640766-67-2Relevant academic research and scientific papers
Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop
Bueno, Oskia,Gargantilla, Marta,Estévez-Gallego, Juan,Martins, Solange,Díaz, J. Fernando,Camarasa, María-José,Liekens, Sandra,Pérez-Pérez, María-Jesús,Priego, Eva-María
, p. 195 - 208 (2019/03/28)
Microtubule targeting agents represent a very active arena in the development of anticancer agents. In particular, compounds binding at the colchicine site in tubulin are being deeply studied, and the structural information recently available on this binding site allows structure-directed design of new ligands. Structural comparison of our recently reported high resolution X-Ray structure of the cyclohexanedione derivative TUB075 bound to tubulin and the tubulin-DAMA-colchicine complex has revealed a conformational change in the αT5 loop. By a grid-based computational analysis of the tubulin-DAMA-colchicine binding site, we have identified a new favourable binding area in the colchicine-site that was unexplored by our lead TUB075. Thus, based on a structure-guided design, new cyclohexanedione derivatives have been synthesized and tested for tubulin binding and in cellular assays. As a result, we have identified diphenyl ether derivatives with IC50 values around 10–40 nM against three different tumor cell lines and affinity constants for tubulin similar to that of colchicine around 107 M?1. As expected, they halted the cell cycle progression at G2/M phase at concentrations as low as 0.08 μM.
COMPOUND AND ORGANIC ELECTRONIC DEVICE COMPRISING THE SAME
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, (2018/02/08)
An embodiment of the present invention relates to a compound represented by a chemical formula 1 and an organic electronic device including the same. In the chemical formula 1, R1 to R7 are the same as or different from and are individually and independently hydrogen; heavy hydrogen; a halogen group; a nitrile group; a nitro group; a hydroxy group; a carbonyl group; an ester group; an imide; an amide group; a substituted or unsubstituted alkoxy group; a substituted or unsubstituted alkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted alkenyl group; a substituted or unsubstituted silyl group; a substituted or unsubstituted boron group; a substituted or unsubstituted phosphine oxide group; a substituted or unsubstituted amine group; a substituted or unsubstituted arylamine group; a substituted or unsubstituted aryl group; or a substituted or unsubstituted heteroaryl group. The compound enables the organic electronic device to obtain high efficiency and high color purity.COPYRIGHT KIPO 2017
Synthesis of tetrasubstituted alkenes through a palladium-catalyzed domino carbopalladation/C-H-activation reaction
Tietze, Lutz F.,Hungerland, Tim,Duefert, Alexander,Objartel, Ina,Stalke, Dietmar
, p. 3286 - 3291 (2012/04/17)
Helical tetrasubstituted alkenes (7) were obtained in a highly efficient way through a palladium-catalyzed domino-carbopalladation/CH-activation reaction of propargylic alcohols 6 in good to excellent yields. Electron-withdrawing- and electron-donating substituents can be introduced onto the upper and lower aromatic rings. The substrates (6) for the domino process were synthesized by addition of the lithiated alkyne (20) to various aldehydes (19); moreover, the substrates were accessible enantioselectively (in 95 % ee) by reduction of the corresponding ketone using the Noyori procedure. Copyright
