214783-17-2Relevant articles and documents
The development of a versatile trifunctional scaffold for biological applications
Vaněk, Václav,Pícha, Jan,Fabre, Benjamin,Budě?ínsky, Milo?,Lep?ík, Martin,Jirá?ek, Ji?í
, p. 3689 - 3701 (2015)
We describe the synthesis of a trifunctional scaffold constructed from a planar core of trimesic acid derivatized with three propargylamine moieties. The scaffold was attached to a solid-phase resin through the carboxylic group of a fluorinated alkyl spacer arm. The orthogonal protection of two of the alkyne groups with triethylsilyl and triisopropylsilyl moieties enabled modular and efficient derivatization of the scaffold with three different azides by using solid-phase synthesis on amphiphilic ChemMatrix resin. We showed that a fluorine label can be used to quantify the content of fluorine-containing compounds by 19F NMR spectroscopic analysis after cleavage from the resin. We have thus designed a versatile and convenient tool that could be useful for simple and rapid solid-phase syntheses of combinatorial libraries of the scaffold-based compounds, for example as new protein binders. The development of a trifunctional scaffold derivatized with three orthogonally protected alkyne moieties that is useful for the solid-phase synthesis of combinatorial libraries is described.
Synthesis of 1,2,3-triazole benzophenone derivatives and evaluation of in vitro sun protection, antioxidant properties, and antiproliferative activity on HT-144 melanoma cells
Dias, Maria C.F.,de Sousa, Bianca L.,Ionta, Marisa,Teixeira, Róbson R.,Goulart, Thiago Q.,Ferreira-Silva, Guilherme á.,Pilau, Eduardo J.,dos Santos, Marcelo H.
, p. 572 - 587 (2021/02/12)
Benzophenones display several biological activities, including antioxidant, anticancer, and photoprotective. Furthermore, antioxidants can minimize both ultraviolet absorption and tumor development. In the present investigation, a series of twenty-six 1,2
A caffeic acid-ferulic acid hybrid compound attenuates lipopolysaccharide-mediated inflammation in BV2 and RAW264.7 cells
Kwon, Mi-Youn,Kim, Sang-Min,Park, Jiwon,Lee, JuWon,Cho, Hyeongjin,Lee, Haneul,Jeon, Cheolmin,Park, Jeong-Ho,Han, Inn-Oc
, p. 565 - 571 (2019/06/27)
In the present study, we synthesized and evaluated the anti-inflammatory effects of the two component hybrids, caffeic acid (CA)-ferulic acid (FA), FA-Tryptamine (Trm), CA-Piperonyl Triazol (PT) and FA-PT. Of these five hybrids, CA-FA had the most potent
Selective synthesis of mono- and di-methylated amines using methanol and sodium azide as C1 and N1 sources
Chakrabarti, Kaushik,Mishra, Anju,Panja, Dibyajyoti,Paul, Bhaskar,Kundu, Sabuj
supporting information, p. 3339 - 3345 (2018/07/29)
A Ru(ii) complex mediated synthesis of various N,N-dimethyl and N-monomethyl amines from organic azides using methanol as a methylating agent is reported. This methodology was successfully applied for a one-pot reaction of bromide derivatives and sodium azide in methanol. Notably, by controlling the reaction time several N-monomethylated and N,N-dimethylated amines were synthesized selectively. The practical applicability of this tandem process was revealed by preparative scale reactions with different organic azides and synthesis of an anti-vertigo drug betahistine. Several kinetic experiments and DFT studies were carried out to understand the mechanism of this transformation.