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 E 2 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.