School of Chemistry, National University of Ireland Galway, University Road, H91 TK3 Galway, Ireland.
Biochemistry, School of Natural Sciences, National University of Ireland Galway, University Road, H91 TK33 Galway, Ireland.
Molecules. 2018 Mar 3;23(3):574. doi: 10.3390/molecules23030574.
Cell viability studies for benzo[1,2,4]triazin-7-ones and 1,2,4-benzotriazinyl (Blatter-type) radical precursors are described with comparisons made with 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). All of the stable free radicals were several orders of magnitude less cytotoxic than the benzo[1,2,4]triazin-7-ones. The synthesis and evaluation of two new pyrid-2-yl benzo[1,2,4]triazin-7-ones are described, where altering the 1,3-substitution from phenyl to pyrid-2-yl increased cytotoxicity against most cancer cell lines, as indicated using National Cancer Institute (NCI) one-dose testing. COMPARE analysis of five-dose testing data from the NCI showed very strong correlations to the naturally occurring anti-cancer compound pleurotin. COMPARE is program, which analyzes similarities in cytotoxicity data of compounds, and enables quantitative expression as Pearson correlation coefficients. Compounds were also evaluated using the independent MTT assay, which was compared with SRB assay data generated at the NCI.
苯并[1,2,4]三嗪-7-酮和 1,2,4-苯并三嗪基（Blatter 型）自由基前体的细胞活力研究，并与 2,2,6,6-四甲基-1-哌啶氧基（TEMPO）进行了比较。所有稳定的自由基的细胞毒性都比苯并[1,2,4]三嗪-7-酮低几个数量级。描述了两种新型吡啶-2-基苯并[1,2,4]三嗪-7-酮的合成和评价，其中将 1,3-取代基从苯基改变为吡啶-2-基，提高了对大多数癌细胞系的细胞毒性，这是使用国家癌症研究所（NCI）单剂量测试表明的。NCI 的五剂量测试数据的 COMPARE 分析与天然抗癌化合物 pleurotin 显示出非常强的相关性。COMPARE 是一种分析化合物细胞毒性数据相似性的程序，并以 Pearson 相关系数进行定量表达。还使用独立的 MTT 测定法对化合物进行了评估，并将其与 NCI 生成的 SRB 测定数据进行了比较。
