首页> 外文期刊>Journal of Medicinal Chemistry >Antitumor Agents.239.Isolation,Structure Elucidation,Total Synthesis,and Anti-Breast Cancer Activity of Neo-tanshinlactone from Salvia miltiorrhiza
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Antitumor Agents.239.Isolation,Structure Elucidation,Total Synthesis,and Anti-Breast Cancer Activity of Neo-tanshinlactone from Salvia miltiorrhiza

机译:239.丹参中新丹参内酯的分离,结构鉴定,全合成及抗乳腺癌活性

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摘要

Neo-tanshinlactone(1)was isolated and synthesized for the first time and evaluated in vitro against several human cancer cell lines.Compound 1 showed significant inhibition against two ER+ human breast cancer cell lines and was 10-fold more potent and 20-fold more selective as compared to tamoxifen citrate.Compound 1 also potently inhibited an ER-,HER-2 overexpressing breast cancer cell line.Therefore,this novel compound merits further development as an anti-breast cancer drug candidate.
机译:首次分离并合成了新丹参内酯(1),并在体外针对几种人类癌细胞系进行了评估。化合物1对两种ER +人类乳腺癌细胞系具有明显的抑制作用,其效力高10倍,而功效高20倍与柠檬酸他莫昔芬相比,该化合物具有选择性。化合物1还有效抑制ER-,HER-2过表达的乳腺癌细胞系。因此,该新化合物作为抗乳腺癌药物候选者值得进一步开发。

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