ANTICANCER ACTIVITY EVALUATION OF NEW PHORTRESS ANALOGUES AND IDENTIFICATION OF BIOACTIVE METABOLISM PRODUCTS USING LCMS-IT-TOF

摘要

Phortress, including benzothiazole moiety, is a prodrug displaying anticancer activity. The active metabolite of phortress is a potent agonist of the aryl hydrocarbon receptor and switches on cytochrome P450 CYP1A1 gene expression [1]. In the present study, new analogues of phortress were synthesized and investigated for anticancer activity. In order to identify a probable active metabolite, biotransformation studies were conducted and results were examined by mass spectroscopic analyses.