RESUMEN
Synthesis of 4-amino-4,6-androstadiene-3,17-dione 7, an analog of formestane used in breast cancer therapy as an aromatase inhibitor, from 4-acetoxy-4-androstene-3,17-dione 2 is described. This is the first report of a 4-amino diene (4,6) system in this series of molecules. The new (7) and reported molecules were screened by the National Cancer Institute (NCI, Bethesda, USA) for in vitro antitumor activity against 60 human cancer cell lines. Molecule 7 showed best activity against breast cancer cell line (MCF-7).
Asunto(s)
Androstadienos/química , Androstenodiona/análogos & derivados , Antineoplásicos/síntesis química , Neoplasias de la Mama/tratamiento farmacológico , Química Farmacéutica/métodos , Androstenodiona/síntesis química , Androstenodiona/química , Androstenodiona/farmacología , Antineoplásicos/farmacología , Aromatasa/metabolismo , Línea Celular Tumoral , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Modelos QuímicosRESUMEN
8-Iodo-11-(4-methylpiperazino)-5H-dibenzo[b,e][1,4]-diazepine: Iozapine, a potential D(4)-receptor ligand was synthesized using oxidative iodo-destannylation reaction. The preliminary biodistribution studies of radioiodinated iozapine have shown that the compound is taken up in the brains of mice and rabbits.