309947-86-2Relevant articles and documents
Synthesis of Rigid Rod, Trigonal, and Tetrahedral Nucleobase-Terminated Molecules
Jin, Xiao-Yang,Wu, Chuan-Shuo,Liu, An-Di,Liu, Li,Cheng, Liang
, p. 1643 - 1651 (2022/01/12)
An efficient fragment splicing method for the construction of multiple nucleobase-terminated monomers has been developed. Conformationally fixed rod, trigonal planar and tetrahedral thymine and adenine structures were generated in moderate to good yields,
Decatungstate-Mediated C(sp3)–H Heteroarylation via Radical-Polar Crossover in Batch and Flow
Capaldo, Luca,Frederick, Michael O.,García-Losada, Pablo,Laudadio, Gabriele,Mateos, Carlos,No?l, Timothy,Nu?o, Manuel,Nyuchev, Alexander V.,Rincón, Juan A.,Wan, Ting
, p. 17893 - 17897 (2021/07/14)
Photocatalytic hydrogen atom transfer is a very powerful strategy for the regioselective C(sp3)–H functionalization of organic molecules. Herein, we report on the unprecedented combination of decatungstate hydrogen atom transfer photocatalysis with the oxidative radical–polar crossover concept to access the direct net-oxidative C(sp3)–H heteroarylation. The present methodology demonstrates a high functional group tolerance (40 examples) and is scalable when using continuous-flow reactor technology. The developed protocol is also amenable to the late-stage functionalization of biologically relevant molecules such as stanozolol, (?)-ambroxide, podophyllotoxin, and dideoxyribose.
MLL1 INHIBITORS AND ANTI-CANCER AGENTS
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Page/Page column 30-31, (2021/04/01)
The present invention provides a compound of Formula (I): or an enantiomer, an enantiomeric mixture, or a pharmaceutically acceptable salt thereof; wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds; and methods of using such compounds for treating a disease or condition mediated by mixed lineage leukemia 1 (MLL).
PIPERIDINYL-METHYL-PURINEAMINES AS NSD2 INHIBITORS AND ANTI-CANCER AGENTS
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, (2021/02/19)
The present invention provides a compound of Formula (I): (I) or an enantiomer, an enantiomeric mixture, or a pharmaceutically acceptable salt thereof; wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds; and methods of using such compounds for treating a disease or condition mediated by nuclear SET domain-containing protein 2 (NSD2).
MLL1 INHIBITORS AND ANTI-CANCER AGENTS
-
, (2021/12/08)
The present invention provides a compound of Formula (I): or an enantiomer, an enantiomeric mixture, or a pharmaceutically acceptable salt thereof; wherein the variables are as defined herein. The present invention further provides pharmaceutical composit
Discovery of Nucleic Acid Binding Molecules from Combinatorial Biohybrid Nucleobase Peptide Libraries
Pomplun, Sebastian,Gates, Zachary P.,Zhang, Genwei,Quartararo, Anthony J.,Pentelute, Bradley L.
supporting information, p. 19642 - 19651 (2020/12/18)
Nature has three biopolymers: oligonucleotides, polypeptides, and oligosaccharides. Each biopolymer has independent functions, but when needed, they form mixed assemblies for higher-order purposes, as in the case of ribosomal protein synthesis. Rather tha
Base glycosylation method taking o-alkylenyl phenol ether as leaving group
-
, (2019/07/04)
The invention discloses a method for building C-N glycosidic bond of nucleoside. The method is simple in operation, mild in condition and high in stereoselectivity and regioselectivityof reaction. Themethod includes: taking o-alkylenyl phenol ether as the
COMPOSITIONS AND METHODS USING THE SAME FOR TREATMENT OF NEURODEGENERATIVE AND MITOCHONDRIAL DISEASE
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, (2015/09/22)
The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for the treatment and/or prevention of neurodegenerative disease and/or mitchonodrial disease including Parkinson's disease and Leigh's disease.
Progesterone-adenine hybrids as bivalent inhibitors of P-glycoprotein- mediated multidrug efflux: Design, synthesis, characterization and biological evaluation
Zeinyeh, Wael,Mahiout, Zahia,Radix, Sylvie,Lomberget, Thierry,Dumoulin, Axel,Barret, Roland,Grenot, Catherine,Rocheblave, Luc,Walchshofer, Nadia,Matera, Eva-Laure,Dumontet, Charles
, p. 1177 - 1191,15 (2020/08/20)
Bivalent ligands were designed on the basis of the described close proximity of the ATP-site and the putative steroid-binding site of P-glycoprotein (ABCB1). The syntheses of 19 progesterone-adenine hybrids are described. Their abilities to inhibit P-glycoprotein-mediated daunorubicin efflux in K562/R7 human leukemic cells overexpressing P-glycoprotein were evaluated versus progesterone. The hybrid with a hexamethylene linker chain showed the best inhibitory potency. The efficiency of these progesterone-adenine hybrids depends on two main factors: (i) the nature of the linker and (ii) its attachment point on the steroid skeleton.
Regioselective alkylation of the exocyclic nitrogen of adenine and adenosine by the Mitsunobu reaction
Fletcher, Steven
scheme or table, p. 2948 - 2950 (2010/06/21)
A novel synthetic route to N6-substitution of adenine is presented, employing the Mitsunobu reaction as the key step. A range of primary and secondary alcohols all coupled in very good to excellent yields within 30 min at 45 °C, offering a milder alternative to the traditional nucleophilic aromatic substitution of 6-chloropurine. The utility of this protocol is further demonstrated by its application to the syntheses of N6,N9-di-substituted adenines, including the potent and selective A1 adenosine receptor agonist N6-cyclopentyladenosine.
