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Synthesis of sesquiterpene-inspired derivatives designed for covalent binding and their inhibition of the NF-κB pathway

Authors
Duplan, Vincent
Garcia, Jose
Valot, Gaëlle
Published in Organic and Biomolecular Chemistry. 2014, vol. 12, no. 2, p. 370-375
Abstract A significant portion of bioactive secondary metabolites are endowed with reactive functionalities that can engage in covalent interactions with their target. Sesquiterpene lactones in particular are rich in Michael acceptors that react with cysteines. Several polycyclic scaffolds derived from total synthesis or readily available polycyclic terpenes were used as the starting point in the synthesis of a library aiming to project mildly reactive functionalities (Michael acceptors or chloroacetates) with diverse geometries. Screening of the library for inhibition of the NF-κB pathway revealed several potent inhibitors that are chemically readily accessible.
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Other version: http://xlink.rsc.org/?DOI=c3ob42049c
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DUPLAN, Vincent et al. Synthesis of sesquiterpene-inspired derivatives designed for covalent binding and their inhibition of the NF-κB pathway. In: Organic and Biomolecular Chemistry, 2014, vol. 12, n° 2, p. 370-375. https://archive-ouverte.unige.ch/unige:32027

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Deposited on : 2013-12-11

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