刘格歌,陈旺.化学通报,2022,85(11):1346-1351.
抗肿瘤甾体药物依西美坦的合成进展
Progress in the synthesis of Exemestane
投稿时间:2022-03-15  修订日期:2022-04-15
DOI:
中文关键词:  依西美坦  6-亚甲基雄甾-1,4-二烯-3,17-二酮  芳香化酶抑制剂  合成
英文关键词:exemestane  6-methylenandrosta-1,4-diene-3,17-dione  aromatase inhibitors  synthesis
基金项目:陕西省科技厅项目
作者单位E-mail
刘格歌 陕西理工大学生物科学与工程学院 2432896540@qq.com 
陈旺 陕西理工大学生物科学与工程学院 chenwang0519@126.com 
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中文摘要:
      高复发性和高死亡率的乳腺癌是女性中最常见的恶性肿瘤,对其预防和治疗已成为当前全球公共卫生领域的一大研究热点。依西美坦是一种不可逆的甾体芳香化酶失活剂,主要用于雌激素拮抗剂治疗失败的绝经后晚期乳腺癌患者,可显著抑制芳香化酶和血浆雌激素水平且无雌激素抑制剂常见的副作用。本文总结了依西美坦的合成方法,对其活性和研究现状进行了综述,希望对其合成优化和应用具有参考意义。
英文摘要:
      Recurrent and high mortality breast cancer is the most common malignant tumor among women, and its prevention and treatment has become a major research in the field of global public health. Exemestane is an irreversible steroid aromatase inactivator, which is mainly used for postmenopausal women with advanced breast cancer who have failed to be treated by estrogen antagonists. It can significantly inhibit aromatase and plasma estrogen levels without the common side effects of estrogen inhibitors. In this paper, the research status of its activity and synthesis methods are summarized, hoping to provide reference for its synthesis optimization and application.
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