Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors

Samir Yahiaoui; Christelle Pouget; Catherine Fagnere; Yves Champavier; Gérard Habrioux; Albert José Chulia

doi:10.1016/j.bmcl.2004.07.090

Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5215-8. doi: 10.1016/j.bmcl.2004.07.090.

Authors

Samir Yahiaoui¹, Christelle Pouget, Catherine Fagnere, Yves Champavier, Gérard Habrioux, Albert José Chulia

Affiliation

¹ UPRES EA 1085 Biomolécules et Cibles Cellulaires Tumorales, Faculté de Pharmacie, 2 rue du Docteur Marcland, 87025 Limoges, France.

PMID: 15380230
DOI: 10.1016/j.bmcl.2004.07.090

Abstract

Aromatase is a target of pharmacological interest for the treatment of estrogen-dependent cancers. Azole derivatives such as letrozole or anastrozole have been developed for aromatase inhibition and are used for the treatment of breast tumors. In this paper, four 4-triazolylflavans were synthesized and were found to exhibit moderate to high inhibitory activity against aromatase.

Publication types

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

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Aromatase Inhibitors / chemical synthesis*
Aromatase Inhibitors / chemistry
Aromatase Inhibitors / pharmacology
Flavones / chemical synthesis*
Flavones / chemistry
Flavones / pharmacology
Humans
In Vitro Techniques
Microsomes / drug effects
Microsomes / enzymology
Placenta / ultrastructure
Structure-Activity Relationship
Triazoles / chemical synthesis*
Triazoles / chemistry
Triazoles / pharmacology

Substances

Antineoplastic Agents
Aromatase Inhibitors
Flavones
Triazoles