130351-68-7Relevant academic research and scientific papers
2′,3′-Cyclopropanated Nucleoside Dimers
Yannopoulos, Constantin G.,Zhou, Wen-Qiang,Nower, Peter,Peoc'h, Didier,Sanghvi, Yogesh S.,Just, George
, p. 378 - 380 (1997)
Syntheses of three novel conformationally rigid dimers containing cyclopropyl -amide and -sulfonamide functionalities are described. Their incorporation into an oligonucleotide sequence resulted in considerable lowering of the Tm's in binding to their complementary RNA sequences.
Design of Glycosyltransferase Inhibitors: Serine Analogues as Pyrophosphate Surrogates?
Wang, Shuai,Cuesta-Seijo, Jose A.,Striebeck, Alexander,Lafont, Dominique,Palcic, Monica M.,Vidal, Sébastien
, p. 1525 - 1532 (2015)
Mimicking the diphosphate moiety of nucleotide diphosphate sugars with serine analogues provided modest glycosyltransferase inhibitors. The synthetic strategy employed a combination of glycosylation, amide bond formation and azide-alkyne "click" chemistry. Inhibition constants (Ki) in the high micromolar range were obtained with a selection of five galactosyltransferases. Cocrystals of three inhibitors bound at the active site of a blood group A/B synthesizing glycosyltransferase were analysed. The structures and inhibitory patterns of the analogues demonstrate the flexibility of the enzymes which complicates the rational design of glycosyltransferase inhibitors. Moving targets: Nucleotide diphosphate sugar analogues were synthesized through a combination of glycosylation, amide bond formation and azide-alkyne "click" chemistry. High micromolar inhibitors were obtained with a selection of five galactosyltransferases. The structures and inhibitory patterns of the analogues demonstrate the flexibility of the enzymes which complicates the rational design of glycosyltransferase inhibitors.
NUCLEIC ACID-POLYPEPTIDE COMPOSITIONS AND USES THEREOF
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Paragraph 0466, (2019/04/27)
Disclosed herein are compositions and pharmaceutical formulations that comprise a binding moiety conjugated to a modified polynucleic acid molecule and a polymer. Also described herein include methods for treating a cancer which utilize a composition or a pharmaceutical formulation comprising a binding moiety conjugated to a polynucleic acid molecule and a polymer.
Synthesis and in vitro growth inhibitory activity of novel silyl- and trityl-modified nucleosides
Panayides, Jenny-Lee,Mathieu, Véronique,Banuls, Laetitia Moreno Y.,Apostolellis, Helen,Dahan-Farkas, Nurit,Davids, Hajierah,Harmse, Leonie,Rey, M.E. Christine,Green, Ivan R.,Pelly, Stephen C.,Kiss, Robert,Kornienko, Alexander,Van Otterlo, Willem A.L.
, p. 2716 - 2724 (2016/06/08)
Seventeen silyl- and trityl-modified (5′-O- and 3′,5′-di-O-) nucleosides were synthesized with the aim of investigating the in vitro antiproliferative activities of these nucleoside derivatives. A subset of the compounds was evaluated at a fixed concentra
Synthesis and cell transfection properties of cationic uracil-morpholino tetramer
Paul, Sibasish,Pattanayak, Sankha,Sinha, Surajit
supporting information, p. 1072 - 1076 (2014/02/14)
Synthesis and cell transfection properties of guanidinium-functionalized uracil morpholino tetramer have been reported for the first time. Due to the basic nature of guanidinium groups they remain protonated under physiological conditions. Such cationic tetramer exhibits efficient cellular uptake properties as visualized by microscopy imaging using fluorescent dye BODIPY. 7′-End of this morpholino tetramer was functionalized with an azide group for conjugation with various types of biomolecules or drugs for cellular delivery.
Synthesis and cell transfection properties of cationic uracil-morpholino tetramer
Paul, Sibasish,Pattanayak, Sankha,Sinha, Surajit
supporting information, p. 1072 - 1076 (2015/02/05)
Synthesis and cell transfection properties of guanidinium-functionalized uracil morpholino tetramer have been reported for the first time. Due to the basic nature of guanidinium groups they remain protonated under physiological conditions. Such cationic tetramer exhibits efficient cellular uptake properties as visualized by microscopy imaging using fluorescent dye BODIPY. 7′-End of this morpholino tetramer was functionalized with an azide group for conjugation with various types of biomolecules or drugs for cellular delivery.
2',3'-O-phosphonoalkylidene derivatives of ribonucleosides: Synthesis and reactivity
Endova, Magdalena,Masojidkova, Milena,Budesinsky, Milos,Rosenberg, Ivan
, p. 11151 - 11186 (2007/10/03)
A novel type of nucleotide analogues, the 2',3'-O-(1- diethylphosphono)alkylidene derivatives of ribonucleosides was prepared by redox reaction of diethyl chlorophosphite with various nucleoside orthoesters. Some of these compounds undergo interesting rearrangements when treated with nucleophiles. The configuration of the title compounds was determined by 2D-ROESY experiments. Biological activity of partially protected nucleotide analogues is also discussed.
Novel Solid-phase Synthesis of Branched Oligoribonucleotides, including a Substrate for the RNA Debranching Enzyme
Sproat, Brian S.,Beijer, Barbro,Groetli, Morten,Ryder, Ursula,Morand, Kenneth L.,Lamond, Angus I.
, p. 419 - 432 (2007/10/02)
An effective new route for synthesizing branched oligoribionucleotides in the solid phase in the 5' to 3' direction has been developed.This required the synthesis of reversed monomers, viz. protected nucleoside 5'-phosphoramidites bearing 2'-O-Fpmp and 3'
