二(喹唑啉-4-基)二硒醚的合成、表征及生物活性研究

Synthesis,Characterization and Biological Activities of 1,2-Bis( quinazolin-4-yl) diselane

含硒喹唑啉类化合物表现出优异的生物活性,本文选取其中的一个化合物二(喹唑啉-4-基)二硒醚,深入探讨了其合成,利用IR、~1H NMR、^(13)C NMR和MS谱图表征了其结构,并测定了对6种癌细胞株的体外抗癌活性和3种植物病原菌的抑菌活性.测试结果表明,二(喹唑啉-4-基)二硒醚有较好的体外抗肿瘤活性和中等的抑菌活性,并进行作用位点和作用机理的初步研究,结果表明该类化合物有可能成为潜在的抗肿瘤药物或抑菌药物的候选开发先导化合物.

Selenide compounds especially heterocyclic containing-selenium compounds exert multi-targeted bi- ological activities effects through various mechanisms. 1,2-Bis（quinazolin-4-yl） diselane was designed and synthesized with 4-chloroquinazoline and sodium diselenide. The structure was confirmed by 1R, 1H NMR, 13 C NMR and MS. The antitumor activity of 1,2-bis （quinazolin-4-yl）diselane was evaluated by MTr method a- gainst MDA-MB-435, A549, MDA-MB-231, SiHa, HeLa and PC3 cells in vitro. The antimicrobial activity of 1,2-bis （quinazolin-4-yl）diselane was evaluated by plate growth rate method against Gibberella zeae, Fusarium oxysporum and Cytospora mandshurica Miura in vitro. Antitumor activities test results suggested that title compound 1,2-bis （quinazolin-4-yl）diselane had superior antitumor activities. Antimicrobial activities test results suggested that title compound 1,2-bis （quinazolin-4-yl）diselane had moderate antibacterial activi- ties. The target sites and the preliminary mechanism studies suggested that 1,2-bis（quinazolin-4-yl） diselane could be used as lead compound to design and synthesis of more active and low toxicity anticancer and antimi- crobial drugs.