| 第 48 卷第 5 期 |  | Vol. 48 No. 5 | | 2018 年 10 月 | Oct 2018 |
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所屬欄目：醫藥及中間體
17-芳基取代去氫表雄酮的合成及其體外抗腫瘤活性研究 |
| 楊 俊，聶昌平，丁麗娜，陳東林，萬(wàn)路平，梁光平*
（遵義醫藥高等專(zhuān)科學(xué)校，貴州 遵義 563000） |
| 摘 要：以去氫表雄酮為起始原料，經(jīng)乙�；�、酯化、Suzuki反應，水解反應，還原反應得到9種去氫表雄酮衍生物（C-1～C-3，D-1～D-3，E-1～E-3），收率 61%～95%，其結構經(jīng)1H NMR、13C NMR和ESI-MS表征與確證，利用MTT法研究了所合成的化合物對人前列腺癌細胞DU-145的體外抑制活性，結果表明C-1～C-3和D-1～D-3對DU-145均有一定抑制活性，其中D-1和D-3對DU-145具有較好的抑制活性。 |
| 關(guān)鍵詞：去氫表雄酮；衍生物；體外抗腫瘤活性 |
| 中圖分類(lèi)號：R979.1 文獻標識碼：A 文章編號：1009-9212（2018）05-0017-05 |
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| Synthesis and Antitumor Activities of 17-Aryl Substituted Dehyd Roepiandrosterone |
| YANG Jun, NIE Chang-ping, DING Li-na, CHEN Dong-lin, WAN Lu-ping, LIANG Guang-ping*
(Zunyi Medical and Pharmaceutical College, Zunyi 563006, China) |
| Abstract：Nine dehydroepiandrosterone derivatives were synthesized using dehydroepiandrosterone as the starting material through a series of reactions including acetylation, esterification, suzuki reaction, hydrolysis and reduction. The yields for the derivatives were in the range between 61% and 95%. The structures were characterized by 1H NMR，13C NMR and ESI-MS．The in vitro antitumor activities of dehydroepiandrosterone derivatives against human prostate cancer cells(DU-145) were investigated using MTT method. The results showed that D-1, D-3 exhibited well inhibition activities against DU-145. |
| Key words：dehydroepiandrosterone; derivatives; in vitro antitumor activity |
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基金項目：遵義市科技計劃課題（遵市科合社字［2018］46號、［2018］37號）。
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作者簡(jiǎn)介： 楊 �。�1992-）男，貴州遵義人，碩士，主要從事天然活性物質(zhì)的全合成及結構修飾的研究（E-mail：420625539@ qq.com）。
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聯(lián) 系 人： 梁光平，副教授，博士，主要從事中藥及民族藥的開(kāi)發(fā)利用。
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收稿日期：2018-10-06
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