754199-86-5Relevant academic research and scientific papers
Synthesis method of novel estrogen receptor targeting inhibitor and application of novel estrogen receptor targeting inhibitor in breast cancer treatment
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Paragraph 0398-0401; 0432-0435, (2021/11/26)
The invention provides a synthesis method of a novel estrogen receptor targeting inhibitor and application of the novel estrogen receptor targeting inhibitor in breast cancer treatment, and belongs to the technical field of pharmaceutical chemical application. According to the technical scheme, a series of estrogen receptor targeting inhibitors containing indazole and indole skeletons are synthesized, the inhibitory activity of the inhibitors on breast cancer cells is tested respectively, and a series of compounds with higher cancer cell inhibitory activity than lonidamine are found; wherein the compounds (21) and (23) show the best breast cancer cell inhibition activity, and the IC50 values of the compounds (21) and (23) are 45 mu M and 53 mu M respectively. The synthesis method and applicationhave the beneficial effects that a series of bilonidamine small molecule compounds with higher breast cancer cell inhibitory activity are provided, the compounds (21) and (23) show the strongest biological activity, and molecular docking experimental results prove that the compounds (21) and (23) play a role in inhibiting breast cancer cells through a targeted estrogen receptor.
