Anticancer activity of some new series of 2-(substituted)amino-1,3-thiazole derivatives

Abstract

A series of thiazole derivatives were synthesized and structurally elucidated by IR, 1H NMR, 13C NMR, mass and elemental analyses. The prepared compounds were screened for their cytotoxic activity against Leukemia HL-60 cell line. Compound 4b was considered as the most promising antitumor candidate among the tested compounds. Mechanism of action of compound 4b evaluated by flow cytometric assay revealed cell cycle arrest at G2/M phase and pre-G1 apoptosis. The ratio of apoptosis was also determined. Moreover, compound 4b increased the concentration of caspase 3 by 4 fold more than untreated control.

Thiazole Ring—A Biologically Active Scaffold

“…Bakare [120] reported the synthesis of a new series of 2-(substituted) amino-1,3thiazole derivatives and evaluation of their effect on the viability of the Leukemia HL-60 cell line using a colorimetric MTT assay. Compounds 77a, 77b, and 78 (Figure 30) exhibited the best activity among all compounds tested with IC 50 values in range of 1.3-8.9 µM.…”

“…Compounds 76a and 76b increased the life span of EAC-bearing mice due to the reduced viability of EAC cells and decreasing tumor value, thus proving the result of Gabr[119].The mean values of caspase-3 in the liver tissue were found to be 3.07 ± 0.119 (ng/mL) in the negative control group, which decreased in the positive control group by 70.57%, while the mean values of caspase-3 activities for both therapeutic and preventive groups treatments with compounds 76a and 76b significantly increase by 13.25% and 229.4%; 116.9% and 139.77%; respectively. Compound 76b was more active than 76a against the EAC of mice.Bakare[120] reported the synthesis of a new series of 2-(substituted) amino-1,3thiazole derivatives and evaluation of their effect on the viability of the Leukemia HL-60 cell line using a colorimetric MTT assay. Compounds 77a, 77b, and 78 (Figure30) exhibited the best activity among all compounds tested with IC 50 values in range of 1.3-8.9 µM.…”