Synthesis and anticancer activity of some novel benzothiazole-thiazolidine derivatives

<p>Sixteen new 2-(benzothiazol-2-ylthio)-N′-(3-substituted-4-(3,4-substitutedphenyl)thiazol-2(3H)-ylidene)acetohydrazide derivatives (<b>4a</b>-<b>4p</b>) were synthesized. The structures of the synthesized compounds were elucidated using FT-IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and HRMS spectral data. Anticancer activity of the compounds <b>4a</b>-<b>4p</b> 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, <b>4a</b> and <b>4d</b> were found to be the most active compounds against C6 cell line with an IC<sub>50</sub> value of 0.03 mM. Moreover, IC<sub>50</sub> values of <b>4a</b> (0.2 mM) and <b>4d</b> (0.1 mM) against NIH3T3 (mouse embryo fibroblast cell line) were higher than their IC<sub>50</sub> values (0.03 mM) against C6 cell line. Accordingly, selectivity of compound <b>4a</b> against C6 cell line was two-fold higher than that of compound <b>4d.</b> Flow cytometry analysis showed that these compounds display anticancer activity by inducing apoptosis. As a result, compound <b>4a</b> has a remarkable anticancer activity and a good selectivity towards C6 cell lines.</p>