Abstract
BackgroundDescribed 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 HNO2 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).ResultsA 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 IC50 value 3.6 μM, followed by compounds 9, 5a, 8, 5e, 6e, 5b, 5f, 7a, 5c, 6c, 7b, 6a, 11, 5d and 6d.ConclusionA 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.
Highlights
Described a series of main target compounds pyrimido[5,4-e][1,2,4]triazines is obtained via conden‐ sation of 6-hydrazinyluracil with different aromatic aldehydes to give the hydrazones followed by nitrosation with HNO2 intramolecular cyclization
Chemistry In continuation to our research, the importance of fervenulin and its diverse pharmacological activity on the medical field, especially as antitumors, we became interested in the prospect of developing our strategies to synthesize new fervenulin analogues of pyrimidotriazine and pyrazolopyrimidine derivatives using 6-hydrazinyl-1-propyluracil (4) as a core for construction
Our strategy is directed towards the synthesis of new pyrimido[5,4-e][1,2,4]triazine and pyrazolopyrimidine compounds because they have found wide applications in pharmaceutical fields
Summary
Described a series of main target compounds pyrimido[5,4-e][1,2,4]triazines is obtained via conden‐ sation of 6-hydrazinyluracil with different aromatic aldehydes to give the hydrazones followed by nitrosation with HNO2 intramolecular cyclization. 1,2,4-triazine and their fused ring structures with one or more heterocycles represent an important class of nitrogen heterocycles compounds. It possess the motif part of naturally and synthetic pharmaceutical products [1–9]. They exhibit a broad spectrum biological effects [10] with antibacterial [11, 12], antitumor [13, 14], anticonvulsant [15], anti-inflammatory [16], and antiviral properties [17]. 6-Azacytosine and 6-azauracil are used as effective antiviral and antitumor activities [18–21]. The tirapazamine (TPZ) is efficacious in the treatment of different human cancer cells via inducing DNA damage in poorly oxygenated tumor cells [22].
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