RESUMEN

We synthesized 9alpha-fluoromedroxyprogesterone acetate (FMPA) in order to test whether it is a more potent anti-angiogenic agent than medroxyprogesterone acetate (MPA), which has been widely used as a therapeutic agent for breast and endometrium cancers. FMPA was previously synthesized in 10 steps (total yield: 1%). An efficient synthesis of FMPA has been achieved in 6 steps (total yield: 12%). We examined the anti-tumor effect of FMPA, complexed with dimethyl-beta-cyclodextrin (DM-beta-CyD), on rat mammary carcinomas induced by 7,12-dimethylbenz[a]anthracene (DMBA). FMPA showed great anti-tumor effect on DMBA-induced rat mammary carcinomas.

Asunto(s)

Antineoplásicos/síntesis química , Carcinoma/tratamiento farmacológico , Flúor/química , Neoplasias Mamarias Experimentales/tratamiento farmacológico , Acetato de Medroxiprogesterona/análogos & derivados , Administración Oral , Animales , Antineoplásicos/administración & dosificación , Antineoplásicos/química , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Acetato de Medroxiprogesterona/administración & dosificación , Acetato de Medroxiprogesterona/síntesis química , Acetato de Medroxiprogesterona/química , Conformación Molecular , Ratas , Ratas Sprague-Dawley , Estereoisomerismo