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Scientific article
English

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

Published inOrganic & biomolecular chemistry, vol. 12, no. 2, p. 370-375
Publication date2014
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.

Citation (ISO format)
DUPLAN, Vincent et al. Synthesis of sesquiterpene-inspired derivatives designed for covalent binding and their inhibition of the NF-κB pathway. In: Organic & biomolecular chemistry, 2014, vol. 12, n° 2, p. 370–375. doi: 10.1039/c3ob42049c
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ISSN of the journal1477-0520
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Creation12/11/2013 10:33:00 AM
First validation12/11/2013 10:33:00 AM
Update time03/14/2023 8:42:33 PM
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