93366-88-2Relevant academic research and scientific papers
Design and evaluation of a potential mutagen for Hepatitis C virus
Koh, Yung-Hyo,Shim, Jae Hoon,Girardet, Jean-Luc,Hong, Zhi
, p. 5261 - 5264 (2007)
Pyrrolopyrimidine nucleoside 1 was designed and synthesized as a potential mutagen for HCV. An in vitro HCV NS5B enzymatic assay indicated that pyrrolopyrimidine triphosphate acts as a CTP analog rather than a UTP analog. The SATE-prodrug of pyrrolopyrimidine monophosphate showed a weak inhibitory activity in an HCV replicon system (EC50 = 60 μM) and did not exhibit cytotoxicity (CC50 > 100 μM). Investigation of phosphorylation events using nucleoside kinases and LC-MS analysis revealed that the second phosphorylation step, from monophosphate ester to diphosphate ester, is unfavorable.
Compound with 2-aminopyrimidine structure as well as preparation method and purpose thereof
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Paragraph 0168-0171, (2019/06/08)
The invention provides a compound of a 2-aminopyrimidine structure shown as a general formula (1), or a stereisomer, enantiomers or medically acceptable salt of the compound, a preparation method of the compound, a medicine composition containing the composition or a purpose of the composition. The compound shown as the general formula (1) can be used for preparing NIK kinase inhibitors, and can be used for preventing and/or treating diseases relevant to NIK kinase, particularly cancer and metabolic diseases, such as B-cell dysfunction related cancer such as multiple myeloma, lymphocyte carcinoma, diffuse large B cell lymphoma of liver cancer, hodgkin lymphoma and chronic lymphocytic leukemia, prostatic cancer, liver cancer, intestinal cancer, medicine induced liver damage, alcohol inducedliver damage, toxic induced acute liver injury, chronic liver inflammation and the like. The general formula (1) is shown in the description.
COMPOUNDS FOR THE TREATMENT OF HIV
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Page/Page column 325; 326, (2013/03/26)
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization
Harris, Christopher M.,Ericsson, Anna M.,Argiriadi, Maria A.,Barberis, Claude,Borhani, David W.,Burchat, Andrew,Calderwood, David J.,Cunha, George A.,Dixon, Richard W.,Frank, Kristine E.,Johnson, Eric F.,Kamens, Joanne,Kwak, Silvia,Li, Biqin,Mullen, Kelly D.,Perron, Denise C.,Wang, Lu,Wishart, Neil,Wu, Xiaoyun,Zhang, Xiaolei,Zmetra, Tami R.,Talanian, Robert V.
scheme or table, p. 334 - 337 (2010/04/02)
We describe structure-based optimization of a series of novel 2,4-diaminopyrimidine MK2 inhibitors. Co-crystal structures (see accompanying Letter) demonstrated a unique inhibitor binding mode. Resulting inhibitors had IC50 values as low as 19 nM and moderate selectivity against a kinase panel. Compounds 15, 31a, and 31b inhibit TNFα production in peripheral human monocytes.
CYTIDINE ANALOGS AND METHODS OF USE
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Page/Page column 32, (2010/02/08)
Cytidine analogs, their prodrugs and/or metabolites are employed as pharmaceutically active compounds for treatment of diseases responsive to such compounds. Particularly preferred diseases include viral diseases (e.g., HCV infection) and neoplasms.
Synthesis of 2'-Deoxyribofuranosides of 7H-Pyrrolopyrimidine: Influence of the C-2 Substituents on the Fluorescence
Seela, Frank,Steker, Herbert
, p. 1719 - 1730 (2007/10/02)
7-Deaza-2'-deoxynebularine (2a), its 2-methylthio (2b) and 2-amino derivative (2c) have been synthesized via phase-transfer glycosylation of the nucleobases 3a, 3b, and 3c, respectively, with the 2-deoxyhalogenose 6.Glycosylation of 3a leads to the formation of a 3:1 mixture of the anomers 7a and 8a in 48-percent total yield, the corresponding reaction of 3b or 3c gives mainly the β anomers in increased yield.Cleavage of the protecting groups yields 2a-c or the anomers 8a and 8c.The 2-methylthio group, as well as the 2-amino group increase the fluorescence of the parent nucleoside 2a.
