2. Academic Validation
  3. Anticancer activity of (1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl)-pyrimidines and -purines against the MCF-7 cell line: Preliminary cDNA microarray studies

Anticancer activity of (1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl)-pyrimidines and -purines against the MCF-7 cell line: Preliminary cDNA microarray studies

  • Bioorg Med Chem Lett. 2008 Feb 15;18(4):1457-60. doi: 10.1016/j.bmcl.2007.12.070.
Mónica Díaz-Gavilán 1,  José A Gómez-Vidal,  Fernando Rodríguez-Serrano,  Juan A Marchal,  Octavio Caba,  Antonia Aránega,  Miguel A Gallo,  Antonio Espinosa,  Joaquín M Campos
Affiliations

Affiliation

  • 1 Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, c/Campus de Cartuja s/n, 18071 Granada, Spain.
PMID: 18194866 DOI: 10.1016/j.bmcl.2007.12.070
Abstract

Completing a SAR study, a series of (RS)-1- or 3-(1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl)-pyrimidines and (RS)-6-substituted-7- or 9-(1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl)-7H- or 9H-purines have been prepared. Their antiproliferative activities on MCF-7 cells are here presented and discussed. (RS)-6-Chloro-9-[1-(9H-9-fluorenylmethoxycarbonyl)-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl]-9H-purine (28) is the most active (IC(50)=0.67+/-0.18 microM) of the series so far described. cDNA microarray technology reveals potential drug targets, which are mainly centred on Apoptosis regulatory pathway genes.

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