Abstract
ABSTRACTThis work focuses the light on some remarkable achievements in clean and efficient green experimental synthesis, characterization and evaluation of the pharmaceutical and biochemical importance of new series of pyrazolo[1,2-b]phthalazinediones which synthesized through one-pot three-component condensation reaction of the appropriate of 1,2,3-triazolyl-pyrazole-carbaldehydes with active methylene compounds (as malononitriles or ethyl cyanoacetate) and 6-nitrophthalhydrazide using the grinding method in the presence of sodium hydroxide under solvent-free condition at room temperature, in very excellent yields. All the newly synthesized compounds were characterized by physical and chemical tools (FT-IR, 1H NMR and mass spectrometry). In addition, all the new synthesized derivatives were screened for their anticancer activity against hepatic cancer cell lines to evaluate their pharmaceutical importance.
Highlights
Identification of novel structures may be used in designing potent, new, less toxic and selective anticancer agents remains a major challenge for medical chemistry researchers
Multi-component reactions were considered as an excellent tool for synthesis of complex heterocycles owing to their advantages of the structure diversity, simpler procedures, intrinsic atom economy, energy saving and reduced waste (28–34)
Owing to the biochemical and pharmaceutical significance of 1,2,3-triazole and pyrazole rings, our growing interest in this part of the work is to incorporate between 1,2,3-triazole and pyrazole rings
Summary
Identification of novel structures may be used in designing potent, new, less toxic and selective anticancer agents remains a major challenge for medical chemistry researchers. The 1,2,3-triazole-based heterocyclic compounds have been well exploited for the generation of many medicinal scaffolds exhibiting anti-HIV(1), antibacterial (2) inhibitors of galectin-3 (3) activities, etc. Researchers reported 1,2,3-triazole derivatives that exhibited anticancer activities with excellent IC50 and IG50 (4–10). Pyrazole and pyrazole derivatives have drawn great attention of the researchers through the past few decades due to their high therapeutic importance as anti-inflammatory (11), antiglaucoma (12), antiviral (13), antimicrobial (14), antidiabetic (15) activities, etc. Fused phthalazines are considered as effective therapeutically active compounds; they possess a wide range of pharmaceutical applications such as anticancer (21, 22), anticonvulsant (23, 24), antimicrobial (25), antifungal (26) and anti-inflammatory (27) activities. The development of new methods for the synthesis of pyrazoles, triazoles and phthalazines continues to be an active area of research. Multi-component reactions were considered as an excellent tool for synthesis of complex heterocycles owing to their advantages of the structure diversity, simpler procedures, intrinsic atom economy, energy saving and reduced waste (28–34)
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