Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition

Christelle Pouget; Catherine Fagnere; Jean-Philippe Basly; Gérard Habrioux; Albert Jośe Chulia

doi:10.1016/s0960-894x(02)00565-6

Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2859-61. doi: 10.1016/s0960-894x(02)00565-6.

Authors

Christelle Pouget¹, Catherine Fagnere, Jean-Philippe Basly, Gérard Habrioux, Albert Jośe Chulia

Affiliation

¹ UPRES EA 1085, Biomolécules et cibles cellulaires tumorales, Faculté de Pharmacie, 2 rue du Docteur Marcland, Limoges, France.

PMID: 12270163
DOI: 10.1016/s0960-894x(02)00565-6

Abstract

Two 4-imidazolylflavans were synthesized and their relative stereochemistry was established by 1H and 13C NMR data. These compounds were tested for their activity to inhibit aromatase. It was observed that the introduction of an imidazolyl group at carbon 4 on flavan nucleus led to potent molecules.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Aromatase / chemistry
Aromatase Inhibitors*
Drug Design
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Female
Flavonoids / chemical synthesis*
Flavonoids / pharmacology*
Humans
Imidazoles / chemical synthesis*
Imidazoles / pharmacology*
In Vitro Techniques
Magnetic Resonance Spectroscopy
Placenta / enzymology
Pregnancy
Protons
Stereoisomerism
Structure-Activity Relationship

Substances

Aromatase Inhibitors
Enzyme Inhibitors
Flavonoids
Imidazoles
Protons
Aromatase