In Vitro and In Vivo Anti-Breast Cancer Activities of Some Synthesized Pyrazolinyl-estran-17-one Candidates.

A series of estrone derivatives, 2 ⁻ 4 , were synthesized from the corresponding arylidine estrone, 2a , b , 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 2a , b with hydrazine derivatives in acetic acid or propionic acid afforded pyrazoline derivatives, 3a ⁻ f and 4a ⁻ f , 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 ( 4f ) decreased the development of tumor volume by about 87.0% after 12 days.