C,O-Nitration of 17beta-Acetoxy-17alpha-ethynylestra-1,3,5(10)-triene-3,11alpha-diol

摘要

A combination of antiestrogenic and cytostatic properties in a single molecule could give rise to anti-tumor compounds which are especially effective in the treatment of breast cancer [1].We previously described [2,3] the synthesis of 11alpha-nitroxy-17alpha-ethynylestra-diol 3,17-diacetate;the corresponding phenol exhibits antiestrogenic activity [4].The present work was aimed at synthesizing 2-and 4-nitro derivatives of that phenol,i.e.,compounds II and IV,respectively.It is known that introduction of a nitro group into aromatic ring makes estrogen cytotoxic [5].