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CarbORev-5901: The First Carborane-Based Inhibitor of the 5-Lipoxygenase Pathway
dc.creator | Kuhnert, Robert | |
dc.creator | Sárosi, Menyhárt-Botond | |
dc.creator | George, Sven | |
dc.creator | Lönnecke, Peter | |
dc.creator | Hofmann, Bettina | |
dc.creator | Steinhilber, Dieter | |
dc.creator | Murganić, Blagoje | |
dc.creator | Mijatović, Sanja | |
dc.creator | Maksimović-Ivanić, Danijela | |
dc.creator | Hey-Hawkins, Evamarie | |
dc.date.accessioned | 2017-11-23T11:33:23Z | |
dc.date.available | 2900-01-01 | |
dc.date.issued | 2017 | |
dc.identifier.issn | 1860-7179 | |
dc.identifier.uri | http://doi.wiley.com/10.1002/cmdc.201700309 | |
dc.identifier.uri | https://radar.ibiss.bg.ac.rs/handle/123456789/2789 | |
dc.description.abstract | The progression of cancer is accelerated by increased proliferation, angiogenesis, and inflammation. These processes are mediated by leukotrienes. Several cancer cell lines overexpress 5-lipoxygenase, an enzyme that converts arachidonic acid into leukotrienes. An early inhibitor of the 5-lipoxygenase pathway is Rev-5901, which, however, lacks in invivo efficacy, as it is rapidly metabolized. We investigated the introduction of carboranes as highly hydrophobic and metabolically stable pharmacophores into lipoxygenase inhibitors. Carboranes are icosahedral boron clusters that are remarkably stable and used to increase the metabolic stability of unstable pharmaceutics without changing their biological activity. By introduction of meta-carborane into Rev-5901, the first carborane-based inhibitor of the 5-lipoxygenase pathway was obtained. We report the synthesis and inhibitory and cytotoxic behavior of these compounds toward several melanoma and colon cancer cell lines and their related anticancer mechanisms. | en |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/173013/RS// | |
dc.relation | Deutsche Forschungsgemeinschaft. Grant Numbers: HE 1376/38-1, SFB 1039, SA 2902/2-1 | |
dc.relation | Fonds der Chemischen Industrie | |
dc.relation | European Social Fund | |
dc.relation | Graduate School Leipzig School of Natural Sciences - Building with Molecules and Nano-objects (BuildMoNa) | |
dc.relation | Else Kröner-Fresenius Foundation | |
dc.rights | restrictedAccess | |
dc.source | ChemMedChem | |
dc.subject | Aasthma | |
dc.subject | Cancer | |
dc.subject | Carboranes | |
dc.subject | Inhibitors | |
dc.subject | Lipoxygenase | |
dc.title | CarbORev-5901: The First Carborane-Based Inhibitor of the 5-Lipoxygenase Pathway | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Кухнерт, Роберт; Мијатовић, Сања; Георге, Свен; Хеy-Хаwкинс, Евамарие; Мурганић, Благоје; Стеинхилбер, Диетер; Хофманн, Беттина; Лöннецке, Петер; Сáроси, Менyхáрт-Ботонд; Максимовић-Иванић, Данијела; | |
dc.rights.holder | © 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim | |
dc.citation.issue | 13 | |
dc.citation.volume | 12 | |
dc.identifier.doi | 10.1002/cmdc.201700309 | |
dc.identifier.pmid | 28569429 | |
dc.identifier.scopus | 2-s2.0-85021132429 | |
dc.identifier.wos | 000407431200007 | |
dc.citation.apa | Kuhnert, R., Sárosi, M.-B., George, S., Lönnecke, P., Hofmann, B., Steinhilber, D., Murganic, B., et al. (2017). CarbORev-5901: The First Carborane-Based Inhibitor of the 5-Lipoxygenase Pathway. ChemMedChem, 12(13), 1081–1086. | |
dc.citation.vancouver | Kuhnert R, Sárosi M-B, George S, Lönnecke P, Hofmann B, Steinhilber D, Murganic B, Mijatovic S, Maksimovic-Ivanic D, Hey-Hawkins E. CarbORev-5901: The First Carborane-Based Inhibitor of the 5-Lipoxygenase Pathway. ChemMedChem. 2017;12(13):1081–6. | |
dc.citation.spage | 1081 | |
dc.citation.epage | 1086 | |
dc.type.version | publishedVersion | en |
dc.citation.rank | M21 |