The Experts below are selected from a list of 300 Experts worldwide ranked by ideXlab platform
Larsoliver Klotz - One of the best experts on this subject based on the ideXlab platform.
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1 4 Naphthoquinones from oxidative damage to cellular and inter cellular signaling
Molecules, 2014Co-Authors: Larsoliver Klotz, Claus JacobAbstract:Naphthoquinones may cause oxidative stress in exposed cells and, therefore, affect redox signaling. Here, contributions of redox cycling and alkylating properties of quinones (both natural and synthetic, such as plumbagin, juglone, lawsone, menadione, methoxy-Naphthoquinones, and others) to cellular and inter-cellular signaling processes are discussed: (i) naphthoquinone-induced Nrf2-dependent modulation of gene expression and its potentially beneficial outcome; (ii) the modulation of receptor tyrosine kinases, such as the epidermal growth factor receptor by Naphthoquinones, resulting in altered gap junctional intercellular communication. Generation of reactive oxygen species and modulation of redox signaling are properties of Naphthoquinones that render them interesting leads for the development of novel compounds of potential use in various therapeutic settings.
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1 4 Naphthoquinones as inducers of oxidative damage and stress signaling in hacat human keratinocytes
Archives of Biochemistry and Biophysics, 2010Co-Authors: Viola Klaus, Tobias Hartmann, Juan Gambini, Peter Graf, Wilhelm Stahl, A Hartwig, Larsoliver KlotzAbstract:Abstract Selected biological effects of 1,4-naphthoquinone, menadione (2-methyl-1,4-naphthoquinone) and structurally related quinones from natural sources – the 5-hydroxy-Naphthoquinones juglone, plumbagin and the 2-hydroxy-Naphthoquinones lawsone and lapachol – were studied in human keratinocytes (HaCaT). 1,4-naphthoquinone and menadione as well as juglone and plumbagin were highly cytotoxic, strongly induced reactive oxygen species (ROS) formation and depleted cellular glutathione. Moreover, they induced oxidative DNA base damage and accumulation of DNA strand breaks, as demonstrated in an alkaline DNA unwinding assay. Neither lawsone nor lapachol (up to 100 μM) were active in any of these assays. Cytotoxic and oxidative action was paralleled by stimulation of stress signaling: all tested quinones except lawsone and lapachol strongly induced phosphorylation of the epidermal growth factor receptor (EGFR) and the related ErbB2 receptor tyrosine kinase. EGFR activation by plumbagin, juglone and menadione was attenuated by a superoxide dismutase mimetic, indicating that ROS-related mechanisms contribute to EGFR activation by these Naphthoquinones.
Dongxuan Ni - One of the best experts on this subject based on the ideXlab platform.
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synthesis and anti proliferative activity evaluation of novel 1 4 Naphthoquinones possessing pyrido 2 3 d pyrimidine scaffolds
RSC Advances, 2016Co-Authors: Chong Zhang, Qiujv Peng, Dongxuan NiAbstract:A series of novel 1,4-Naphthoquinones possessing pyrido[2,3-d]pyrimidine scaffolds were synthesized in very good yields using one-pot condensation of 2-hydroxy-1,4-naphthoquinone, aldehydes, and 2-substituted 4,6-diaminopyrimidine. The in vitro anti-proliferative activity of these novel compounds was evaluated in SGC7901 and HepG2 cell lines. Almost all the tested compounds showed manifested potent inhibitory activity against the two tested cancer cell lines.
Liqiang Wu - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of novel 1 2 Naphthoquinones possessing tetrazolo 1 5 a pyrimidine scaffolds as potent antitumor agents
RSC Advances, 2015Co-Authors: Liqiang WuAbstract:A series of novel 1,2-Naphthoquinones possessing tetrazolo[1,5-a]pyrimidine scaffolds were synthesized in very good yields using one-pot condensation of 2-hydroxy-1,4-naphthoquinone, aldehydes, and 5-aminotetrazole. All the synthesized compounds were evaluated for their antitumor activity in vitro against HCT116 (human colon cancer) and HepG2 (human hepatoma) cell lines. Among the screened compounds, 4o, 4k, 4g, 4q, and 4s showed significant inhibitory activity against the two human cell lines.
Aurelio G Csaky - One of the best experts on this subject based on the ideXlab platform.
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In vitro antiamyloidogenic properties of 1,4-Naphthoquinones.
Biochemical and Biophysical Research Communications, 2010Co-Authors: Paloma Bermejo-bescós, Maria Teresa Molina, Sagrario Martín-aragón, Karim L. Jiménez-aliaga, Andrea Ortega, Eduardo Buxaderas, Guillermo Orellana, Aurelio G CsakyAbstract:Abstract The aim of this study is to find out whether several 1,4-Naphthoquinones (1,4-NQ) can interact with the amyloidogenic pathway of the amyloid precursor protein processing, particularly targeting at β-secretase (BACE), as well as at β-amyloid peptide (Aβ) aggregation and disaggregating preformed Aβ fibrils. Compounds bearing hydroxyl groups at the quinoid (2) or benzenoid rings (5, 6) as well as some 2- and 3-aryl derivatives (11–15) showed BACE inhibitory activity, without effect on amyloid aggregation or disaggregation. The halogenated compounds 8 and 10 were selective for the inhibition of amyloid aggregation. On the other hand, 1,4-naphthoquinone (1), 6-hydroxy-1,4-naphthoquinone (4) and 2-(3,4-dichlorophenyl)-1,4-naphthoquinone (26) did not show any BACE inhibitory activity but were active on amyloid aggregation and disaggregation preformed Aβ fibrils. Juglone (5-hydroxy-1,4-naphthoquinone (3), and 3-(p-hydroxyphenyl)-5-methoxy-1,4-napththoquinone (19) were active on all the three targets. Therefore, we suggest that 1,4-NQ derivatives, specially 3 and 19, should be explored as possible drug candidates or lead compounds for the development of drugs to prevent amyloid aggregation and neurotoxicity in Alzheimer’s disease.
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n heterocyclic carbene catalyzed monoacylation of 1 4 Naphthoquinones with aldehydes
Journal of Organic Chemistry, 2009Co-Authors: Maria Teresa Molina, Cristina Navarro, Ana Moreno, Aurelio G CsakyAbstract:The NHC-catalyzed conjugate hydroacylation of 1,4-Naphthoquinones allows for the synthesis of monoacylated 1,4-dihydroxynaphthalene derivatives. These targets, difficult to prepare selectively by standard protocols, represent important intermediates in the elaboration of highly substituted 1,4-naphthoquinone derivatives, which constitute relevant pharmaceutical scaffolds. High regioselectivity has been observed in the hydroacylation reaction when starting from nonsymmetrical quinones.
Kevin W Wellington - One of the best experts on this subject based on the ideXlab platform.
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understanding cancer and the anticancer activities of Naphthoquinones a review
RSC Advances, 2015Co-Authors: Kevin W WellingtonAbstract:The non-communicable disease, cancer, is one of the major causes of death across the world and is forecast to increase by 75% to reach close to 25 million cases over the next two decades. Radiotherapy and surgical approaches have been unsuccessful in controlling the incidence of most cancers. The development of chemotherapeutic strategies involving novel small molecule antitumour agents has therefore been the focus area of cancer chemotherapy for several decades as another strategy to combat and control the incidence of cancer. Many natural products as well as several synthetic drugs have a naphthoquinone chromophore. The anticancer activities of Naphthoquinones have been the focus of much research to discover novel anticancer agents. The naturally occurring 1,2-naphthoquinone-based compound, β-lapachone (ARQ 761), is currently being assessed for its anti-tumour activity against advanced solid tumours. This review describes the most recent applications of Naphthoquinones and their derivatives in cancer drug discovery. The biology relevant to the design of novel naphthoquinone anticancer agents is also discussed. Furthermore, the discussion of the biology will contribute to understanding cancer as well as the applications of Naphthoquinones as anticancer agents.
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Understanding cancer and the anticancer activities of Naphthoquinones – a review
RSC Advances, 2015Co-Authors: Kevin W WellingtonAbstract:The non-communicable disease, cancer, is one of the major causes of death across the world and is forecast to increase by 75% to reach close to 25 million cases over the next two decades. Radiotherapy and surgical approaches have been unsuccessful in controlling the incidence of most cancers. The development of chemotherapeutic strategies involving novel small molecule antitumour agents has therefore been the focus area of cancer chemotherapy for several decades as another strategy to combat and control the incidence of cancer. Many natural products as well as several synthetic drugs have a naphthoquinone chromophore. The anticancer activities of Naphthoquinones have been the focus of much research to discover novel anticancer agents. The naturally occurring 1,2-naphthoquinone-based compound, β-lapachone (ARQ 761), is currently being assessed for its anti-tumour activity against advanced solid tumours. This review describes the most recent applications of Naphthoquinones and their derivatives in cancer drug discovery. The biology relevant to the design of novel naphthoquinone anticancer agents is also discussed. Furthermore, the discussion of the biology will contribute to understanding cancer as well as the applications of Naphthoquinones as anticancer agents.
