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Background  Described a series of main target compounds pyrimido[5,4- e ][1,2,4]triazines is obtained via condensation of 6-hydrazinyluracil with different aromatic aldehydes to give the hydrazones followed by nitrosation with HNO 2  then intramolecular cyclization. On the other hand, pyrazolopyrimidines can be obtained by the reaction of hydrazones with dimethylformamide-dimethylacetal (DMF-DMA), DMF-DMA in the presence of DMF or by refluxing the hydrazinyluracil with DMF-DMA in the presence of DMF directly. The newly synthesized compounds are evaluated in vitro for their anticancer activity against human lung carcinoma (A549).    Results  A newly substituted compounds of benzaldehyde-pyrimidin-4-yl)hydrazones ( 5a – f ), pyrimido[5,4- e ][1,2,4]triazines  6a – e , arylethylidenehydrazinylpyrimidine  7a , b  and pyrazolopyrimidines  9 , 11  are screened for cytotoxic activity against human lung carcinoma (A549) cell line. They exhibited a good yield. Compound  6b  shows the highest effect with IC 50  value 3.6 μM, followed by compounds  9 ,  5a ,  8 ,  5e ,  6e ,  5b ,  5f ,  7a ,  5c ,  6c ,  7b ,  6a ,  11 ,  5d  and  6d .    Conclusion  A simple and efficient route is used for the synthesis of pyrimido[5,4- e ][1,2,4]triazines and pyrazolopyrimidines. The synthesized compounds are screened for antitumor activity.

chemistry central journal

Synthesis and anticancer evaluation of some novel pyrimido[5,4-e][1,2,4]triazines and pyrazolo[3,4-d]pyrimidine using DMF-DMA as methylating and cyclizing agent