| 白洁,金文聪,杨振乾,等.雄激素受体N末端结构域抑制剂的设计、合成与活性评价[J].中国海洋药物,2023,42(5):34-40. |
| 雄激素受体N末端结构域抑制剂的设计、合成与活性评价 |
| Design, synthesis and evaluation of the activity of androgen receptor N-terminal domain inhibitors |
| 投稿时间：2022-05-10 修订日期：2022-09-28 |
| DOI：10.13400/j.cnki.cjmd.2023.05.007 |
| 中文关键词: 雄激素受体、EPI-002、AR-V7、抗肿瘤细胞增殖活性 |
| English Keywords:androgen receptor EPI-002 AR-V7 Antitumor cell proliferation activity |
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| 中文摘要: |
| 目的 以EPI-002为先导化合物,通过结构修饰设计合成其衍生物并进行活性评价。方法 以双酚A为起始原料,通过取代、Lewis酸催化开环等反应合成EPI-002衍生物,并对其进行抗肿瘤细胞增殖以及免疫印迹测试。结果 合成共计6个EPI-002衍生物a-e,抗肿瘤细胞活性均优于EPI-002与恩杂鲁胺,同时免疫印迹实验显示出化合物b与c能够下调AR-FL、AR-V7以及AR下游基因FKBP51与TMPRSS2的表达。 |
| English Summary: |
| Objective A series of androgen receptor N-terminal domain antagonist were designed and synthesized with EPI-002 as the lead compound, and their activities were evaluated. Methods EPI-002 derivatives were synthesized by substitution, Lewis acid catalyzed ring opening, and their anti-tumor cell proliferation and immunoblotting were tested. Results EPI-002 derivatives a-e were synthesized, which showed better anti-tumor activity than EPI -002 and enzalutamide. Western blot showed that b and c could down regulate the expression of AR-FL, AR-V7 and AR downstream gene FKBP51 and TMPRSS2. |
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