Synthesis, Characterization and Cytotoxicity Evaluation of Some Novel Pyridine Derivatives

摘要

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 5a – e , 6 and 7 , respectively. 4,4'-Bipyridine derivatives 9a – d were synthesized by a three-component reaction of isonicotinaldehyde, 2-cyanoacetohydrazide and activated nitriles 8a – d . Treatment of compound 9a with different aromatic aldehydes gave [1,2,4]triazolo[1,5- a ]pyridine derivatives 11a – c . 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.