PDF(Pubmed)
Abstract：
Various cancer-associated morbidities remain a growing global health challenge, resulting in a significant burden on healthcare systems worldwide due to high mortality rates and a frequent lack of novel therapeutic options for advanced and localized disease. Reactive oxygen species (ROS) play an important role in cancer pathogenesis and response to chemotherapeutics; therefore, it is crucial to develop novel compounds with both antioxidant and anticancer activity. In this study, a series of previously reported 3-((4-hydroxyphenyl)amino)propanoic acid derivatives (compounds 1-36) were evaluated for their anticancer and antioxidant activities. Compounds 12, 20-22, and 29 were able to reduce A549 cell viability by 50% and suppress A549 cell migration in vitro. These compounds also showed favorable cytotoxicity properties towards noncancerous Vero cells. The most promising candidate, compound 20, exhibited potent antioxidant properties in the DPPH radical scavenging assay. These results demonstrate that 3-((4-hydroxyphenyl)amino)propanoic acid could be further explored as an attractive scaffold for the development of novel anticancer and antioxidant candidates.
摘要：
各种与癌症相关的疾病仍然是一个日益严重的全球健康挑战。由于高死亡率和经常缺乏针对晚期和局部疾病的新型治疗选择，导致全球医疗保健系统负担巨大。活性氧（ROS）在癌症发病机理和对化疗药物的反应中起重要作用；因此，开发具有抗氧化和抗癌活性的新型化合物至关重要。在这项研究中,评价了一系列先前报道的3-((4-羟苯基)氨基)丙酸衍生物(化合物1-36)的抗癌和抗氧化活性。化合物12、20-22和29能够在体外将A549细胞活力降低50%并抑制A549细胞迁移。这些化合物还对非癌性Vero细胞显示出有利的细胞毒性性质。最有前途的候选人,化合物20在DPPH自由基清除试验中表现出有效的抗氧化特性。这些结果表明，3-（（4-羟苯基）氨基）丙酸可以进一步探索作为一种有吸引力的支架，用于开发新的抗癌和抗氧化剂候选物。
