Design, Synthesis and Biological Evaluation of Cyanopyridines, Pyridopyrazolopyrimidines and Pyridopyrazolotriazines as Potential Anticancer Agents

Author(s): Reda Mohammed Keshk*, Batoul Mohamed Izzularab

Journal Name: Current Organic Synthesis

Volume 18 , Issue 5 , 2021

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Graphical Abstract:


Background: The continuous need for new anticancer drugs is never-ending task due to cancer resistance to the existing drugs.

Objective: This article aimed to design, synthesis, characterization, and anticancer evaluation of cyanopyridines, pyridopyrazolopyrimidines and pyridopyrazolotriazines.

Methods: Anticancer activity of the synthesized compounds was determined using MTT assay against three cancer cell lines, namely liver cancer cell line (HepG-2), pancreatic cancer cell line (PANC-1), non-small lung cancer cell line (A-549) and normal fibroblast.

Results and Discussion: A series of 3-cyanopyridines (2a,b, 4, 5, 9), pyridopyrimidine (10), pyridopyrazolopyrimidines (11a-c, 12a,b, 18), pyrazolopyridine salt (13) and pyridopyrazolotriazines (16a,b) were synthesized from 3-cyano-4,6-dimethyl-2-pyridone. The synthesized compounds were evaluated in vitro for their anticancer activity and their chemical structures were determined by elemental analysis and spectroscopic data.

Conclusion: Some of the synthesized compounds showed remarkable anticancer activities, especially 11a exhibited superior potency to the reference drug cisplatin against A-549 (IC50 = 9.24 μg mL-1 compared to 11.76 μg mL-1 for reference drug) and was found to be safe (IC50 = 66 μg mL-1) for normal fibroblast. Furthermore, compound 16a displayed the highest activity among the tested compounds against HepG-2 (IC50 = 6.45 μg mL-1 equipotent to cisplatin) with the highest safety profile for normal fibroblast (IC50=113.97 μg mL-1).

Keywords: Cyanopyridines, pyrazolopyridines, pyrazolopyridine salt, pyridopyrazolopyrimidines, pyridopyrazolotriazines, anticancer activity, cytotoxicity assay.

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Article Details

Year: 2021
Published on: 29 December, 2020
Page: [483 - 492]
Pages: 10
DOI: 10.2174/1570179417666201229163045
Price: $65

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