One-Pot Synthesis of New Pyrazolo [3, 4, -d] Pyrimidine Derivatives and Study of their Antioxidant and Anticancer Activities

Abstract

An effort was made to synthesize a new series of pyrazolo [3,4-d] pyrimidine derivatives (2-5). The synthesis of these compounds was achieved via reaction of 3-methyl-1,4-dihydropyrazol-5-one (1) with a substituted aromatic aldehyde and urea or thiourea in mild reaction conditions, giving satisfactory yields. FT-IR and 1 H-NMR spectroscopies were used to characterize the structure of the newly synthesized compounds (2-5), where the spectral data confirmed the formation of these compounds. The antioxidant activity of these compounds (2-5) was examined in this study the synthesized compounds showed a moderate-high antioxidant effect, which was examined by using 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assays. The cellular toxicity of the compounds (2-5) was studied on MCF-7 cell lines using MTT assay. Compound (5) showed the highest toxicitytowards MCF-7 cell lines.

Recent medicinal approaches of novel pyrimidine analogs: A review

“…Among all compounds ( 26 ) exhibited good antioxidant activity (Inhibition: 82%) compared with the standard (Inhibition: 94%). The observed activity is due to the presence of hydroxy naphthalene and pyrazolo-pyrimidine scaffold [ 30 ].…”

Synthesis of New Oxopyrimidine and Cyanopyridine Derivatives Containing the Pyrimidine Benzothiazole Moiety with the Evaluating their Colon Anticancer Bioactivity

“…There are many fused rings that have been found to have wide applications for pharmacological activities [7]. Several literature reviews revealed a variety of fused ring systems of pyrimidines and their various chemotherapeutic activities, including anticancer [8][9][10], antioxidant [11], anti-inflammatory, and anti-microbial [12]. Heterocyclic, benzothiazole and pyrimidine constitute two highly active anti-tumor and antimicrobial active drugs.…”