ESTRONE DERIVATIVE AND PROCESS FOR PRODUCING THE SAME

摘要

Estrone derivatives (I) are new. Estrone derivatives of formula (I) and their stereoisomers, hydrates, salts or ester are new. [Image] X 1, X 2H or (CH 2) mCH(COOH)(CH 2) nR 1; R 11-7C haloalkyl; R aOH; and R b2-5C alkynyl; or CR aR b= CO; m : 2-14; n : 2-7; and provided that X 1and X 2are not both H. ACTIVITY : Cytostatic; Osteopathic. In tests using ICR mice, administration of 10-(3-hydroxy-17-oxo-estra-1,3,5 (10)-trien-11beta -yl)-2-(4,4,5,5,6,6,7,7,7-nonafluoroheptyl)decanoic acid (Ia) at 10 mg/kg orally for 3 days inhibited 99% of estrogen activity. MECHANISM OF ACTION : Aromatase-Inhibitor; Anti-Estrogen.