701-72-4Relevant articles and documents
Palladium-Catalyzed Annulation of Aryltriazoles and Arylisoxazoles with Alkynes
Yuan, Hairui,Wang, Min,Xu, Zhenghu,Gao, Hongyin
, p. 4386 - 4392 (2019/08/12)
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.).
UGT74B1 from Arabidopsis thaliana as a versatile biocatalyst for the synthesis of 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
, p. 6252 - 6261 (2016/07/11)
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.
Synthesis and biochemical evaluation of δ2-isoxazoline derivatives as DNA methyltransferase 1 inhibitors
Castellano, Sabrina,Kuck, Dirk,Viviano, Monica,Yoo, Jakyung,López-Vallejo, Fabian,Conti, Paola,Tamborini, Lucia,Pinto, Andrea,Medina-Franco, José L.,Sbardella, Gianluca
, p. 7663 - 7677 (2011/12/21)
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.