Benzilic acid based new 2-aryl-1,3-thiazolidin-4-one derivatives: Synthesis and anticancer activity

Abstract

Some new derivatives of 2-aryl-1,3-thiazolidin-4-one derivatives were produced (3a-p and 4a-p) in thesearch of potentially active new molecules with antitumor features. Compounds were obtained by cyclocondensationof 2-hydroxy-2,2-diphenyl-N-[(substituted phenyl)methylene]acetohydrazides (2) and mercaptoacetic acid or 2-mercaptopropionic acid. Identification and characterization of 32 new 2-aryl substituted thiazolidin-4-ones wereperformed with spectral and elemental analyzes. Compound 3c, 3g, 3j, 4g, 4n, and 4p were chosen as prototypes andassayed for their anticancer activity against diverse several cancer cell lines with in vitro primary anticancer test in theNational Cancer Institute. Compound 4g exhibited significant anticancer activity with the inhibition value 84.19%against a leukemia cell line MOLT-4 while compound 4p had a remarkable inhibition ratio (72.11%) against the growthof a CNS (central nervous system) cancer cell line SF-295 in the primary screen. These preliminary and important resultsindicated that the compounds carried 2-aryl-1,3-thiazolidin-4-one scaffold can be evaluated as potentially promisinganticancer agents.