Graduate School of Pharma-Medical Sciences, University of Toyama, Toyama 930-8555, Japan; Graduate School of Science and Engineering, University of Toyama, Toyama 930-8555, Japan.
Graduate School of Pharma-Medical Sciences, University of Toyama, Toyama 930-8555, Japan.
Bioorg Med Chem. 2022 Oct 1;71:116963. doi: 10.1016/j.bmc.2022.116963. Epub 2022 Aug 10.
Pipernonaline (1), one of the components of the spice pepper, preferentially reduced the survival of human pancreatic cancer PANC-1 cells under nutrient-deprived conditions witha PC value of 7.2 μM, suggesting that1couldpotentially lead to the development ofnew anticanceragents basedon theanti-austerity strategy. We have synthesized a total of 31 pipernonaline derivatives, revealing clear structure-activity relationships. Compound 9, which showed the strongest preferential cytotoxicity among synthesized derivatives, inhibited Akt activation and cancer cell migration, making it an extremely promising candidate compound for new pancreatic cancer agents based on the anti-austerity strategy.
胡椒酚（Pipernonaline，1）是香料胡椒的成分之一，在营养缺乏的条件下，优先降低人胰腺癌细胞 PANC-1 的存活率，其 PC 值为 7.2 μM，这表明 1 可能会潜在地导致基于抗饥饿策略的新型抗癌药物的开发。我们总共合成了 31 种胡椒酚衍生物，揭示了明确的结构-活性关系。合成衍生物中具有最强的选择性细胞毒性的化合物 9 抑制 Akt 激活和癌细胞迁移，使其成为基于抗饥饿策略的新型胰腺癌药物的极具潜力的候选化合物。
