Synthesis and Anticancer Evaluation of Novel Derivatives of Isoxazolo[4,5-][1,2,4]triazepine Derivatives and Potential Inhibitors of Protein Kinase C.

In the present study, using Thorpe's reaction with Gewald's modification, 4-acetylamino-5-acetyl or 5-benzoyl 3-carboxamide compounds or were obtained. From these compounds, two series of compounds (, , and and , , and ) were obtained with 98% hydrazine. Compounds , , , and were then reacted with the appropriate aldehydes to afford a series of new isoxazole derivatives (, , and ) and the main compounds, and , were isoxazolo[4,5-][1,2,4]triazepine derivatives. The anticarcinogenic activities of selected compounds were tested on six lines of cancer cells, and their activities were compared with the relevant concentrations of the anticarcinogenic drugs cisplatin and doxorubicin in IITD PAN. Several compounds were tested on 60 lines of cancer cells by the NCI (Bethesda, MD, USA). The cyclization of compound into derivative was also carried out. Compound showed extremely high antitumor activity.