Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents

• Synthesis of few novel Ospemifene analogs.
• Evaluation as anti-breast cancer agents.
• Few of the synthesized compounds showed anti-breast cancer activities better than Ospemifene and Tamoxifen.
• The experimental results are supported by docking against ERα and ERβ.

The synthesis of some novel Ospemifene derived analogs and their evaluation as anti-breast cancer agents against MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) human breast cancer cell lines are described. Few of these analogs for instance, compounds 6, 7 and 8 are shown to be more effective than recent Selective Estrogen Receptor Modulators (SERMs) i.e. Ospemifene and Tamoxifen, against these cell lines. Compound 8 was relatively more cytotoxic to MCF-7 cells similar to Ospemifene and Tamoxifen, while most potent compounds 6 and 7 were equally effective in inhibiting growth of both ER-positive and ER-negative cell lines. The observed activity profiles were further supported by the docking studies performed against estrogen receptors (ERα and ERβ). Compounds 6, 7 and 8 exhibited stronger binding affinities with both ERα and ERβ compared to Ospemifene and Tamoxifen.

The synthesis and anti-breast cancer activities, supported by docking studies, of few novel Ospemifene analogs is described.Figure optionsDownload as PowerPoint slide