抗肿瘤甾体药物依西美坦的合成进展  

Progress in the Synthesis of Exemestane

作　　者：刘格歌 陈旺 Liu Gege;Chen Wang(School of Biological Science and Engineering,Shaanxi University of Technology;Qinba State Key Laboratory of Biological Resources and Ecological Environment,Hanzhong,723000)

机构地区：[1]陕西理工大学生物科学与工程学院 [2]陕西理工大学秦巴生物资源与生态环境省部共建国家重点实验室(培育),汉中723000

出　　处：《化学通报》2022年第11期1346-1351,共6页Chemistry

基　　金：陕西省科技厅项目(2022JM-576,2022SF-406)资助。

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,希望对其合成路线优化具有参考意义。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.

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 

分 类 号：TQ460.1[化学工程—制药化工]