72585-17-2Relevant academic research and scientific papers
4,5-Diaryl 3(2H)Furanones: Anti-inflammatory activity and influence on cancer growth
Semenok, Dmitrii,Medvedev, Jury,Giassafaki, Lefki-P.,Lavdas, Iason,Vizirianakis, Ioannis S.,Eleftheriou, Phaedra,Gavalas, Antonis,Petrou, Anthi,Geronikaki, Athina
, (2019/05/24)
Apart from their anti-inflammatory action, COX inhibitors have gathered the interest of many scientists due to their potential use for the treatment and prevention of cancer. It has been shown that cyclooxygenase inhibitors restrict cancer cell growth and are able to interact with known antitumor drugs, enhancing their in vitro and in vivo cytotoxicity. The permutation of hydrophilic and hydrophobic aryl groups in COX inhibitors leads to cardinal changes in the biological activity of the compounds. In the present study, thirteen heterocyclic coxib-like 4,5-diarylfuran-3(2H)-ones and their annelated derivatives-phenanthro[9,10-b]furan-3-ones-were synthesized and studied for anti-inflammatory and COX-1/2 inhibitory action and for their cytotoxic activity on the breast cancer (MCF-7) and squamous cell carcinoma (HSC-3) cell lines. The F-derivative of the -SOMe substituted furan-3(2H)-ones exhibited the best activity (COX-1 IC50 = 2.8 μM, anti-inflammatory activity (by carrageenan paw edema model) of 54% (dose 0.01 mmol/kg), and MCF-7 and HSC-3 cytotoxicity with IC50 values of 10 μM and 7.5 μM, respectively). A cytotoxic effect related to the COX-1 inhibitory action was observed and a synergistic effect with the anti-neoplastic drugs gefitinib and 5-fluorouracil was found. A phenanthrene derivative exhibited the best synergistic effect with gefitinib.
Synthesis and biological properties of aryl methyl sulfones
Navarro, Lorena,Rosell, Gloria,Sánchez, Silvia,Boixareu, Núria,Pors, Klaus,Pouplana, Ramon,Campanera, Josep M.,Pujol, M. Dolors
, p. 4113 - 4126 (2018/07/06)
A novel group of aryl methyl sulfones based on nonsteroidal anti-inflammatory compounds exhibiting a methyl sulfone instead of the acetic or propionic acid group was designed, synthesized and evaluated in vitro for inhibition against the human cyclooxygenase of COX-1 and COX-2 isoenzymes and in vivo for anti-inflammatory activity using the carrageenan induced rat paw edema model in rats. Also, in vitro chemosensitivity and in vivo analgesic and intestinal side effects were determined for defining the therapeutic and safety profile. Molecular modeling assisted the design of compounds and the interpretation of the experimental results. Biological assay results showed that methyl sulfone compounds 2 and 7 were the most potent COX inhibitors of this series and best than the corresponding carboxylic acids (methyl sulfone 2: IC50 COX-1 = 0.04 and COX-2 = 0.10 μM, and naproxen: IC50 COX-1 = 11.3 and COX-2 = 3.36 μM). Interestingly, the inhibitory activity of compound 2 represents a significant improvement compared to that of the parent carboxylic compound, naproxen. Further support to the results were gained by the docking studies which suggested the ability of compound 2 and 7 to bind into COX enzyme with low binding free energies. The improvement of the activity of some sulfones compared to the carboxylic analogues would be performed through a change of the binding mode or mechanism compared to the standard binding mode displayed by ibuprofen, as disclosed by molecular modeling studies. So, this study paves the way for further attention in investigating the participation of these new compounds in the pain inhibitory mechanisms. The most promising compounds 2 and 7 possess a therapeutical profile that enables their chemical scaffolds to be utilized for development of new NSAIDs.
MERCAPTO-BENZOPHENONE COMPOUNDS, COMPOSITIONS AND PREPARATION METHODS THEREOF
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Paragraph 0047, (2014/06/24)
The present invention provides a photocurable composition prepared using mercapto benzophenone compounds as key raw materials. The present invention aims to solve the problems existing in the prior photo-curing technology that low-molecular photoinitiator
Mercapto Benzophenone Compounds, Compositions and Preparation Method Thereof
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Paragraph 0080; 0081, (2013/06/27)
The present invention provides a photocurable composition prepared using mercapto benzophenone compounds as key raw materials. The present invention aims to solve the problems existing in the prior photo-curing technology that low-molecular photoinitiator
MoO2Cl2 as a novel catalyst for Friedel-Crafts acylation and sulfonylation
de Noronha, Rita G.,Fernandes, Ana C.,Rom?o, Carlos C.
experimental part, p. 1407 - 1410 (2009/06/18)
The use of MoO2Cl2 as a novel catalyst for Friedel-Crafts acylation and sulfonylation is described. A series of aromatic ketones and sulfones were prepared in moderate to good yields using acyl chloride or sulfonyl chloride in the presence of MoO2Cl2 (20 mol %), under solvent-free conditions.
1,2-diarylmethylene derivatives, their methods of preparation and their uses in therapeutics
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, (2008/06/13)
The present invention relates to the derivatives of formula: STR1 and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.
Diarylmethylidenefuran derivatives and their uses in therapeutics
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, (2008/06/13)
The present invention relates to the derivatives of the formula STR1 and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.
1,2 diarylmethylene derivatives, their methods of preparation and their uses in therapeutics
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, (2008/06/13)
The present invention relates to the derivatives of formula: STR1 and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.
