2. Academic Validation
  3. Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities

Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities

  • Bioorg Med Chem Lett. 2008 Apr 15;18(8):2530-5. doi: 10.1016/j.bmcl.2008.03.055.
Antonello Mai 1,  Andrea Perrone,  Angela Nebbioso,  Dante Rotili,  Sergio Valente,  Maria Tardugno,  Silvio Massa,  Floriana De Bellis,  Lucia Altucci
Affiliations

Affiliation

  • 1 Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Sapienza Università di Roma, P.le A. Moro 5, 00185 Roma, Italy. antonello.mai@uniroma1.it
PMID: 18381238 DOI: 10.1016/j.bmcl.2008.03.055
Abstract

A novel series of non-hydroxamate HDAC inhibitors (HDACi) showing a uracil group at the left and a 2-aminoanilide/2-aminoanilide-like portion at the right head have been reported. In particular, the new compounds incorporating a 2-aminoanilide moiety behaved as class I-selective HDACi. Compound 8, the most potent and class I-selective, showed weak Apoptosis (higher than MS-275) joined to cytodifferentiating activity on U937 cells. Surprisingly, the highest differentiation was observed with 13, through an effect that seems to be unrelated to HDAC inhibition.

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