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目前,对斑蝥素(cantharidin)和去甲斑蝥素进行结构改造及合成是抗肿瘤药物的研究热点之一。近十年来,有关斑蝥素及其衍生物构效关系的研究,取得较大的进展。人们结合肿瘤病理药理学研究成果对斑蝥素进行合理的结构优化,合成出大量的斑蝥素和去甲斑蝥素衍生物并对其进行活性筛选,其中有少数衍生物具有较强的生理活性,已经投入临床使用。本文探讨了斑蝥素衍生物结构-活性-毒性之间的关系。
At present, structural modification and synthesis of cantharidin and norcantharidin are one of the research hotspots for antitumor drugs. In the past ten years, great progress has been made in studies on the structure-activity relationship of cantharidin and its derivatives. Based on the results of tumor pathology and pharmacology, people can rationalize the structural optimization of cantharidin, synthesize a large number of cantharidin and norcantharidin derivatives and screen them for activity. Among them, a few derivatives have strong physiological activity. Put into clinical use. This article explored the relationship between the structure-activity-toxicity of cantharidin derivatives.