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Synthesis, Characterization and Cytotoxicity Evaluation of Some Novel Pyridine Derivatives

Khaled Samir Mohamed, Eman H. Tawfik, Hemat M. Dardeer, Ahmed Ali Fadda


Reaction of isonicotinaldehyde with 2-cyanoacetohydrazide afforded (E)-2-cyano-N'-(pyridin-4-ylmethylene)acetohydrazide (1). Compound 1 was used as the precursor for the synthesis of novel pyridine derivatives by reaction with different arylidene malononitriles, malononitrile and acetylacetone to give pyridine derivatives 5ae, 6 and 7, respectively. 4,4'-Bipyridine derivatives 9ad were synthesized by a three-component reaction of isonicotinaldehyde, 2-cyanoacetohydrazide and activated nitriles 8ad. Treatment of compound 9a with different aromatic aldehydes gave [1,2,4]triazolo[1,5-a]pyridine derivatives 11ac. All reaction products were characterized by analytical and spectral data. For the novel compounds their bioactivity as antitumor agents was examined for in vitro cytotoxicity against HepG-2 and MCF-7. It was found that compounds 9a and 9b have high cytotoxic activity against both HepG-2 and MCF-7.


Pyridine; 4,4'-Bipyridine; Isonicotinaldehyde; 2-Cyanoacetohydrazide

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