Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
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.
Yahiaoui
Samir
S
UPRES EA 1085 Biomolécules et Cibles Cellulaires Tumorales, Faculté de Pharmacie, 2 rue du Docteur Marcland, 87025 Limoges, France.
Pouget
Christelle
C
Fagnere
Catherine
C
Champavier
Yves
Y
Habrioux
Gérard
G
Chulia
Albert José
AJ
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047072:Aromatase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047309:Flavones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D010920:Placenta / Q000648:ultrastructure; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; D047309:Flavones; D014230:Triazoles