Synthesis and antiproliferative activity of 7-substituted amide estradiol derivatives

The modification of the 7-position in the estradiol structure has drawn significant attention from pharmacologists. In this paper, we synthesize various amine derivatives of estradiol, functionalized with a side chain at the 7-position. The anti-tumor activities of target compounds were evaluated using MTT assay. As the side chain is alkyl amides or halogen atoms substituted alkyl amine, the compounds exhibit excellent activity, with short chains being more active than long chains. Additionally, we studied the antitumor mechanism of the 7-substituted estradiol amide compounds. Compounds 9o can effectively inhibit the proliferation and migration of MCF-7 cells and induce early apoptosis in breast cancer tumors under certain concentration conditions.