Synthesis of chromenone, pyrimidinone, thiazoline, and quinolone derivatives as prospective antitumor agents

Abstract

Hydrazide-hydrazone namely, 2-cyano-N′-((1-phenyl-3-[thiophen-2-yl]-1H-pyrazol-4-yl)methylene)acetohydrazide (3) underwent a series of reactions with some chemical reagents to construct new biologically active N-heterocycles, for example, chromenone, benzochromenone, thiazoline, and quinolone derivatives. Treating the nitrile derivative 3 with 2,4-dichlorobenzaldehyde and pyrazole aldehyde 1 afforded the corresponding condensed products. Some of the synthesized compounds were screened for their in vitro antitumor activities against two different human tumor cell lines including hepatocellular liver carcinoma (HepG2) and breast adenocarcinoma (MCF7) activities. Compound 3 was the most potent against the two tumors.