3-Methoxy-17-aza-D-homo-1,3,5(10)-estratriene-16,17a-dione 3, 16, 17a-dioxo
-17-aza-D-homo-1,3,5(10)-estratrien-3-yl acetate 12 and a series of related
compounds have been synthesised from 3-methoxy-16-oximino-1,3,5 (10)-estra
trien-17-one 1 and 3-hydroxy-16-oximino-1,3,5 (10)-estratrien-17-one 2, res
pectively. The compounds 3 (DPJ-280), 14 (DPJ-369), 17 (DPJ-370), 18 (DPJ-3
54), 19 (DPJ-320), 21 (DPJ-321), 22 (DPJ-374) and (DPJ-284) have been evalu
ated for their estrogenic/antiestrogenic effects and the compounds 3-7,8,9,
10,12,15,16,18,20,21,23 and 24 have been screened for antineoplastic activi
ty at NCI, Bethesda.