Insuasty Braulio, Orozco Fabian, Lizarazo Carolina, Quiroga Jairo, Abonia Rodrigo, Hursthouse Mike, Nogueras Manuel, Cobo Justo
Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, A.A. 25360 Cali, Colombia.
Bioorg Med Chem. 2008 Sep 15;16(18):8492-500. doi: 10.1016/j.bmc.2008.08.023. Epub 2008 Aug 12.
Novel racemic indeno[1,2-e]pyrimido[4,5-b][1,4]diazepine-5,11-diones 3-29 were obtained regioselectivily from the reaction of 5,6-diamino-3,4-dihydropyrimidin-4-ones 1 and 2-arylideneindandiones 2 as reagents. These compounds have been evaluated at the US National Cancer Institute (NCI) for their ability to inhibit approximately 60 different human tumor cell lines, where 5 and 6 presented remarkable activity against 57 and 48 cancer cell lines, respectively, with the most important GI(50) values ranging from 0.49 to 1.46 microM, in vitro assay.
新型外消旋茚并[1,2-e]嘧啶并[4,5-b][1,4]二氮杂卓-5,11-二酮3-29是由5,6-二氨基-3,4-二氢嘧啶-4-酮1与2-亚芳基茚满二酮2作为试剂反应区域选择性得到的。这些化合物在美国国立癌症研究所（NCI）进行了评估，以检测它们抑制约60种不同人类肿瘤细胞系的能力，其中化合物5和6分别对57种和48种癌细胞系表现出显著活性，体外试验中最重要的GI(50)值范围为0.49至1.46微摩尔。
