29377-71-7Relevant articles and documents
Styrylcyanine-based fluorescent probes with red-emission and large Stokes shift for the detection of viscosity
Cao, Xiangbin,Liu, Jianhui,Hong, Pan,Li, Guanglan,Hao, Ce
, p. 444 - 451 (2017)
Based on the mechanism of intramolecular charge transfer (ICT), two new styrylcyanine dyes, DPA-1 and DPA-2, composed of an electron-rich N-phenylaniline and a cationic benzothiazene connected with ethylene(s) bridge, were designed and synthesized. These two dyes exhibited red-emission (653/607?nm) and simultaneously impressive large Stokes shift (111/92?nm) due to intramolecular charge transfer effect, twisted geometry and extended conjugation system. When their solution viscosity increased from 1.01?cP to 234?cP in the water-glycerol system, the fluorescence intensity of the synthetic dyes was enhanced by 81-fold and 64-fold, respectively. Additionally, a favorable linear relationship between the fluorescence intensity and the environmental viscosity was observed within the above viscosity range for the obtained samples (R2?>?0.99), which led to the establishment of a method for the quantitative determination of the solution viscosity. Such dyes with improved photophysical properties, including emission wavelength and Stokes shift, could be used as promising candidates for intracellular viscosity detection. Moreover, the mechanism of fluorescence emission of the resultant products toward viscosity was further investigated. Of the two probes studies, DPA-1 is better than DPA-2 in terms of emission wavelength, Stokes shift and the sensitivity of the fluorescence intensity to viscosity.
Novel symmetrical ureas as modulators of protein arginine methyl transferases
Fontán, Noelia,García-Domínguez, Patricia,álvarez, Rosana,De Lera, ángel R.
supporting information, p. 2056 - 2067 (2013/05/09)
Methylation of histone arginine residues is an epigenetic mark related to gene expression that is implicated in a variety of biological processes and can be reversed by small-molecule modulators of protein arginine methyltransferases (PRMTs). A series of symmetrical ureas, designed as analogues of the known PRMT1 inhibitor AMI-1 have been synthesized using Pd-catalyzed Ar-N amide bond formation processes or carbonylation reactions as key steps. Their inhibitory profile has been characterized. The enzymatic assays showed a weak effect on PRMT1 and PRMT5 activity for most of the compounds. The acyclic urea that exhibited the strongest effect on the inhibition of the PRMT1 activity also showed the greatest effect on the expression of some androgen receptor target genes (TMPRSS2 and FKBP5), which may be related with its enzymatic activity. Surprisingly, AMI-1 behaved as an activator of PRMT5 activity, a result not reported so far.
Optimization of the central linker of dicationic bis-benzimidazole anti-MRSA and anti-VRE agents
Hu, Laixing,Kully, Maureen L.,Boykin, David W.,Abood, Norman
scheme or table, p. 3374 - 3377 (2010/02/28)
A series of bis-benzimidazole diamidine compounds containing different central linkers has been synthesized and evaluated for in vitro antibacterial activities, including drug-resistant bacterial strains. Seven compounds have shown potent antibacterial activities. The anti-MRSA and anti-VRE activities of compound 1h were more potent than that of the lead compound 1a and vancomycin.