RESUMEN
A series of 4'-acylamino modified Δ1,4-pregnadien-21E-benzylidene-3,20-dione derivatives (6a-v) was synthesized from the commercially available progesterone (1). These title compounds were evaluated for their toxicity against brine shrimp (Artemia salina) and cytotoxic activities against two human cancer cell lines (HeLa and MCF-7). The results revealed that compound 6f exhibited promising in vitro cytotoxic activity to the two cancer cell lines and the nature of acylamino functional group in the benzylidene moiety had a significant influence on cytotoxicity.
Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Pregnadienos/síntesis química , Pregnadienos/farmacología , Animales , Antineoplásicos/química , Artemia/efectos de los fármacos , Técnicas de Química Sintética , Células HeLa , Humanos , Células MCF-7 , Pregnadienos/química , Pregnadienos/toxicidadRESUMEN
A toxicological study of 17,21-bis(acetyloxy)-2-bromo-6beta,9-difluoro-11beta-hydroxypregna-1,4-dien-3,20-dione(halopredone acetate; Topicon), a new topical antiinflammatory steroid, administered a laboratory animals, was carried out in order to evaluate the safety of this compound. Halopredone acetate compared favorably with either hydrocortisone acetate or potent synthetic corticoids in acute and subacute toxicity studies in mice and rats. This compound did not induce gastric ulcers in rats after repeated administration and did not have any teratogenic effect in rats and rabbits. Also, repeated daily application for 4 months to the skins of mice from two different strains was well-tolerated.