Synthesis of New Benzothiazole Derivatives and Evaluation of Cytotoxicity of N-(6-Substitued-1,3-benzothiazol-2-yl)-4-phenyl-1,3-thiazol-2(3H)-imine Compounds

Cyclization of unsymmetrical thioureas affords N-(6-substitued-1,3-benzothiazol-2-yl)-4-phenyl-1,3-thiazol-2(3H)-imine compounds by the reaction of 1-(1,3-benzothiazol-2-yl)thiourea derivatives and 2-bromoacetophenone in the presence of Et3N. Also, methyl-1,3-benzothiazol-2-yl carbamodithioate derivatives with methyl anthranilate were reacted and 3-(benzo[d]thiazol-2-yl)-2-thioxo-2,3-dihydroquinazolin-4(1H)-one derivatives as new compounds are synthesized. In the following, synthesized compounds (2a- 2d) were evaluated for anti-tumor activity against MCF-7, MAD-MD-231, HT-29, HeLa, Neuro-2a, K-562 and L-929 cell lines and the results obtained from MTT-assay revealed the best cytotoxicity for 2b compound containing a phenolic segment in their buildings. On the other hand, apoptosis assay for this compound was also carried out by flow cytometry supporting the other results.

Synthesis of New Benzothiazole Derivatives and Evaluation of Cytotoxicity of N-(6-Substitued-1,3-benzothiazol-2-yl)-4-phenyl-1,3-thiazol-2(3H)-imine Compounds Keywords:

Unsymmetrical thioureas , MTT-assay , Flow Cytometry , TUNEL assay , 1-(1 , 3-benzothiazol-2-yl)thiourea , 3-(benzo[d]thiazol-2- yl)-2-thioxo-2 , 3-dihydroquinazolin-4(1H)-one