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 2018 , Vol 22 , Issue 4
Synthesis and characterization of 1,2,4-triazole containing hydrazide-hydrazones derived from (S)-Naproxen as anticancer agents
Muhammed İhsan HAN1,Hatice BEKÇİ2,Ahmet CUMAOĞLU2,Ş. Güniz KÜÇÜKGÜZEL1
1Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpaşa 34668 İstanbul, Turkey
2Erciyes University, Faculty of Pharmacy, Department of Pharmaceutical Biochemistry, Talas 38280 Kayseri, Turkey
DOI : 10.12991/jrp.2018.98 A novel series of new naproxen derivatives (S)-ethyl{[4-(4-fluorophenyl)-5-[(1-(6-methoxynaphtalen-2-yl)ethyl)]-4H-1,2,4-triazole-3-yl]sulphanyl}acetate (5), (S)-2-({5-[1-(6-methoxynaphtalen-1-yl)ethyl]-4-fluorophenyl-4H-1,2,4-triazole-3-yl}sulphanyl)acetohydrazide (6), 2-{[5-[1-(6-methoxynaphtalen-2-yl)ethyl]-4-(4-fluorophenyl)-4H-1,2,4-triazole-3-yl]sulphanyl}-N'-[(substituted)methylidene]acetohydrazides (7a-m) were synthesized, in this study. The structures of compounds 5, 6 and 7a-m were defined by spectral (1H-NMR, 13C-NMR, HR-MS and FT-IR) methods and their purity was proven by elemental analysis, thin layer chromatography and high pressure liquid chromatography. These compounds were evaluated for in vitro anticancer activity by using MTS method against PC-3 and DU-143 (androgen-independent human prostate cancer cell lines) and LNCaP (androgen-sensitive human prostate adenocarcinoma) prostate cancer cell lines. Cisplatin was used as the positive sensitivity reference standard. Compounds (7a-m) exhibited anticancer activity with IC50 values of 87.2-400 μM against prostate cancer cell lines. Keywords : Anticancer activity; MTS method; (S)-Naproxen; hydrazide-hydrazones
Marmara University