Synthesis of new indeno[1,2-e]pyrimido[4,5-b][1,4]diazepine-5,11-diones as potential antitumor agents

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 GI50 values ranging from 0.49 to 1.46 μM, in vitro assay.

Novel indeno[1,2-e]pyrimido[4,5-b][1,4]diazepine-5,11-diones were synthesized and screened as antitumorals. Some derivatives exhibited remarkable GI50 values ranging from 0.49 to 1.46 μM, in vitro assay.Figure optionsDownload as PowerPoint slide