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Article dans une revue
2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors
Abstract : 2,3-Dihydrobenzofurans are proposed as privileged structures and used as chemical platform to design small compound libraries. By combining molecular docking calculations and experimental verification of biochemical interference, we selected some potential inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1. Starting from low affinity natural product 1, by our combined approach we identified the compounds 19 and 20 with biological activity in the low micromolar range. Our data suggest that the 2,3-dihydrobenzofuran derivatives might be suitable bioinspired lead compounds for development of new generation mPGES-1 inhibitors with increased affinity.
https://hal-univ-bourgogne.archives-ouvertes.fr/hal-01390150
Contributeur : Icmub - Université de Bourgogne Connectez-vous pour contacter le contributeur
Soumis le : lundi 31 octobre 2016 - 19:00:56
Dernière modification le : jeudi 16 décembre 2021 - 03:55:59
Contributeur : Icmub - Université de Bourgogne Connectez-vous pour contacter le contributeur
Soumis le : lundi 31 octobre 2016 - 19:00:56
Dernière modification le : jeudi 16 décembre 2021 - 03:55:59