Synthesis and characterization of 1,2,4-triazole containing hydrazide-hydrazones derived from (S)-Naproxen as anticancer agents
Autor: | Muhammed İhsan Han, Ahmet Cumaoğlu, Hatice Bekci, Şükriye Küçükgüzel |
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Přispěvatelé: | Han, Muhammed Ihsan, Bekci, Hatice, Cumaoglu, Ahmet, Kucukguzel, S. Guniz |
Jazyk: | angličtina |
Rok vydání: | 2017 |
Předmět: |
Naproxen
ANALOGS ANTIPROLIFERATIVE ACTIVITY DERIVATIVES BIOLOGICAL-ACTIVITIES Pharmacology toxicology 1 2 4-Triazole (S)-Naproxen MTS method hydrazide-hydrazones Hydrazide ANTI-HCV Combinatorial chemistry Anticancer activity APOPTOSIS chemistry.chemical_compound ETODOLAC chemistry MICROWAVE-ASSISTED SYNTHESIS medicine DIFLUNISAL HYDRAZIDE NAPROXEN medicine.drug |
Popis: | 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 (H-1-NMR, C-13-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 mu M against prostate cancer cell lines. |
Databáze: | OpenAIRE |
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