167015-84-1Relevant articles and documents
Combined Approach of Backbone Amide Linking and On-Resin N-Methylation for the Synthesis of Bioactive and Metabolically Stable Peptides
Wesche, Frank,Adihou, Hélène,Kaiser, Astrid,Wurglics, Mario,Schubert-Zsilavecz, Manfred,Kaiser, Marcel,Bode, Helge B.
, p. 3930 - 3938 (2018)
Rhabdopeptides are a large class of nonribosomal peptides from the bacteria Xenorhabdus and Photorhabdus with low micromolar activity against different protozoa, which are the causative agents of several tropical diseases. The development of a facile and flexible synthesis combining backbone amide linking with on-resin peralkylation for the synthesis of permethylated rhabdopeptides is described. This strategy allows the fast generation of permethylated naturally occurring and artificial rhabdopeptides for a structure-activity study. Furthermore, in vitro experiments revealed their superior properties regarding their stability and passive membrane diffusion.
INHIBITORS FOR PROLIFERATING CELL NUCLEAR ANTIGEN AND USES
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, (2017/07/06)
The present invention relates to series of compounds as an inhibitor targeting Proliferating Cell Nuclear Antigen (PCNA). Pharmaceutical compositions of those compounds and methods of using them in the treatment of cancer are within the scope of this disclosure.
Toward general access to the Aspidosperma-type terpenoid indole alkaloids: Synthesis of the key 3,3-disubstituted piperidones through enantioselective intramolecular Heck-type reaction of chloroformamides
Yasui, Yoshizumi,Takeda, Hiroshi,Takemoto, Yoshiji
experimental part, p. 1567 - 1574 (2009/11/30)
An enantioselective intramolecular Heck-type reaction of chloroformamides has been developed for the synthesis of 3,3-disubstituted piperidones. The desired piperidone was formed in the presence of a palladium catalyst, an optically active phosphoramidite ligand, K3PO4 and Ag 3PO4. The obtained piperidone was converted to epieburnamonine.