Editor-in-Chief
Hatice Kübra Elçioğlu
Vice Editors
Levent Kabasakal
Esra Tatar
Online ISSN
2630-6344
Publisher
Marmara University
Frequency
Bimonthly (Six issues / year)
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
1Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpaşa 34668 İstanbul, Turkey2Marmara 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.