1. Academic Validation
  2. Bioactive Aurones, Indanones, and Other Hemiindigoid Scaffolds: Medicinal Chemistry and Photopharmacology Perspectives

Bioactive Aurones, Indanones, and Other Hemiindigoid Scaffolds: Medicinal Chemistry and Photopharmacology Perspectives

  • J Med Chem. 2022 Oct 13;65(19):12594-12625. doi: 10.1021/acs.jmedchem.2c01150.
Leticia M Lazinski 1 2 Guy Royal 2 Maxime Robin 3 Marc Maresca 4 Romain Haudecoeur 1
Affiliations

Affiliations

  • 1 Université Grenoble Alpes, CNRS 5063, DPM, 38000 Grenoble, France.
  • 2 Université Grenoble Alpes, CNRS 5250, DCM, 38000 Grenoble, France.
  • 3 Mediterranean Institute of Marine and Terrestrial Biodiversity and Ecology (IMBE), Aix Marseille Université, 27 Boulevard Jean Moulin, 13385 Marseille, France.
  • 4 Aix Marseille Université, CNRS, Centrale Marseille, iSm2, 13397 Marseille, France.
Abstract

Hemiindigoids comprise a range of natural and synthetic scaffolds that share the same aromatic hydrocarbon backbone as well as promising biological and optical properties. The encouraging therapeutic potential of these scaffolds has been unraveled by many studies over the past years and uncovered representants with inspiring pharmacophoric features such as the acetylcholinesterase inhibitor donezepil and the tubulin polymerization inhibitor indanocine. In this review, we summarize the last advances in the medicinal potential of hemiindigoids, with a special attention to molecular design, structure-activity relationship, ligand-target interactions, and mechanistic explanations covering their effects. As their strong fluorogenic potential and photoswitch behavior recently started to be highlighted and explored in biology, giving rise to the development of novel fluorescent probes and photopharmacological agents, we also discuss these properties in a medicinal chemistry perspective.

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