Abstract
A series of estrone derivatives,
⁻
, were synthesized from the corresponding arylidine estrone,
,
, as starting materials, which were prepared by condensation of estrone (3-hydroxy-estran-17-one, 1) with 4-bromobenzaldehyde and thiophene-2-aldehyde. Treating of
,
with hydrazine derivatives in acetic acid or propionic acid afforded pyrazoline derivatives,
⁻
and
⁻
, respectively. Furthermore, results proved the superiority of thienyl derivatives over 4-bromophenol derivatives in terms of cytotoxic effects on MCF-7 cancer cells. In vivo xenograft breast cancer animal model experiments revealed that the synthesized derivatives can be used for decreasing tumor volume, while the most potent derivative (
) decreased the development of tumor volume by about 87.0% after 12 days.