19097-44-0Relevant articles and documents
Tetrahydrofuran ring opening with acid chlorides catalyzed by samarium triiodides
Yu,Zhang,Ling
, p. 1973 - 1977 (1993)
SmI3 acts as Lewis-acid catalysts in tetrahydrofuran ring opening reactions with acid chlorides under mild conditions.
Discovery of Macrocyclic Pyrimidines as MerTK-Specific Inhibitors
McIver, Andrew L.,Zhang, Weihe,Liu, Qingyang,Jiang, Xinpeng,Stashko, Michael A.,Nichols, James,Miley, Michael J.,Norris-Drouin, Jacqueline,Machius, Mischa,DeRyckere, Deborah,Wood, Edgar,Graham, Douglas K.,Earp, H. Shelton,Kireev, Dmitri,Frye, Stephen V.,Wang, Xiaodong
supporting information, p. 207 - 213 (2017/02/15)
Macrocycles have attracted significant attention in drug discovery recently. In fact, a few de novo designed macrocyclic kinase inhibitors are currently in clinical trials with good potency and selectivity for their intended target. In this study, we successfully engaged a structure-based drug design approach to discover macrocyclic pyrimidines as potent Mer tyrosine kinase (MerTK)-specific inhibitors. An enzyme-linked immunosorbent assay (ELISA) in 384-well format was employed to evaluate the inhibitory activity of macrocycles in a cell-based assay assessing tyrosine phosphorylation of MerTK. Through structure–activity relationship (SAR) studies, analogue 11 [UNC2541; (S)-7-amino-N-(4-fluorobenzyl)-8-oxo-2,9,16-triaza-1(2,4)-pyrimidinacyclohexadecaphane-1-carboxamide] was identified as a potent and MerTK-specific inhibitor that exhibits sub-micromolar inhibitory activity in the cell-based ELISA. In addition, an X-ray structure of MerTK protein in complex with 11 was resolved to show that these macrocycles bind in the MerTK ATP pocket.
The backbone N-(4-azidobutyl) linker for the preparation of peptide chimera
Fernandez-Llamazares, Ana I.,Garcia, Jesus,Adan, Jaume,Meunier, David,Mitjans, Francesc,Spengler, Jan,Albericio, Fernando
supporting information, p. 4572 - 4575 (2013/09/24)
A robust synthetic strategy for the introduction of the N-(4-azidobutyl) linker into peptides using standard SPPS techniques is described. Based on the example of Cilengitide it is shown that the N-(4-azidobutyl) group exerts similar conformational restra
Nucleotide and oligonucleotide prodrugs
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Page/Page column 19, (2008/06/13)
The present invention discloses compounds of formula (I): which exhibit antiviral properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of anti-HBV