| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371625 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Alastair D.G. Donald, 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,