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目的：探寻喜树碱类化合物的构效关系及其与受体的可能作用方式。方法：对近年来喜树碱类化合物的结构修饰、改造及活性的研究结果进行综述。结果：对该类化合物的构效关系及其与酶－ＤＮＡ复合物的可能作用方式有了深入认识。结论：喜树碱类化合物的芳环共轭平面为结构必需，其中α－ＯＨ内酯环（Ｅ环）是发挥作用的关键部位，而对７及９－１１位进行适当取代可望增效降毒。
Objective: To explore the structure-activity relationship of camptothecins and their possible interaction with receptors. Methods: The structural modification, modification and activity of camptothecins in recent years were reviewed. RESULTS: The structure-activity relationship of these compounds and their possible interaction with enzyme-DNA complexes were well understood. CONCLUSION: The aromatic ring conjugation planes of camptothecins are required for structure. Among them, the α-OH lactone ring (E ring) is the key part that plays an important role. However, proper substitution of 7 and 9-11 is expected Poisoning.