Department of Chemistry, Mangalore University, Mangalagangothri, Konaje Post, Mangalore, Karnataka 574199, India.
Eur J Med Chem. 2012 Nov;57:407-16. doi: 10.1016/j.ejmech.2012.06.059. Epub 2012 Jul 7.
On account of the reported anticancer activity of triazolothiadiazines, we have synthesized a novel series of 6-arylsubstituted-3-[2-(4-substitutedphenyl)propan-2-yl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and tested for in-vitro cytotoxicity by trypan blue exclusion and MTT assay. These compounds were also evaluated for their in-vivo anthelmintic activity, as well as in-vitro antimicrobial studies. Amongst the tested compounds, the compound 7j was the most promising cytotoxic agent with IC(50) value of 10.54μM in MCF-7 cells. The compounds 7l and 7q exhibited excellent anthelmintic activity. The compounds 7d, 7f, 7j, 7l, 7o, 7p and 7r showed good antibacterial activity, whereas compounds 7e and 7k exhibited excellent antifungal activity. The structures of newly synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR and LCMS analysis.
鉴于三唑并噻二嗪类化合物具有抗癌活性,我们合成了一系列新型的 6-芳基取代-3-[2-(4-取代苯基)丙-2-基]-7H-[1,2,4]三唑并[3,4-b][1,3,4]噻二嗪,并通过台盼蓝排除法和 MTT 测定法测试其体外细胞毒性。这些化合物还评估了它们的体内驱虫活性以及体外抗菌研究。在所测试的化合物中,化合物 7j 是最有前途的细胞毒性剂,在 MCF-7 细胞中的 IC(50)值为 10.54μM。化合物 7l 和 7q 表现出优异的驱虫活性。化合物 7d、7f、7j、7l、7o、7p 和 7r 表现出良好的抗菌活性,而化合物 7e 和 7k 表现出优异的抗真菌活性。新合成化合物的结构通过 IR、(1)H NMR、(13)C NMR 和 LCMS 分析进行了表征。