Synthesis, antileukemic and antiplatelet activities of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines

The synthesis, antileukemic and antiplatelet activity evaluation of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines are described. In general, it was found that compound 17o showed moderate antileukemic activity against MOLT3 human leukemic cancer cell lines. An arachidonic acid induced platelet aggregation effect on washed rat platelets was studied. Compound 17i was found to be the most potent. The antiplatelet properties may be mediated by interference with the arachidonic acid pathway.

Graphical abstractVarious vicinal diaryl heterocycles (1) are found to be pharmacologically important in medicinal chemistry. In this paper 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines (17a–r) were synthesized and evaluated for antileukemic and antiplatelet activities. The 2,3-diaryl-1,4-diazepine motif showed an interesting antiplatelet activity profile.Figure optionsDownload full-size imageDownload as PowerPoint slide