89047-46-1Relevant academic research and scientific papers
Non-symmetric substituted ureas locked in an (E,Z) conformation: An unusual anion binding via supramolecular assembly
Olivari, Martina,Caltagirone, Claudia,Garau, Alessandra,Isaia, Francesco,Light, Mark E.,Lippolis, Vito,Montis, Riccardo,Scorciapino, Mariano Andrea
, p. 663 - 669 (2013)
Two new asymmetric ureidic receptors L1 (1-(1H-indol-7-yl)-3- (quinolin-2-yl)urea) and L2 (1-(quinolin-2-yl)-3-(quinolin-8-yl)urea) have been synthesised and their affinity towards different anions tested in DMSO-d6. L1 adopts both in solution and in the solid state an (E,Z) conformation. A moderate affinity for acetate has been observed for L1 while no interaction has been observed for L2. The different behaviour has been ascribed to the presence/absence of the indole group. In the case of L1 the indole group causes the formation of a peculiar supramolecular architecture with two molecules of the receptor binding the anions in the (E,Z) conformation via H-bonds. L2 also adopts an (E,Z) conformation in the solid state. However, the absence of the indole group in L2 hampers the formation of the supramolecular assembly with the participation of anionic species.
Azine-imidazole aza-BODIPY analogues with large Stokes shift
Bukowska, Patrycja,Piechowska, Joanna,Loska, Rafa?
, p. 312 - 321 (2016/11/21)
A series of azine-imidazole aza-BODIPY analogues has been prepared by a simple synthesis from 2-azinecarboxylic acids and imidazole N-oxides. The new fluorescent complexes exhibit large Stokes shifts (up to 10?000?cm?1), fluorescence in crystal
Novel optimization of valmerins (tetrahydropyrido[1,2- a ]isoindolones) as potent dual CDK5/GSK3 inhibitors
Ouach, Aziz,Boulahjar, Rajaa,Vala, Christine,Bourg, Stéphane,Bonnet, Pascal,Guguen-Guillouzo, Christiane,Ravache, Myriam,Le Guevel, Rémy,Lozach, Olivier,Lazar, Sa?d,Troin, Yves,Meijer, Laurent,Ruchaud, Sandrine,Akssira, Mohamed,Guillaumet, Gérald,Routier, Sylvain
, p. 311 - 325 (2016/04/05)
An efficient synthetic strategy able to modulate the structure of the tetrahydropyridine isoindolone (Valmerin) skeleton was developed. A library of more than 30 novel final structures was generated. Biological activities on CDK5 and GSK3 as well as cellular effects on cancer cell lines were measured for each novel compound. Additionally to support the SAR, a docking study was performed. A potent GSK3/CDK5 dual inhibitor (37, IC50 CDK5/GSK3 35/7 nM) was obtained. Best antiproliferative effects were obtained on lung and prostate cell lines with IC50 Combining double low line 20 nM.
