22924-19-2Relevant academic research and scientific papers
2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease
Mezeiova, Eva,Janockova, Jana,Andrys, Rudolf,Soukup, Ondrej,Kobrlova, Tereza,Muckova, Lubica,Pejchal, Jaroslav,Simunkova, Miriama,Handl, Jiri,Micankova, Petra,Capek, Jan,Rousar, Tomas,Hrabinova, Martina,Nepovimova, Eugenie,Marco-Contelles, Jose Luis,Valko, Marian,Korabecny, Jan
, (2021)
Alzheimer's disease is a progressive brain disorder with characteristic symptoms and several pathological hallmarks. The concept of “one drug, one target” has not generated any new drugs since 2004. The new era of drug development in the field of AD build
Novel juglone and plumbagin 5-O derivatives and their in vitro growth inhibitory activity against apoptosis-resistant cancer cells
Fiorito, Serena,Genovese, Salvatore,Taddeo, Vito Alessandro,Mathieu, Véronique,Kiss, Robert,Epifano, Francesco
supporting information, p. 334 - 337 (2016/01/09)
Juglone 1 an plumbagin 2 are plant secondary metabolites nowadays well known for their anticancer properties. In this study we synthesized analogues of 1 and 2 deriving from the functionalization of the OH group in position 5 with different side chains in form of esters and ethers. Therefore the growth inhibitory activities of these adducts were evaluated in vitro on six cancer cell lines using the MTT colorimetric assays along with the two natural parent compounds. The data revealed that these latter displayed the strongest growth inhibitory activities in vitro. Quantitative videomicroscopy analyses were then carried out on human U373 glioblastoma cells, which are characterized by various level of resistance to pro-apoptotic stimuli. We compared the naturally occurring reference compounds 1 and 2 with the derivatives exerting the best activities in terms of IC50 growth inhibitory values. These analyses showed that both juglone and plumbagin had a cytostatic effect on U373 cells and were able to overcome the intrinsic resistance of U373 cancer cells to pro-apoptotic stimuli.
Solar photochemistry: Optimisation of the photo Friedel-Crafts acylation of naphthoquinones
Mitchell, Lorna J.,Lewis, William,Moody, Christopher J.
supporting information, p. 2830 - 2842 (2013/10/08)
A practical and robust photo Friedel-Crafts acylation of naphthoquinones is described. Although the reaction proceeds slowly in sunlight, the optimised conditions offer a substantial improvement to those already reported, by the utilisation of a more reliable and practical 'sun-mimicking' light source, a less hazardous solvent system (trifluorotoluene) and faster reaction times. Using these conditions, the reaction scope has been expanded to include functionalised aldehyde and naphthoquinone substrates, affording the desired photo-products in acceptable to excellent yields (17-81%). Factors influencing the regiochemistry of the photo Friedel-Crafts reaction on unsymmetrical naphthoquinones have also been investigated.
