Synthesis and Anticancer Activity of Some Novel Tolmetin Thiosemicarbazides

Abstract

A novel series of new ten tolmetin hydrazide derivatives, N-Alkyl/Arylsubstituted-2-{[1-methyl-5-(4-methylbenzoyl)-1H- pyrrol-2-yl]acetyl}hydrazinecarbothioamides [4a-j] have been synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, H-1-NMR, C-13-NMR and 2D-NMR) methods and their purity were proven by elemental analysis and TLC. Tolmetin [1] and N-(4-fluorophenyl)-2-{[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2- yl] acetyl}hydrazinecarbothioamide [4d] were evaluated for in vitro using the MTT colorimetric method for anticancer activity. Androjen-independed human prostate cancer cell line PC-3 (ATCC, CRL-1435), human colon cancer cell lines HCT-116 (ATCC, CCL-247) and HT-29 (ATCC, HTB-38) were used in this study. Compound 4d exhibited anticancer activity against PC-3 whereas Tolmetin showed minor activity comparing to compound 4d.