Christine Batzl

Structure-activity studies and evaluation of mammary tumor inhibiting activity of new aromatase-inhibitors of the aminoglutethimide-type [Poster 17]

Abstract Structural modifications of the mammary tumor-inhibiting aromatase inhibitor aminoglutethimide (AG) were performed. Replacement of the 3-ethyl group by a 3-cyclohexyl substituent resulted in a promising new compound, showing a 123-fold stronger inhibition of aromatase and a markedly decreased inhibition of desmolase. In vivo the cyclohexyl compound was also more active regarding reduction of plasma E2 concentration and tumor area and showed no central nervous system depressive activity. Thus, the new compound might be a better candidate for the treatment of hormone-dependent breast cancer.