Expression of Tissue Transglutaminase in Human Thyroid Cancer Cell Lines: Effect of Novel Enantiopure Triazole Derivatives

A synthesis of (-)5b and (-)6d according to enzymatic resolution of racemic triazole derivatives 5b and 6d was performed with Lipozyme in 1,4-dioxane, using vinyl benzoate as the acyl donor. The effect of the compounds on TG2 overexpression in human thyroid cancer cell lines cultures at two degrees of malignancy and invasiveness was assessed. The involvement of TG2 in the activation of the apoptotic pathway is also shown. We found that the obtained compounds are able to reduce TG2 overexpression in follicular (FTC-133) and anaplastic (8305C) human thyroid cancer cell lines either in the cytosol, or in the nuclear compartment, activating also the apoptotic pathway. Our data suggest that they may represent new anticancer agents for human thyroid cancer.