582313-57-3Relevant articles and documents
Fluorine substituted adenosines as probes of nucleobase protonation in functional RNAs
Suydam, Ian T.,Strobel, Scott A.
, p. 13639 - 13648 (2008)
Ionized nucleobases are required for folding, conformational switching, or catalysis in a number of functional RNAs. A common strategy to study these sites employs nucleoside analogues with perturbed pKa, but the interpretation of these studies
COMPOUNDS ACTIVE TOWARDS NUCLEAR RECEPTORS
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Page/Page column 124, (2021/10/11)
Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.
SELECTIVE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5
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Paragraph 0251, (2020/10/20)
The disclosure is directed to methods of treating disease using compounds of Formula (I).
Synthesis and anti-HBV activity of carbocyclic nucleoside hybrids with salient features of entecavir and aristeromycin
Baba, Masanori,Bal, Chandralata,Jha, Ashok Kumar,Neeladri, Seshubabu,Pallaka, Renuka Sivasankar,Samunuri, Ramakrishnamraju,Toyama, Masaaki
, p. 597 - 601 (2020/06/08)
Modified carbocyclic nucleosides (4a-g) constituting 7-deazapurine, 4′-methyl, exocyclic double bond and 2′,3′-hydroxy were synthesized. NOE and X-ray studies of4cconfirmed the α-configuration of 4′-methyl. The anti-HBV assay demonstrated4e(IC50/sub
CYCLIC DINUCLEOTIDES AS STING AGONISTS
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Page/Page column 288-290, (2019/07/19)
Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein B2,X2, R2a, R2b, R2c, Z-M-Y, Y1-M1Z1, B1, X1, R1a, R1b, R1c are as defined herein.
Selective Inhibitors Of Protein Arginine Methyltransferase 5 (PRMT5)
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Paragraph 0282; 0283, (2019/02/24)
The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
SUBSTITUTED NUCLEOSIDE DERIVATIVES USEFUL AS ANTICANCER AGENTS
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Paragraph 0310; 0311, (2016/09/26)
Compounds of the general formula (I): processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms
Spurr, Sophie S.,Bayle, Elliott D.,Yu, Wenyu,Li, Fengling,Tempel, Wolfram,Vedadi, Masoud,Schapira, Matthieu,Fish, Paul V.
supporting information, p. 4518 - 4522 (2016/08/24)
A number of new nucleoside derivatives are disclosed as inhibitors of DOT1L activity. SARs established that DOT1L inhibition could be achieved through incorporation of polar groups and small heterocycles at the 5-position (5, 6, 12) or by the application of alternative nitrogenous bases (18). Based on these results, CN-SAH (19) was identified as a potent and selective inhibitor of DOT1L activity where the polar 5-nitrile group was shown by crystallography to bind in the hydrophobic pocket of DOT1L. In addition, we show that a polar nitrile group can be used as a non-traditional replacement for heavy halogen atoms.
4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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, (2015/12/08)
Provided is 4'-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.
Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Nav1.7 antagonists
Chakka, Nagasree,Bregman, Howie,Du, Bingfan,Nguyen, Hanh Nho,Buchanan, John L.,Feric, Elma,Ligutti, Joseph,Liu, Dong,McDermott, Jeff S.,Zou, Anruo,McDonough, Stefan I.,Dimauro, Erin F.
scheme or table, p. 2052 - 2062 (2012/04/17)
Herein we describe the discovery, optimization, and structure-activity relationships of novel potent pyrrolopyrimidine Nav1.7 antagonists. Hit-to-lead SAR studies of the pyrrolopyrimidine core, head, and tail groups of the molecule led to the identification of pyrrolopyrimidine 48 as exceptionally potent Nav1.7 blocker with good selectivity over hERG and improved microsomal stability relative to our hit molecule and pyrazolopyrimidine 8 as a promising starting point for future optimization efforts.