Abstract

In this paper, a series of novel derivatives of camptothecin substituted norcantharimide was designed by mimic strategy. These compounds were synthesized in moderate yields by directly coupling CPT with N-amino acid norcantharimides. Their cytotoxicity to four human tumour cell lines (HepG2, BGC-803, SW480 and PANC-1) and normal human cell lines L-O2 and HIEC was evaluated. The synthesized CPT substituted norcantharimide analogs (3g and 3f) showed better anti-hepatocarcinoma activity than CPT. Compounds 3d, 3e, 3g, 3h and 3i also showed strong inhibition activity against BGC803.

中文翻译：

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喜树碱取代去甲斑蝥酰亚胺衍生物的合成及生物学评价

摘要

本文采用拟态策略设计了一系列喜树碱取代去甲斑蝥酰亚胺的新型衍生物。这些化合物是通过将 CPT 与 N-氨基酸去甲斑蝥直接偶联以中等产率合成的。评估了它们对四种人类肿瘤细胞系（HepG2、BGC-803、SW480 和 PANC-1）和正常人类细胞系 L-O2 和 HIEC 的细胞毒性。合成的 CPT 取代的去甲斑蝥胺类似物（3g和3f）显示出比 CPT 更好的抗肝癌活性。化合物3d、3e、3g、3h和3i对BGC803也表现出很强的抑制活性。