PDF(Pubmed)
Abstract：
One of the most essential health problems is cancer, the first or second cause of death worldwide. Head and neck cancers are hard to detect due to non-specific symptoms. The treatment often relies on a combination of radio and chemotherapy. For this reason, the research of new anticancer compounds is fundamental. The natural and synthetic compounds with 1,4-naphthoquinone scaffold is characterized by high anticancer activity. The study aimed to evaluate the synthesis and anticancer activity of hybrids 1,4-naphthoquinone with thymidine derivatives. The series of compounds allows us to check the influence of the substituent in the C3\' position of the thymidine moiety on the cytotoxicity against squamous cancer cell lines (SCC-9 and SCC-25) and submandibular gland cancer (A-253). An annexin V/propidium iodide (PI) co-staining assay shows that derivatives cause the apoptotic in SCC-25 and A-253 cell lines. The molecular docking study examined the interaction between the active site of the BCL-2 protein and the hybrids.
摘要：
最重要的健康问题之一是癌症，全球第一或第二大死亡原因。由于非特异性症状，头颈部癌症很难发现。治疗通常依赖于放疗和化疗的组合。出于这个原因,新的抗癌化合物的研究是基础。具有1,4-萘醌支架的天然和合成化合物具有高抗癌活性。该研究旨在评估具有胸苷衍生物的杂化1,4-萘醌的合成和抗癌活性。该系列化合物使我们能够检查胸苷部分C3位置的取代基对针对鳞状癌细胞系（SCC-9和SCC-25）和颌下腺癌（A-253）的细胞毒性的影响。膜联蛋白V/碘化丙啶(PI)共染色测定显示衍生物在SCC-25和A-253细胞系中引起细胞凋亡。分子对接研究检查了BCL-2蛋白的活性位点与杂种之间的相互作用。
