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Synthesis and anticancer activity studies of novel 1-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)uracil and (6′-substituted)-7- or 9-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-7H- or 9H-purines |
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| Authors: | Marí a C. Nú ñ ez,Mó nica Dí az-Gavilá n,José A. Gó mez-Vidal,Antonia Ará nega,Antonio Espinosa |
| Affiliation: | a Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Universidad de Granada, c/ Campus de Cartuja s/n, 18071 Granada, Spain b Departamento de Ciencias de la Salud, Facultad de Ciencias Experimentales y de la Salud, Paraje de las Lagunillas s/n, 23071 Jaén, Spain c Departamento de Ciencias Morfológicas, Facultad de Medicina, Avenida de Madrid s/n, 18071 Granada, Spain |
| Abstract: | On the basis of a molecular variation on an isosteric replacement (F→H) from the prototype (RS)-1-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-5-fluorouracil, the derivative (RS)-1-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)uracil 4 was prepared. Later on, the pyrimidine base was substituted by the purine moiety with the objective of increasing both the lipophilicity and the structural diversity of the target molecules. The 6′-halogen substituent of the (RS)-9- or 7-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-9H- or 7H-purines shows an interesting reactivity, which is presented and discussed. The anticarcinogenic potential of the target molecules is reported against the MCF-7 cancer cell line. |
| Keywords: | Amination Antitumour compounds Benzodioxepins Suzuki reaction Trifluoromethylation reaction |
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