STRUCTURE-ACTIVITY RELATION OF STEROIDAL AMINE TERATOGENS

摘要: I. ABSTRACT Derivatives of jervine and 11-deoxojervine were tested for teratogenic activity in the hamster. Interpretation results is based on structure-activity correlation. Testing derivatives altered steroid ring suggests that these compounds act as hormone blocking agents. muldamines a rigid side chain portion may not be required potency. The substituent effects N-substituted jervines were, order decreasing activity, CHO ≃ H CH3 > n-Bu Ac (CH3)2I-. This indicates an imino function was substantial teratogenicity, negative center such amide carbonyl similar to amino group teratogens. Two having (22S, 25R)-solanidanine configuration about similarly active jervine. Compounds 25S) (22R, configurations produced increases resorption without significant incidence malformations. conformation nitrogen used explain differences activity. Findings support hypothesis highly present negatively charged accessible α face.