Reactions with Dimethylformamide‐Dimethylacetal: Synthesis and Reactions of Several New Pyridine and Pyrazolo[3,4‐b]pyridine Derivatives.

Elneairy, Mohamed A. A.; Gad‐Elkareem, Mohamed A. M.; Taha, Adel M.

doi:10.1002/chin.200738035

Cited by 1 publication

(1 citation statement)

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“…The starting compound, 4-((4fluorophenyl)diazenyl)-1H-pyrazole-3,5-diamine, 3, was prepared by diazotization of fluoroaniline then condensation with malononitrile followed by cycloaddition with hydrazine hydrate according to the reported procedure in the literature 24,25 . Enaminones,4a-c, were prepared in accordance to the reported procedure 26,27 .…”

Section: Chemical Partmentioning

confidence: 99%

Development of pyrazolo[1,5-a]pyrimidine derivatives: Synthesis, anticancer activity and docking study

Elbakry,

Harras,

Elsebaei

et al. 2023

Azhar International Journal of Pharmaceutical and Medical Scien

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It has been revealed that scaffolds made from pyrazolo [1,5-a]pyrimidines exhibit valuable biological activities, particularly anti-proliferative efficacy and blocking CDK activity. Therefore, new derivatives of pyrazolo[1,5-a]pyrimidines 5a-c were synthesized, and their chemical structures were validated using several spectral studies. These compounds were screened against MCF-7, HCT-116, and HepG2 malignant cell lines in comparison to doxorubicin to determine their anticancer activity. From the results, it is found that the order of activity of the examined compounds in general is 5b with a methoxy group, which is better in activity than 5a having phenyl group and 5c bearing methyl group. The anti-tumor potency against HCT-116 demonstrated that compound 5b was promising and close to the reference (IC50 = 8.64 µM). In addition, the synthesized compounds were submitted to molecular docking research against the CDK2 kinase enzyme in order to investigate the method of binding and understand the mechanism of the promising cytotoxic activity.

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