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Scientific article
English

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

Contributors

Duplan, Vincent; Serba, Christelle; Garcia, Jose; Valot, Gaëlle; Barluenga Badiola, Sofia; Hoerle, Mélanie; Cuendet, Muriel; Winssinger, Nicolas

Published in

Organic & biomolecular chemistry, vol. 12, no. 2, p. 370-375

Publication date

2014

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.

UNIGE affiliation entities

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

Main files (1)

Article (Published version)

Identifiers

Additional URL for this publication

http://xlink.rsc.org/?DOI=c3ob42049c

Journal ISSN

1477-0520
777views
14downloads

Technical informations

Creation

11/12/2013 10:33:00

First validation

11/12/2013 10:33:00

Update

13/10/2025 23:13:29

Status update

14/03/2023 20:42:32

Last indexation

01/07/2026 06:10:30
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