2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

Bioorganic & Medicinal Chemistry
Simone Di MiccoGiuseppe Bifulco

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.

References

Nov 30, 2007·Mini Reviews in Medicinal Chemistry·Carolina D DuarteCarlos A M Fraga
Nov 17, 2010·ACS Chemical Biology·Brett LomenickJing Huang

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Citations

Mar 26, 2016·International Journal of Biological Macromolecules·Ashish Gupta, Polamarasetty Aparoy
Aug 10, 2016·Journal of Natural Products·Nunzio CardulloCorrado Tringali
Oct 1, 2016·European Journal of Medicinal Chemistry·Gianluigi LauroGiuseppe Bifulco
Dec 23, 2016·Medicinal Research Reviews·Catarina Pereira-LeiteSalette Reis
May 13, 2017·Journal of Natural Products·Luana PulvirentiCorrado Tringali
Sep 25, 2020·International Journal of Molecular Sciences·Giuseppe FlorestaCorrado Tringali
Mar 5, 2019·Anti-cancer Agents in Medicinal Chemistry·Bahadır Bülbül, İlkay Küçükgüzel
Feb 13, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nunzio CardulloCorrado Tringali
May 29, 2021·Frontiers in Chemistry·Simone Di MiccoGiuseppe Bifulco

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