73502-43-9Relevant articles and documents
Efficient synthesis and antibacterial activities of some novel 1,2,3-triazoles prepared from propargylic alcohols and benzyl azides
Hosseinzadeh, Rahman,Abolfazli, Mohammadreza Khadem,Mohseni, Mojtaba,Mohadjerani, Maryam,Lasemi, Zahra
, p. 1298 - 1305 (2015/04/27)
A simple and effective procedure for regioselective preparation of 1,2,3-triazoles from benzyl azides and propargylic alcohols is described using CuSO4·5H2O and sodium ascorbate. To screen the antibacterial activity of some newly synthesized triazole derivatives, minimum inhibitory concentration of 3d and 3k was evaluated against gram positive Staphylococcus aureus and Bacillus subtilis and gram negative Escherichia coli and Pseudomonas aeruginosa.
Design of pH responsive clickable prodrugs applied to histone deacetylase inhibitors: A new strategy for anticancer therapy
Delatouche, Régis,Denis, Iza,Grinda, Marion,Bahhaj, Fatima El,Baucher, Estelle,Collette, Floraine,Héroguez, Valérie,Grégoire, Marc,Blanquart, Christophe,Bertrand, Philippe
, p. 862 - 872 (2014/01/06)
The aim of this study was to develop clickable prodrugs bearing a tunable pH responsive linker designed for acidic pH-mediated release of histone deacetylase inhibitors. HDACi are an important class of molecules belonging to the epigenetic modulators used for innovative cancer strategies. The behavior of these prodrugs was determined by a bioluminescence resonance energy transfer assay in living tumor cells. This work demonstrated that this innovative type of clickable prodrugs entered cancer cells and showed restored anti proliferative properties attributed to the effective release of the HDAC inhibitors. A correlation between kinetic studies, dose responses, and biological activities was obtained, making such clickable prodrugs good candidates for new strategies in epigenetic-oriented anticancer therapies.
The synthesis and properties of vinyl substituted naphthopyrans and their styrene copolymers
Blackwell, Catherine J.,Gabbutt, Christopher D.,Guthrie, James T.,Heron, B. Mark
experimental part, p. 408 - 420 (2012/08/28)
A comprehensive series of mono-, di- and tri-bromo-3H-naphtho[2,1-b]pyrans was synthesised by the traditional union of a 2-naphthol with an alkynol. The bromine atom(s) in these naphthopyrans was readily replaced by a vinyl group using a Suzuki coupling reaction with vinyl boronic anhydride pyridine complex. The efficiency of the Suzuki vinylation reaction decreases with the increasing number of bromine atoms to be substituted. The vinylnaphthopyrans served as styrene analogues and readily underwent a thermally initiated free radical addition co-polymerisation with styrene to efficiently afford low molecular weight poly(styrene-co-naphthopyrans). The photochromic response of the bromonaphthopyrans and vinylnaphthopyrans followed the established colour-structure relationships for photochromic naphthopyrans. The photochromic response of toluene solutions of the poly(styrene-co-naphthopyrans) was characterised by a hypsochromic shift of the λmax relative to that recorded for the vinylnaphthopyran monomers. Increased half-lives were noted for the copolymers derived from the bis- and tris-vinylnaphthopyrans where some degree of crosslinking was expected. A further hypsochromic shift in λmax resulted for the thin films of the poly(styrene-co- naphthopyrans). Of particular note was the behaviour of the 3-(2-vinylphenyl)-3- phenylnaphthopyran which gave the typical yellow colour of the photomerocyanine coupled with the predictable large half-life. However, all photochromism of this naphthopyran was lost upon polymerisation suggesting that an alternative pathway supervenes in the expected polymerisation sequence.
