دراسة تأثير مركبات ثيازولية جديدة في الخط الخلوي السرطاني MDA-MB-231

Abstract EN

Background and aim : Due to the side effects associated with available breast cancer treatments, it is an urgent challenge for medicinal research to develop more safe and selective anticancer drugs.

Among the design strategies in drug discovery, special attention has been paid to molecules containing sulfur heterocycles in their structures.

A series of thiazole derivatives is designed by the Faculty of Science in Damascus University through changing the substituents groups in the Thiazole ring.

We are testing the effect of two compounds on the growth of MDA MB-231 cell line and its migration in vitro.

Materials and methods : Cytotoxicity of the compounds against the MDA-MB-231 cell line was assessed using MTT assay within different incubation times and different concentrations.

Scratch assay was used to determine possible effects of compounds on the migratory capacity of MDA-MB-231.

Results : The compound 5-nitro-1,3-thiazol-2-amine showed an inhibitory effect on cancer cell migration while showing no effect on the cytotoxicity of the cancer cell line MDA-MB-231 using different concentrations (1, 5, 10, 25, 50, 100 µM/L) after incubation periods (24, 48, 72 h) (p.

value= 0.1076).

While the derived compound 4-[4-chloro-1-(5-nitro-1,3-thiazol-2-yl)-3 oxoazetidin-2-yl]benzaldehyde showed, in addition to the inhibitory effect of cell migration, a statistically significant cytotoxic effect on MDA-MB-231 cell line at a concentration of 100 µM/L after incubation for 72 h (p.value=0.0164), while no effect was shown after incubation for 24,48h.

Conclusion : Nitrothiazole compounds are considered as an excellent starting point to achieve future drug candidates in breast cancer management.

The addition of an oxoazetidin ring - containing a chlorine atom- at position 2 gives the thiazole ring a cytotoxic effect towards MDA MB-231 cell line.

These compounds also have an inhibitory effect on the migration of MDA-MB 231 cells in vitro.