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Cover Feature: A One‐Pot “Triple‐C” Multicyclization Methodology for the Synthesis of Highly Constrained Isomerically Pure Tetracyclic Peptides (ChemBioChem 18/2018)
Author(s) -
Richelle Gaston J. J.,
Schmidt Marcel,
Ippel Hans,
Hackeng Tilman M.,
van Maarseveen Jan H.,
Nuijens Timo,
Timmerman Peter
Publication year - 2018
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201800491
Subject(s) - bifunctional , chemistry , cover (algebra) , feature (linguistics) , combinatorial chemistry , stereochemistry , bicyclic molecule , triple bond , organic chemistry , catalysis , double bond , mechanical engineering , linguistics , philosophy , engineering
The cover feature picture shows the combination of CEPS, CLIPS and CuAAC (Triple‐C) that enables the efficient one‐pot synthesis of isomerically pure tetracyclic peptides. The use of this Triple‐C methodology allowed the synthesis of mono‐ and bifunctional tetracycles, based on previously reported bicyclic leads, which showed good inhibitory activities against both uPA and FXIIa. As the icing on the cake, the 3D structure of these constructs has been unraveled by using 2D NMR analysis. More information can be found in the communication by T. Nuijens, P. Timmerman et al. on page 1934 in Issue 18, 2018 (DOI: 10.1002/cbic.201800346).