Synthesis and Evaluation of the Antitumor Activity of (E)-3-((2-(5-(4-chlorophenyl) thiazol-2-yl) hydrazono) methyl) benzene-1,2-diol “In vitro and In vivo Study”

Abstract

Background: Thiazole nucleus–containing compounds have an antitumor efficiency against various types of cancer. Purpose: The present study was designed to determine the cytotoxic effect of newly synthesized thiazole derivative (TD1) on human cancer cell lines, in addition to evaluate its antitumor activity against Ehrlich ascites carcinoma (EAC) in mice. Materials and Methods: TD1 was synthesized and investigated for its cytotoxic effect on HCT116 (colon cancer), HepG2 (liver cancer), PC3 (prostate cancer) and MCF7 (breast cancer). The effect of TD1 on cell viability, tumor volume, and percent of increase in life span (% ILS) in Ehrlich–bearing mice was studied. Hematological parameters, liver and kidney function tests were evaluated. The activity of superoxide dismutase (SOD) and catalase (CAT), as well as malondialdehyde (MDA) and reduced glutathione levels were determined in liver and kidney tissues. The expression of P53 in EAC was analyzed by flow cytometry. Results: TD1 demonstrated an inhibitory effect on both cancer cell lines in vitro and Ehrlich ascites cells in vivo. TD1 increased in life span of Ehrlich–bearing mice compared to control. Cell cycle and flow cytometric analysis revealed that TD1 directed Ehrlich cells toward apoptosis by increasing of P53 expression. Conclusion: It was concluded that TD1 have a potent antitumor activity against Ehrlich ascites carcinoma in mice beside a cytotoxic effect on MCF-7, PC3, HepG2 and HCT-116.