Synthesis and anticancer activity of some novel benzothiazole-thiazolidine derivatives.

Sixteen new 2-(benzothiazol-2-ylthio)-N′-(3-substituted-4-(3,4-substitutedphenyl)thiazol-2(3H)-ylidene)acetohydrazide derivatives (<bold>4a</bold>-<bold>4p</bold>) were synthesized. The structures of the synthesized compounds were elucidated using FT-IR, 1H-NMR, 13C-NMR, and HRMS spectral data. Anticancer activity of the compounds <bold>4a</bold>-<bold>4p</bold> against C6 (rat brain glioma) and A549 (human lung adenocarcinoma) cell lines was evaluated by using MTT, inhibition of DNA synthesis, and flow cytometric analysis assays. According to MTT assay, <bold>4a</bold> and <bold>4d</bold> were found to be the most active compounds against C6 cell line with an IC50 value of 0.03 mM. Moreover, IC50 values of <bold>4a</bold> (0.2 mM) and <bold>4d</bold> (0.1 mM) against NIH3T3 (mouse embryo fibroblast cell line) were higher than their IC50 values (0.03 mM) against C6 cell line. Accordingly, selectivity of compound <bold>4a</bold> against C6 cell line was two-fold higher than that of compound <bold>4d.</bold> Flow cytometry analysis showed that these compounds display anticancer activity by inducing apoptosis. As a result, compound <bold>4a</bold> has a remarkable anticancer activity and a good selectivity towards C6 cell lines. [ABSTRACT FROM AUTHOR]