Synthesis, anticancer activity and mechanism of action of new phthalimido-1,3-thiazole derivatives

Abstract

In this work, 22 new compounds were obtained and evaluated for their cytotoxic activity on peripheral blood mononuclear cells (PBMC) and eight different tumor cell lines. All compounds displayed IC₅₀ values above 100 μM when assayed against PBMCs. The cytotoxic assays in tumor cell lines revealed that sub-series of phthalimido-bis-1,3-thiazoles (5a-f) exhibited the best anti-tumor activity profile, presenting viability values below 59 %. As a result, the IC₅₀ value was calculated for compounds 5a-f and 4c, and compounds 5b and 5e were selected for further assays due to their best IC₅₀s. Considering the results presented by the sub-series 5a-f, the importance of the 1,3-thiazole ring in improving the anti-tumor activity was pointed out. Together, the results highlighted the anti-tumor activity of phthalimido-bis-1,3-thiazole derivatives.

Keywords: 1,3-thiazole; Anti-tumor activity; Cancer; Malignant melanoma; Phthalimide.