Editor-in-Chief İlkay Küçükgüzel Associate Editor Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Quarterly (January-April-July-October) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Marmara Pharmaceutical Journal 2015 , Vol 19 , Issue 3
Synthesis and Anticancer Activity of Some Novel Tolmetin Thiosemicarbazides
Yakup DADAS1, Goknil Pelin COSKUN1, Ozlem BINGOL-OZAKPINAR2, Derya OZSAVCI2, Sukriye Guniz KUCUKGUZEL1
1Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpaşa 34668 İstanbul, Turkey
2Marmara University, Faculty of Pharmacy, Department of Biochemistry, Haydarpaşa 34668 İstanbul, Turkey
DOI : 10.12991/mpj.201519328306 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, 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-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. Keywords : Apoptosis, tolmetin, thiosemicarbazide, PC-3, colon cancer.
Marmara University