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245 1 0 _aSynthesis and biological evaluation of 4-imidazolylflavans as nonsteroidal aromatase inhibitors
490 0 _vBioorganic Chemistry, 32(6), p.494-503, 2004
520 3 _aA 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.
650 1 4 _a4-IMIDAZOLYLFLAVANS
650 1 4 _aBREAST CANCER
650 1 4 _aANTI-AROMATASE EFFECT
650 1 4 _aSTRUCTURE-ACTIVITY RELATIONSHIPS
700 1 2 _aPouget, C.
700 1 2 _aYahiaoui,S.
700 1 2 _aFagnere, C.
700 1 2 _aHabrioux, G.
700 1 2 _aChulia, A.J.
856 4 0 _uhttps://drive.google.com/file/d/1v6LIwEaRFYSWdICcvmjpPESfy6FTSW97/view?usp=drivesdk
_zPara ver el documento ingresa a Google con tu cuenta: @cicy.edu.mx
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