1. SYNTHESIS AND ANTICANCER ACTIVITY OF TOLMETIN THIOSEMICARBAZIDES
- Author
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Şükriye Küçükgüzel, Goknil Pelin Coskun, Yakup Dadas, Derya Özsavcı, and Ozlem Bingol-Ozakpinar
- Subjects
chemistry.chemical_classification ,Stereochemistry ,Hydrazide ,Human prostate ,In vitro ,Human colon cancer ,chemistry.chemical_compound ,chemistry ,Apoptosis ,medicine ,Tolmetin ,Pharmacology (medical) ,General Pharmacology, Toxicology and Pharmaceutics ,Cancer cell lines ,Alkyl ,medicine.drug ,Nuclear chemistry - Abstract
A novel series of new tolmetin hydrazide derivatives, N -Alkyl/Arylsubstitued- 2-{[1-methyl-5-(4-methylbenzoyl)-1 H -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, 1 H-NMR, 13 C-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)-1 H- 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 .
- Published
- 2015
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