477781-69-4Relevant articles and documents
A MedChem toolbox for cereblon-directed PROTACs
Steinebach, Christian,Sosi?, Izidor,Lindner, Stefanie,Bricelj, Ale?a,Kohl, Franziska,Ng, Yuen Lam Dora,Monschke, Marius,Wagner, Karl G.,Kr?nke, Jan,Gütschow, Michael
supporting information, p. 1037 - 1041 (2019/06/27)
A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used linkers of different constitution to modulate physicochemical properties. We equipped one terminus of the linker with a set of functional groups, e.g. protected amines, protected carboxylic acids, alkynes, chloroalkanes, and protected alcohols, all of which are considered to be attractive for PROTAC design. We also highlight different opportunities for the expansion of the medicinal chemists' PROTAC toolbox towards heterobifunctional molecules, e.g. with biotin, fluorescent, hydrophobic and peptide tags.
Propargylamine-isothiocyanate reaction: Efficient conjugation chemistry in aqueous media
Viart,Larsen,Tassone,Andresen,Clausen
, p. 7800 - 7802 (2014/07/08)
A coupling reaction between secondary propargyl amines and isothiocyanates in aqueous media is described. The reaction is high-yielding and affords cyclized products within 2-24 h. A functionalized ether lipid was synthesized in 8 steps, formulated as liposomes with POPC and conjugated to FITC under mild conditions using this method. This journal is the Partner Organisations 2014.
Ionic strength mediated hydrophobic force switching of CF 3-terminated ethylene glycol self-assembled monolayers (SAMs) on gold
Bonnet, Nelly,O'Hagan, David,Haehner, Georg
, p. 5066 - 5068 (2008/09/18)
We have synthesised novel oligo(ethylene glycol), CF3-terminated switching self-assembled monolayers, which allow the force experienced by a hydrophobic object to be controlled via the ionic strength of the environment. The Royal Society of Chemistry.