2732-17-4Relevant articles and documents
Synthesis and anti-inflammatory activity of natural and semisynthetic geranyloxycoumarins
Curini, Massimo,Epifano, Francesco,Maltese, Federica,Marcotullio, Maria C.,Tubaro, Aurelia,Altinier, Gianmario,Gonzales, Sylvia Prieto,Rodriguez, Juan C.
, p. 2241 - 2243 (2004)
Nine new 7-geranyloxycoumarin derivatives differently substituted at position 8 were semi-synthesised. Their topical anti-inflammatory activity was evaluated using the Croton oil ear test in mice as a model of acute inflammation. Auraptene (7-geranyloxycoumarin), its 8-methoxy (collinin, 1) and 8-acetoxy derivatives (5) (1μmol/cm2) provoked 50% oedema reduction, similarly to 0.25μmol/cm2 of the reference drug indomethacin, a nonsteroidal anti-inflammatory drug.
Rational Design, Synthesis and Evaluation of Coumarin Derivatives as Protein-protein Interaction Inhibitors
De Luca, Laura,Agharbaoui, Fatima E.,Gitto, Rosaria,Buemi, Maria Rosa,Christ, Frauke,Debyser, Zeger,Ferro, Stefania
, p. 460 - 473 (2016/09/09)
Herein we describe the design and synthesis of a new series of coumarin derivatives searching for novel HIV-1 integrase (IN) allosteric inhibitors. All new obtained compounds were tested in order to evaluate their ability to inhibit the interaction between the HIV-1 IN enzyme and the nuclear protein lens epithelium growth factor LEDGF/p75. A combined approach of docking and molecular dynamic simulations has been applied to clarify the activity of the new compounds. Specifically, the binding free energies by using the method of molecular mechanics-generalized Born surface area (MM-GBSA) was calculated, whereas hydrogen bond occupancies were monitored throughout simulations methods.
Photo-triggered fluorescent theranostic prodrugs as DNA alkylating agents for mechlorethamine release and spatiotemporal monitoring
Cao, Yanting,Pan, Rong,Xuan, Weimin,Wei, Yongyi,Liu, Kejian,Zhou, Jiahong,Wang, Wei
supporting information, p. 6742 - 6748 (2015/06/25)
We describe a new theranostic strategy for selective delivery and spatiotemporal monitoring of mechlorethamine, a DNA alkylating agent. A photo-responsive prodrug is designed and composed of a photolabile o-nitrophenylethyl group, a DNA alkylating mechlor
Synthesis and α-glucosidase inhibitory, DPPH scavenging activity of substituted 2-oxo-2H-chromen-7-yl-dihydrogen phosphate derivatives
Kumar, J. Ashok,Tiwari, Ashok K.,Ali, A.Zehra,Rao, R. Ranga,Raju, B. China
experimental part, p. 1251 - 1257 (2012/01/12)
Series of phosphorylated coumarin derivatives (4a-j) were synthesized by Pechmann condensation, phosphorylation, and debenzylation reactions in very good yields. Thus, synthesized compounds (4a-j) were evaluated for their α-glucosidase and 1,1-diphenyl-2-picrylhydrazyl scavenging activities; few compounds showed moderate to good activity. J. Heterocyclic Chem., 00, 00 (2011). Copyright
Synthesis of hydroxycoumarins and hydroxybenzo[f]- or [h]coumarins as lipid peroxidation inhibitors
Symeonidis, Theodoros,Chamilos, Michael,Hadjipavlou-Litina, Dimitra J.,Kallitsakis, Michael,Litinas, Konstantinos E.
experimental part, p. 1139 - 1142 (2009/08/07)
Substituted hydroxycoumarins and 7- or 8-hydroxybenzo[f]coumarins were prepared by the treatment of phenols and naphthalenediols, respectively, with malic acid and H2SO4 under microwave irradiation. 7- or 8-Hydroxybenzo[f]coumarins and 6-hydroxybenzo[h]coumarin were synthesized by the reaction of naphthalenediols with ethylpropiolate in the presence of ZnCl2 in refluxing dioxane. The compounds were tested in vitro for their ability: (i) to interact with 1,1-diphenyl-2-picryl-hydrazyl (DPPH) stable free radical, (ii) to inhibit lipid peroxidation, (iii) to scavenge the superoxide anion, (iv) to inhibit the activity of soybean lipoxygenase and (v) to inhibit in vivo the carrageenin-induced rat paw edema. Most of them are potent superoxide anion scavengers and inhibit in vitro lipid peroxidation. The majority of the compounds did not show high lipoxygenase inhibitory activity. No differences were observed between biological responses of hydroxycoumarins and hydroxybenzocoumarins. Compound 3i was found to present a promising antioxidant profile.
Design, synthesis, and 3D QSAR of novel potent and selective aromatase inhibitors
Leonetti, Francesco,Favia, Angelo,Rao, Angela,Aliano, Rosaria,Paluszcak, Anja,Hartmann, Rolf W.,Carotti, Angelo
, p. 6792 - 6803 (2007/10/03)
The design, synthesis, and biological evaluation of a series of new aromatase inhibitors bearing an imidazole or triazole ring linked to a fluorene (A), indenodiazine (B), or coumarin scaffold (C) are reported. Properly substituted coumarin derivatives di
A new synthesis of and methylpsoralen utilizing a palladium-copper catalyzed reaction to generate the furan ring and thus allowing for the generation of novel analogs in the 5'-position
Aquila, Brian M.
, p. 2795 - 2798 (2007/10/03)
A rapid synthesis of 1-methylpsoralen is reported that utilizes a palladium-copper catalyzed reaction to generate the furan ring. Since 8-methylpsoralen is considered one of the most photodynamic methylpsoralens known and given the fact that psoralens in general have been shown to have medicinal value against bacteria and viruses, this synthesis allows for the availability to generate new derivatives by supplying a handle in the 5'-position.
