Synthesis and in vitro anticancer activity of 2,4-azolidinedione-acetic acids derivatives

The synthesis and evaluation of anticancer activity of 2,4-thia(imida)zolidinedione-3- and 5-acetic acids amides were described. The structures of compounds were determined by IR, 1H NMR, and MS analysis. In vitro anticancer activity of these compounds has been tested in National Cancer Institute (NCI) and the relationships between structure and anticancer activity are discussed. Among 2,4-azolidinedione-acetic acids derivatives 2-[5-(4-chlorobenzylidene)-2,4-dioxo-imidazolidin-3-yl]-N-(2-trifluoromethyl-phenyl)-acetamide (Ic) was superior to other related compounds in terms of high selectivity for the leukemia CCRF-CEM (log GI50 = −6.06), HL-60(TB) (log GI50 = −6.53), MOLT-4 (log GI50 = −6.52) and SR (log GI50 = −6.51) cell lines.

A number of new 2,4-azolidinedione-acetic acid derivatives I–VI were synthesized and screened as perspective anticancer agents. 2-[5-(4-Chlorobenzylidene)-2,4-dioxo-imidazolidin-3-yl]-N-(2-trifluoromethyl-phenyl)-acetamide (Ic) was superior to other related compounds in terms of high selectivity for the leukemia CCRF-CEM, HL-60(TB), MOLT-4 and SR cell lines.Figure optionsDownload as PowerPoint slide