Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates.

Roberto Scatena, Patrizia Bottoni, Antonello Mai, Silvio Massa, Dante Rotili, Riccardo Pezzi, Joachim Meraner, Gerald Brosch

Risultato della ricerca: Contributo in rivistaArticolo in rivista

39 Citazioni (Scopus)

Abstract

Starting from the pharmacophore model for HDAC inhibitor design, a novel series of hydroxamates bearing a uracil moiety as connecting unit (CU) has been prepared and tested. Almost all compounds exhibited HDAC inhibiting activity at low nanomolar concentrations, the N-hydroxy-6-(3,4-dihydro-4-oxo-6-benzyl- and -6-phenyl-2-pyrimidinylthio)hexanamides 1d and 1l being more potent than SAHA in enzymatic assays. Such compounds also caused hyperacetylation in NIH3T3 cell core histones and were endowed with interesting antiproliferative and cytodifferentiating effects in human leukemia (HL-60) cells.
Lingua originaleEnglish
pagine (da-a)4656-4661
Numero di pagine6
RivistaBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Stato di pubblicazionePubblicato - 2005

Keywords

  • cancer
  • cell differentiation
  • drug

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