薯蓣皂苷元异羟肟酸及季鏻盐衍生物的合成与抗肿瘤活性
Synthesis and Antitumor Activity of Diosgenin Hydroxamic Acid and Quaternary Phosphonium Salt Derivatives.
作者信息
Wang Lin, Yao Maoling, Hu Yuegao, Chen Congdi, Jin Liming, Ma Xiaodong, Yang Hongjun
机构信息
Key Laboratory of General Chemistry of the National Ethnic Affairs Commission, School of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, China.
College of Chemistry and Life Science, Chengdu Normal University, Chengdu 611130, China.
出版信息
ACS Med Chem Lett. 2022 Apr 19;13(5):786-791. doi: 10.1021/acsmedchemlett.1c00581. eCollection 2022 May 12.
Diosgenin, a component separated from Dioscorea plants, is an important starting material for steroid hormone drugs and semisynthetic steroids. In the work, two series of diosgenin derivatives were designed, synthesized, and evaluated for their cellular anticancer activities. Most of the target compounds exhibited good inhibitory activities against four cell lines, Aspc-1 (human colon adenocarcinoma cells), H358 (human nonsmall cell lung cancer cells), HCT116 (human colorectal adenocarcinoma cells), and SW620 (human metastatic pancreatic cancer cells). Among them, the representative compound exhibited 7.9-341.7-fold antiproliferative activities against the above-mentioned four cell lines compared with the lead compound diosgenin.
薯蓣皂苷元是从薯蓣属植物中分离出的一种成分，是甾体激素药物和半合成甾体的重要起始原料。在这项工作中，设计、合成了两个系列的薯蓣皂苷元衍生物，并对其细胞抗癌活性进行了评估。大多数目标化合物对四种细胞系，即Aspc-1（人结肠腺癌细胞）、H358（人非小细胞肺癌细胞）、HCT116（人结肠直肠腺癌细胞）和SW620（人转移性胰腺癌细胞）表现出良好的抑制活性。其中，代表性化合物对上述四种细胞系的抗增殖活性比先导化合物薯蓣皂苷元高7.9至341.7倍。
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