302349-32-2Relevant academic research and scientific papers
Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors
Adhikari, Sharmila,Brownell, James E.,Calderwood, Emily F.,Chouitar, Jouhara,D'Amore, Natalie Roy,England, Dylan B.,Foley, Klaudia,Gould, Alexandra E.,Harrison, Sean J.,Huang, Shih-Chung,LeRoy, Patrick J.,Lok, David,Lublinsky, Anna,Ma, Li-Ting,Menon, Saurabh,Yang, Yu,Zhang, Ji
, (2020/08/13)
Autophagy is postulated to be required by cancer cells to survive periods of metabolic and/or hypoxic stress. ATG7 is the E1 enzyme that is required for activation of Ubl conjugation pathways involved in autophagosome formation. This article describes the design and optimization of pyrazolopyrimidine sulfamate compounds as potent and selective inhibitors of ATG7. Cellular levels of the autophagy markers, LC3B and NBR1, are regulated following treatment with these compounds.
ATG7 INHIBITORS AND THE USES THEREOF
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Paragraph 00466, (2018/05/27)
Disclosed are chemical entities which are compounds of formula (I) : or a pharmaceutically acceptable salt thereof, wherein R1, R2, and Ra have the values described herein. Chemical entities according to the disclosure can be useful as inhibitors of ATG7. Further provided are pharmaceutical compositions comprising a chemical entity of the disclosure and methods of using the compositions in the treatment of cancer.
Synthesis of 2',3'-dideoxy-3'-fluoro-L-ribonucleosides as potential antiviral agents from D-sorbitol
Chun, Byoung K.,Schinazi, Raymond F.,Cheng, Yung-Chi,Chu, Chung K.
, p. 49 - 59 (2007/10/03)
2',3'-Dideoxy-3'-fluoro-L-ribonucleosides were synthesized as potential antiviral agents. The key intermediate, methyl 5-O-benzoyl-2-3-dideoxy-3-fluoro-L-ribofuranoside, which was prepared from D-sorbitol, was condensed with pyrimidine and purine bases to obtain the respective nucleosides. Among them, the cytosine analogue 2',3'-dideoxy-3'-fluoro-α-L-cytidine showed a moderate anti-HBV activity. (C) 2000 Elsevier Science Ltd.
Asymmetric synthesis of carbohydrates: Synthesis of 2-deoxy-D- and 2-deoxy-L-xylofuranosides from a simple achiral precursor
Jung, Michael E.,Gardiner, John M.
, p. 6755 - 6758 (2007/10/02)
The acetylenic alcohol, 3, readily prepared in two steps from propargyl bromide, 1, is converted to methyl 2-deoxy-D-xylofuranoside, 13, and to the unnatural L-enantiomer, 12, in 5 steps and 50% overall yield, utilizing asymmetric dihydroxylation (AD) of alkene 7 for introduction of chirality. A similar strategy from the isomeric Z-allylic alcohol, 4, afforded the 2-deoxy-L-ribofuranoside, but in modest enantiomeric excess.
