Expedient Synthesis and Antitumor Evaluation of Novel Azaheterocycles from Thiazolylenaminone

Thiazole is a functional group used in cancer treatment modalities in synthetic and natural antitumor medications. In this context, convenient synthesis of new 5-heteroaryl-thiazoles is described via reactions of thiazolylenaminone with sulfanilamide, sulfathiazole, hydrazine hydrate, phenylhydrazine, hydroxylamine, guanidine, aminoazoles, beta-dicarbonyl compounds, and diazotized aminoazoles. The constitution of the constructed thiazoles was avowed by elemental analyses and spectral data as well as alternative syntheses wherever possible. Thiazoles were also tested for their antitumor activity toward human cancer cell lines (MCF-7, HCT-116, and HepG-2) and one normal cell line (REP1). Among the synthesized thiazoles, compounds 6, 19, and 23a showed high potent antitumor profiles toward cancer cell lines and found no evidence of human toxicity.

Automated summary

This study describes the convenient synthesis of new 5-heteroaryl-thiazoles through reactions of thiazolylenaminone with various compounds and their evaluation for antitumor activity. Among the synthesized thiazoles, compounds 6, 19, and 23a showed potent antitumor profiles without evidence of human toxicity.