- Palladium-Catalyzed Annulation of Aryltriazoles and Arylisoxazoles with Alkynes
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We developed herein a palladium-catalyzed annulation of aryltriazoles and arylisoxazoles with internal alkynes via C?H bond activation process. 4,5-disubstituted-3H-naphtho[1,2-d][1,2,3]triazoles and 4,5-disubstituted-naphtho[2,1-d]isoxazoles could be afforded in good yields, respectively. The starting materials are readily available and the scope and applications of this transformation were explored. The reaction offers a practical approach to naphthalene fused heterocycles. (Figure presented.).
- Yuan, Hairui,Wang, Min,Xu, Zhenghu,Gao, Hongyin
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p. 4386 - 4392
(2019/08/12)
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- IMIDAZOPYRROLOPYRIDINE AS INHIBITORS OF THE JAK FAMILY OF KINASES
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2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
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- UGT74B1 from Arabidopsis thaliana as a versatile biocatalyst for the synthesis of desulfoglycosinolates
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Thioglycosides, even if rare in Nature, have gained increased interest for their biological properties. Chemical syntheses of this class of compounds have been largely studied but little has been reported on their biosynthesis. Herein, combining experiments from the different fields of enzymology, bioorganic chemistry and molecular modeling, we wish to demonstrate the versatility of the glucosyltransferase UGT74B1 and its synthetic potency for the preparation of a variety of natural and unnatural desulfoglycosinolates.
- Marroun, Sami,Montaut, Sabine,Marquès, Stéphanie,Lafite, Pierre,Coadou, Ga?l,Rollin, Patrick,Jousset, Guillaume,Schuler, Marie,Tatibou?t, Arnaud,Oulyadi, Hassan,Daniellou, Richard
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p. 6252 - 6261
(2016/07/11)
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- Synthesis and anti-inflammatory activity of aromatic glucosinolates
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Aromatic GLs are important members of the glucosinolate family of compounds because of their potential biological activity and medicinal properties. This study has shown success in the high yielding synthesis of some important aromatic GLs as well as the results of testing for anti-inflammatory properties of the synthetic GLs. 3,4-Dimethoxyphenylglucosinolate was found to be the most active anti-inflammatory of the seven glucosinolates assayed.
- Vo, Quan V.,Trenerry, Craige,Rochfort, Simone,Wadeson, Jenny,Leyton, Carolina,Hughes, Andrew B.
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p. 5945 - 5954
(2013/09/23)
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- Synthesis and biochemical evaluation of δ2-isoxazoline derivatives as DNA methyltransferase 1 inhibitors
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A series of Δ2-isoxazoline constrained analogues of procaine/procainamide (7a-k and 8a-k) were prepared and their inhibitory activity against DNA methyltransferase 1 (DNMT1) was tested. Among them, derivative 7b is far more potent in vitro (IC50 = 150 μM) than other non-nucleoside inhibitors and also exhibits a strong and dose-dependent antiproliferative effect against HCT116 human colon carcinoma cells. The binding mode of 7b with the enzyme was also investigated by means of a simple competition assay as well as of docking simulations conducted using the recently published crystallographic structure of human DNMT1. On the basis of the findings, we assessed that the mode of inhibition of 7b is consistent with a competition with the cofactor and propose it as a novel lead compound for the development of non-nucleoside DNMT inhibitors.
- Castellano, Sabrina,Kuck, Dirk,Viviano, Monica,Yoo, Jakyung,López-Vallejo, Fabian,Conti, Paola,Tamborini, Lucia,Pinto, Andrea,Medina-Franco, José L.,Sbardella, Gianluca
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p. 7663 - 7677
(2011/12/21)
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- A simple O-sulfated thiohydroximate molecule to be the first micromolar range myrosinase inhibitor
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New non-hydrolyzable analogues of glucosinolates have been prepared. Myrosinase inhibition was observed with modified aglycon moieties, even bulky phenothiazine analogue 6 gave reasonable inhibition. The simplest structure 8 derived from dimethylaminoethanethiol has shown to be the most potent inhibitor with an IC50 of 3.32 μM.
- Cerniauskaite, Deimante,Gallienne, Estelle,Karciauskaite, Henreta,Farinha, Andrea S.F.,Rousseau, Jolanta,Armand, Sylvie,Tatibou?t, Arnaud,Sackus, Algirdas,Rollin, Patrick
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scheme or table
p. 3302 - 3305
(2009/08/09)
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- ACTION DU CHLORURE D'ACETYLE ET DE L'ANHYDRIDE ACETIQUE SUR LE NITRONATE DE LITHIUM DERIVE DU PHENYL-2 NITROETHANE. REACTIVITE ELECTROPHILE OU DIPOLAIRE, EN FONCTION DU MILIEU, DE L'OXYDE DE NITRILE INTERMEDIAIREMENT FORME
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The lithium nitronate salt derived from 2-phenyl nitroethane reacts with acetic anhydride and with acetyl chloride to give an intermediate nitrile oxide.Depending on the protonating character of the medium, this latter can react either as a 1,3 dipole to give the furoxan or, in the presence of a dipolarophile, the corresponding adduct; or as an electrophile leading to the chlorooxime or to derivatives of benzohydroxamic acid.The formation of the nitrile oxide, by loss of acetic acid from a nitronic-acetic mixed anhydride, appears to be the most plausible reaction pathway accounting for the above observations.
- Cherest, M.,Lusinchi, X
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p. 3825 - 3840
(2007/10/02)
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