TY  - BOOK
AU  - Pouget,C.
AU  - Yahiaoui,S.
AU  - Fagnere,C.
AU  - Habrioux,G.
AU  - Chulia,A.J.
TI  - Synthesis and biological evaluation of 4-imidazolylflavans as nonsteroidal aromatase inhibitors
KW  - 4-IMIDAZOLYLFLAVANS
KW  - BREAST CANCER
KW  - ANTI-AROMATASE EFFECT
KW  - STRUCTURE-ACTIVITY RELATIONSHIPS
N2  - A series of 4-imidazolylflavans having a variety of substituents on the 2-phenyl ring was synthesized and investigated for their inhibitory effect against aromatase. Structure-activity relationships of these compounds were determined. An additional chlorine atom or a cyano group at the 40 position did not enhance aromatase inhibition as well as a 30-hydroxyl group. The influence of an additional 40-hydroxyl group depends on the substitution pattern of A ring. Among these molecules, 40-hydroxy-4-imidazolyl-7-methoxyflavan is only 2.2-fold less active than the letrozole (as assessed by IC50 values). Letrozole is used as the first-line therapy for metastatic breast cancer
UR  - https://drive.google.com/file/d/1v6LIwEaRFYSWdICcvmjpPESfy6FTSW97/view?usp=drivesdk
ER  -