Two series of xanthotoxin-triazole derivatives were designed, synthesized, and studied for their antiproliferative properties. The in vitro cytotoxicity of the compounds in the AGS cancer cell line and the L02 normal cell line was evaluated via MTT assay. Among the synthesized compounds, 9-((1-(4-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl)methoxy)-7H-furo[3,2-g]chromen-7-one (6p) was found to have the greatest antiproliferative activity against AGS cells (IC₅₀ = 7.5 μM) and showed better activity than the lead compound (xanthotoxin, IC₅₀ > 100 μM) and the reference drug (5-fluorouracil, IC₅₀ = 29.6 μM) did. The IC₅₀ value of 6p in L02 cells was 13.3 times higher than that in the AGS cells. Therefore, the compound exhibited better therapeutic activity and specificity compared with the positive control 5-fluorouracil. Cell cycle analysis revealed that compound 6p inhibited cell growth via the induction of S/G2 phase arrest in AGS cells. Compound 6p was identified as a promising lead compound for the further development and identification of 1,2,3-triazole-based anticancer agents.

设计，合成并研究了两个系列的花椒毒素-三唑衍生物的抗增殖特性。通过MTT分析评估化合物在AGS癌细胞系和L02正常细胞系中的体外细胞毒性。在合成的化合物中，9-（（1-（4-（三氟甲基）苯基）-1 H -1,2,3-三唑-4-基）甲氧基）-7 H-呋喃[3,2- g ]色烯发现-7-one（6p）对AGS细胞具有最大的抗增殖活性（IC ₅₀  = 7.5μM），并显示出比先导化合物（xanthotoxin，IC ₅₀  > 100μM）和参考药物（5-氟尿嘧啶）更好的活性，IC ₅₀  = 29.6μM）。IC ₅₀值L02细胞中的6p是AGS细胞中的6p。因此，与阳性对照5-氟尿嘧啶相比，该化合物表现出更好的治疗活性和特异性。细胞周期分析表明，化合物6p通过诱导AGS细胞中S / G2相停滞来抑制细胞生长。化合物6p被鉴定为用于进一步开发和鉴定基于1,2,3-三唑的抗癌剂的有前途的先导化合物。