SYNTHESIS AND ANTICANCER ACTIVITY OF TOLMETIN THIOSEMICARBAZIDES

Year 2015, Volume: 19 Issue: 3, 259 - 267, 29.06.2015

Yakup Dadaş Göknil Coşkun , Özlem Bingöl-özakpınar , Derya Özsavcı , Şükriye Küçükgüzel

https://doi.org/10.12991/mpj.201519328306

https://izlik.org/JA37WK45FL

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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