吕海军,郭佳佳,杨尚金,张金玲,王将瑞.化学通报,2023,86(2):195-198.
抗癌药伐地美生的合成方法研究进展
Progress in Synthesis Methods of Vadimezan
投稿时间:2022-06-20  修订日期:2022-07-07
DOI:
中文关键词:  DMXAA STING激动剂  抗肿瘤活性
英文关键词:Vadimezan  STING agonists  Antitumor activity
基金项目:河北省自然科学基金重点项目(B2020208043)资助
作者单位
吕海军 河北科技大学 
郭佳佳 河北科技大学 
杨尚金* 河北中科金辉药业有限公司 
张金玲 河北科技大学 
王将瑞 河北科技大学 
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中文摘要:
      DMXAA是一种血管阻断剂和DT-黄递酶的竞争性抑制剂,也是第一个被发现的强效小分子鼠源STING激动剂,具有抑制多种实体瘤的生物活性和抗病毒活性,常与其他药物配合用于治疗晚期肺癌和其他肿瘤,如和顺铂、环孢素和紫杉醇等联合应用,具有药效高、副作用少等优点和广阔的市场前景。本文综述了近年来国内外报道的有关DMXAA的合成方法研究进展,并讨论了各方法的优缺点以期对相关化合物的小试合成和工业化生产提供依据。
英文摘要:
      DMXAA is a vascular disrupting agent and a competitive inhibitor of DT-xanthete, the first discovered potent murine STING agonist, which also has antiviral activity along with effect against a variety of solid tumors. Furthermore, It is often used in combination with other drugs such as cisplatin, cyclosporine and paclitaxel to treat advanced lung cancer and other tumors, thus this has the advantages of high efficacy, low side effects and thus broad market prospects. This paper reviews the synthesis methods of DMXAA that reported in recent years, and discusses the advantages and disadvantages of each method in order to provide a foundation for further search and industrial usage.
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