2. Academic Validation
  3. A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo

A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo

  • J Med Chem. 2008 Apr 24;51(8):2350-3. doi: 10.1021/jm800079s.
Philip Jones 1,  Sergio Altamura,  Raffaele De Francesco,  Odalys Gonzalez Paz,  Olaf Kinzel,  Giuseppe Mesiti,  Edith Monteagudo,  Giovanna Pescatore,  Michael Rowley,  Maria Verdirame,  Christian Steinkühler
Affiliations

Affiliation

  • 1 IRBM/Merck Research Laboratories, Via Pontina km 30,600, 00040 Pomezia, Italy. philip_jones@merck.com
PMID: 18370373 DOI: 10.1021/jm800079s
Abstract

Histone deacetylase (HDAC) inhibitors offer a promising strategy for Cancer therapy, and the first generation HDAC inhibitors are currently in the clinic. Entirely novel ketone HDAC inhibitors have been developed from the cyclic tetrapeptide apicidin. These compounds show class I subtype selectivity and levels of cellular activity comparable to clinical candidates. A representative example has demonstrated tumor growth inhibition in a human colon HCT-116 carcinoma xenograft model comparable to known inhibitors.

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