133803-81-3Relevant articles and documents
Efficient synthesis of polyethylene glycol mono-carboxylate via Michael conjugate addition
Chen, Qingqi,Gabathuler, Reinhard
, p. 2425 - 2432 (2004)
Poly(ethylene glycol) (PEG) with one carboxylate group, the very useful precursors for the synthesis of the PEG derived heterobifunctional linkers, are synthesized in high yield in one-pot via Michael conjugate addition of acrylate esters with PEG and catalyst amount of sodium in THF.
Synthesis of 6-O-benzyl guanine and its conjugations with linkers
Barth, Claudia,Seitz, Oliver,Kunz, Horst
, p. 802 - 806 (2004)
An improved synthesis of 6-O-benzyl guanine which is an important inhibitor of O6-alkyl-guanine DNA alkyltransferase (AGT) is described. In addition the conjugation of this guanine derivative was achieved with a functionalised hydrophilic linke
New fluorine-18 pretargeting PET imaging by bioorthogonal chlorosydnone-cycloalkyne click reaction
Richard, Mylène,Truillet, Charles,Tran, Vu Long,Liu, Hui,Porte, Karine,Audisio, Davide,Roche, Mélanie,Jego, Benoit,Cholet, Sophie,Fenaille, Fran?ois,Kuhnast, Bertrand,Taran, Frédéric,Specklin, Simon
, p. 10400 - 10403 (2019)
We report the first pretargeting in vivo study using the Strain-Promoted Sydnone-Alkyne Cycloaadition (SPSAC) reaction. The injection of a fluorine-18 labeled cyclooctyne three days after cetuximab bearing chlorosydnone moieties allowed a significant detection of the tumor by PET imaging suggesting an efficient click reaction inside the tumoral site. With a kinetic constant superior to 300 M-1 s-1, the SPSAC reaction might be an interesting tool, in addition to tetrazine-cyclooctene ligation, for in vivo chemistry.
Synthesis of KUE-siRNA Conjugates for Prostate Cancer Cell-Targeted Gene Silencing
Yang, Chao,Ma, Dejun,Lu, Liqing,Yang, Xing,Xi, Zhen
, p. 2888 - 2895 (2021/08/03)
The delivery of siRNAs to selectively target cells poses a great challenge in RNAi-based cancer therapy. The lack of suitable cell-targeting methods seriously restricts the advance in delivering siRNAs to extrahepatic tissues. Based on prostate-specific m
PCSK9 ANTAGONIST COMPOUNDS
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Page/Page column 71, (2021/06/26)
Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof: (I) wherein A, A1, A2, R1, R2 and R3 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
