A series of biotinylated camptothecin derivatives were designed and synthesized. The key to the synthesis was achieved by employing an esterification reaction and click chemistry. All of the new derivatives were tested for cytotoxicity against five human tumor cell lines, including HL-60, SMMC-7721, A-549, MCF-7, and SW480 with IC₅₀ values ranging from 0.13 to 21.53 μM. Most of the derivatives exhibited potent cytotoxicity, especially compound 17 (IC₅₀ = 0.13–3.31 μM) and compound 18 (IC₅₀ = 0.23–1.48 μM), which exhibited the highest potencies. The structure-activity relationships (SARs) of the biotinylated camptothecin derivatives were discussed for exploring novel anticancer agents.

设计并合成了一系列生物素化喜树碱衍生物。合成的关键是通过酯化反应和点击化学来实现的。测试了所有新衍生物对五种人类肿瘤细胞系的细胞毒性，包括HL-60，SMMC-7721，A-549，MCF-7和SW480，IC ₅₀值为0.13至21.53μM。大多数衍生物表现出强的细胞毒性，尤其是化合物17（IC ₅₀  = 0.13–3.31μM）和化合物18（IC ₅₀  = 0.23–1.48μM），具有最高的细胞毒性。讨论了生物素化喜树碱衍生物的结构-活性关系（SAR），以探索新型抗癌药。