211617-72-0Relevant academic research and scientific papers
METABOLICALLY ROBUST ANALOGS OF CYP-EICOSANOIDS FOR THE TREATMENT OF CARDIAC DISEASE
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, (2017/02/09)
The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs).The present invention further relates to composi
ANALOGS OF CYP-EICOSANOIDS FOR USE IN TREATING OR PREVENTING A DISORDER ASSOCIATED WITH NEOVASCULARIZATION AND/OR INFLAMMATION
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, (2017/10/31)
The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs) for use in treating or reducing the risk of deve
Synthesis and preliminary evaluation of pro-RNA 2′- O -masked with biolabile pivaloyloxymethyl groups in an RNA interference assay
Lavergne, Thomas,Baraguey, Carine,Dupouy, Christelle,Parey, Nora,Wuensche, Winfried,Sczakiel, Georg,Vasseur, Jean-Jacques,Debart, Francoise
scheme or table, p. 5719 - 5731 (2011/09/30)
The cellular delivery of bioactive nucleic acid-based drugs such as small interfering RNA (siRNA) represents a major technical hurdle for their pharmaceutical application. Prodrug-like approaches provide an attractive concept to address the delivery probl
Kinetics of self-immolation: Faster signal relay over a longer linear distance?
Lee, Ho Yong,Jiang, Xuan,Lee, Dongwhan
supporting information; experimental part, p. 2065 - 2068 (2009/10/10)
A counterintuitive observation of a faster signal relay over a longer linear distance prompted detailed kinetic studies of self-immolation reactions. With appropriate conformational bias, trigger-to-reporter signal transduction can take an efficient "shor
Novel fluoride-labile nucleobase-protecting groups for the synthesis of 3'(2')-O-aminoacylated RNA sequences
Stutz, Alfred,Hoebartner, Claudia,Pitsch, Stefan
, p. 2477 - 2503 (2007/10/03)
With the aim to develop a general approach to a total synthesis of aminoacylated t-RNAs and analogues, we describe the synthesis of stabilized, aminoacylated RNA fragments, which, upon ligation, could lead to aminoacylated t-RNA structures. Novel RNA phosphoramidites with fluoride-labile 2'-O-[(triisopropylsilyl)-oxy]methyl (=tom) sugar-protecting and N-{{2-[(triisopropylsilyl)oxy]benzyl}oxy}carbonyl (=tboc) base-protecting groups were prepared (Schemes 4 and 5), as well as a solid support containing an immobilized N6-tboc-protected adenosine with an orthogonal (photolabile) 2'-O-[(S)-1-(2-nitrophenyl)ethoxy]methyl (=(S)-npeom) group (Scheme 6). From these building blocks, a hexameric oligoribonucleotide was prepared by automated synthesis under standard conditions (Scheme 7). After the detachment from the solid support, the resulting fully protected sequence 34 was aminoacylated with L-phenylalanine derivatives carrying photolabile N-protecting groups (→42 and 43; Scheme 9). Upon removal of the fluoride-labile sugar- and nucleobase-protecting groups, the still stabilized, partially with the photolabile group protected precursors 44 and 45, respectively, of an aminoacylated RNA sequence were obtained (Scheme 9 and Fig. 3). Photolysis of 45 under mild conditions resulted in the efficient formation of the 3'(2')-O-aminoacylated RNA sequence 46 (Fig. 4). Additionally, we carried out model investigations concerning the stability of ester bonds of aminoacylated ribonucleotide derivatives under acidic conditions (Table) and established conditions for the purification and handling of 3'(2')-O-aminoacylated RNA sequences and their stabilized precursors.
A novel, highly efficient and selective desilylating method for trialkylsilyl ethers
Lee, Adam Shih-Yuan,Yeh, Hsiu-Chih,Shie, Jiun-Jie
, p. 5249 - 5252 (2007/10/03)
A series of tert-butyldimethylsilyl, tert-butyldiphenylsilyl and triisopropylsilyl ethers are hydrolyzed to theirs corresponding alcohols in CBr4 / CH3OH (0.1 eq. / 10mL) reaction system under refluxing condition. The chemoselectivity can be achieved between primary and secondary triisopropylsilyl ethers when more hindered 2-propanol is used instead of methanol.
