Novel imidazo[4,5-b]pyridine and triaza-benzo[c]fluorene derivatives: Synthesis, antiproliferative activity and DNA binding studies
作者:Marijana Hranjec、Borka Lučić、Ivana Ratkaj、Sandra Kraljević Pavelić、Ivo Piantanida、Krešimir Pavelić、Grace Karminski-Zamola
DOI:10.1016/j.ejmech.2011.03.062
日期:2011.7
paper, we have described the synthesis and biological activity of the novel derivatives of imidazo[4,5-b]pyridines and triaza-benzo[c]fluorenes (7–21, 24–26, 28–29). A preponderance of these compounds exerted strong cytostatic effects on the panel of seven human tumour cell lines in a dose-dependent manner. In particular, imidazo[4,5-b]pyridines and triaza-benzo[c]fluorenes including 2-imidazolinyl derivatives
在本论文中,我们已经描述了咪唑并[4,5的新衍生物的合成和生物活性b ]吡啶和三氮杂-苯并[ Ç ]芴(7 - 21,24 - 26,28 - 29)。这些化合物中的大多数以剂量依赖的方式对七种人类肿瘤细胞系产生了强大的细胞抑制作用。特别地,咪唑并[4,5- b ]吡啶和包括2-咪唑啉基衍生物的三氮杂-苯并[ c ]芴具有最有效的抗肿瘤活性。同样,三氮杂苯并[ c ]芴18和20在正常的人类成纤维细胞中诱导了对测试的肿瘤细胞系的强生长抑制作用,并显示出低细胞毒性。这些化合物的DNA相互作用研究表明,N-甲基化的16和2-咪唑啉基28三氮杂苯并[ c ]芴以嵌入方式与DNA结合。