SYNTHESIS AND ANTICANCER ACTIVITY OF TOLMETIN THIOSEMICARBAZIDES

Abstract

A novel series of new tolmetin hydrazide derivatives, N-Alkyl/Arylsubstitued- 2-{[1-methyl-5-(4-methylbenzoyl)-1H-pyrol-2-yl]acetyl}hydrazinecarbothioamides [4a-j] have been synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, 1H-NMR, 13C-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-pyrol-2-yl]acetyl}hydrazinecarbothioamide [SGK-524; 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. 

Keywords

• Apoptosis
• tolmetin
• thiosemicarbazide
• PC-3
• colon cancer

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