National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, No. 6 Nanhu Yaoyuan, Wuhan 430064, PR China.
Eur J Med Chem. 2012 Aug;54:248-54. doi: 10.1016/j.ejmech.2012.05.003. Epub 2012 May 12.
A series of novel gramine analogues were designed and synthesized via a convenient three-component reaction, and which were evaluated for their inhibition activities against cell proliferation. Their structures were confirmed by satisfactory spectra analyses mainly including (1)H NMR, and ESI-MS analyses. The preliminary assays indicated that some of the newly synthesized compounds displayed significantly good inhibition activities against human lung cancer (NCI-H460), hepatocellular liver carcinoma (HepG2), gastric cancer (SGC-7901 and BGC-823) cell lines compared with the control 5-Fluorouracil (5-FU), which might be developed as novel lead scaffold for potential anticancer agents.
设计并合成了一系列新型的禾本科类似物，通过方便的三组分反应，并评估了它们对细胞增殖的抑制活性。它们的结构通过满意的光谱分析主要包括（1）H NMR 和 ESI-MS 分析得到确认。初步试验表明，与对照 5-氟尿嘧啶（5-FU）相比，一些新合成的化合物对人肺癌（NCI-H460）、肝癌（HepG2）、胃癌（SGC-7901 和 BGC-823）细胞系表现出显著的良好抑制活性，它们可能被开发为新型的潜在抗癌药物的先导骨架。
