Therapeutics, 93 Milton Park, Abingdon, Oxfordshire OX14 4RY, UK. adonald@chromatherapeutics.com
PMID: 20884208 DOI: 10.1016/j.bmcl.2010.09.016
Abstract

Inhibition of histone deacetylase activity represents a promising new modality in the treatment of a number of cancers. A novel HDAC series demonstrating inhibitory activity in cell proliferation assays is described. Optimisation based on the introduction of basic amine linkers to effect good drug distribution to tumour led to the identification of a compound with oral activity in a human colon Cancer xenograft study associated with increased histone H3 acetylation in tumour tissue.

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