Microwave assisted synthesis of some novel flurbiprofen hydrazidehydrazones as anti-HCV NS5B and anticancer agents [Anti-HCV NS5B ve antikanser ajani{dotless} olarak bazi{dotless} yeni flurbiprofen hidrazit-hidrazonlari{dotless}ni{dotless}n mikrodalga destekli sentezi]
dc.contributor.author | Aydin S. | |
dc.contributor.author | Kaushik-Basu N. | |
dc.contributor.author | Arora P. | |
dc.contributor.author | Basu A. | |
dc.contributor.author | Nichols D.B. | |
dc.contributor.author | Talele T.T. | |
dc.contributor.author | Akkurt M. | |
dc.contributor.author | Çelik I. | |
dc.contributor.author | Büyükgungör O. | |
dc.contributor.author | Guniz Kucukguzel Ş. | |
dc.date.accessioned | 2019-07-27T12:10:23Z | |
dc.date.accessioned | 2019-07-28T09:32:29Z | |
dc.date.available | 2019-07-27T12:10:23Z | |
dc.date.available | 2019-07-28T09:32:29Z | |
dc.date.issued | 2013 | |
dc.identifier.issn | 1309-0801 | |
dc.identifier.uri | https://dx.doi.org/10.12991/201317389 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/5553 | |
dc.description.abstract | The synthesis of a new series of flurbiprofen hydrazide-hydrazones using microwave assisted reactions is described. Substituted aldehydes were condensed with flurbiprofen hydrazide by microwave irradiation to corresponding hydrazones. Synthesis of N'-[(4-bromothiophen-2-yl)methylidene]-2-(2-fluorobiphenyl-4-yl) propanehydrazide (3o) employing microwave assisted process resulted in higher yields, in faster time and with less chemical waste compared to traditional techniques. (2-fluorobiphenyl-4-yl)-N'- (phenylmethylidene)propanehydrazide (3p) and N'-[(2-chloro-6-fluorophenyl) methylidene]- 2-(2-fluorobiphenyl-4-yl)propanehydrazide (3s) inhibited the growth of a leukemia cancer cell line HL-60 (TB) by 66.37% and an ovarian cancer cell line OVCAR-4 by 77.34% (single dose, 10 ?M), respectively at the National Cancer Institute (NCI), but had no significant effect on a panel of sixty human tumor cell lines. Flurbiprofen hydrazide-hydrazones were weak inhibitors of hepatitis C virus NS5B polymerase activity with N'-[(5-ethylfuran-2-yl) methylidene]-2-(2-fluorobiphenyl-4-yl)propanehydrazide (3m) being the most active of this series. Binding mode investigations of compound 3m suggested that allosteric pocket (AP)- B may be the potential binding site for flurbiprofen hydrazones and these results will also assist in further derivatization of 3m using the green chemistry approach and improve the potency of S-flurbiprofen hydrazide-hydrazones. | en_US |
dc.description.sponsorship | Guniz Kucukguzel, Ş.; Marmara University, Department of Pharmaceutical Chemistry, Istanbul, Turkey; email: gkucukguzel@marmara.edu.tr | en_US |
dc.language.iso | eng | en_US |
dc.relation.isversionof | 10.12991/201317389 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Anticancer activity | en_US |
dc.subject | E-Z isomerism | en_US |
dc.subject | Flurbiprofen | en_US |
dc.subject | Hepatitis C NS5B polymerase | en_US |
dc.subject | Hydrazide-hydrazone | en_US |
dc.subject | Microwave | en_US |
dc.title | Microwave assisted synthesis of some novel flurbiprofen hydrazidehydrazones as anti-HCV NS5B and anticancer agents [Anti-HCV NS5B ve antikanser ajani{dotless} olarak bazi{dotless} yeni flurbiprofen hidrazit-hidrazonlari{dotless}ni{dotless}n mikrodalga destekli sentezi] | en_US |
dc.type | article | en_US |
dc.relation.journal | Marmara Pharmaceutical Journal | en_US |
dc.contributor.department | Aydin, S., Marmara University, Department of Pharmaceutical Chemistry, Istanbul, Turkey -- Kaushik-Basu, N., UMDNJ-New Jersey Medical School, Department of Biochemistry and Molecular Biology, Newark, United States -- Arora, P., UMDNJ-New Jersey Medical School, Department of Biochemistry and Molecular Biology, Newark, United States -- Basu, A., UMDNJ-New Jersey Medical School, Department of Biochemistry and Molecular Biology, Newark, United States -- Nichols, D.B., UMDNJ-New Jersey Medical School, Department of Biochemistry and Molecular Biology, Newark, United States -- Talele, T.T., St. John's University, Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, Jamaica, NY 11439, United States -- Akkurt, M., Erciyes University, Department of Physics, Kayseri, Turkey -- Çelik, I., Cumhuriyet University, Department of Physics, Sivas, Turkey -- Büyükgungör, O., Ondokuz Mayis University, Department of Physics, Samsun, Turkey -- Guniz Kucukguzel, Ş., Marmara University, Department of Pharmaceutical Chemistry, Istanbul, Turkey | en_US |
dc.identifier.volume | 17 | en_US |
dc.identifier.issue | 1 | en_US |
dc.identifier.endpage | 34 | en_US |
dc.identifier.startpage | 26 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
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