专利号:US-8476313-B2 优先权日:2004-08-26 标 题:Heteroaryl-containing isoflavones as aromatase inhibitors 发明人:BRUEGGEMEIER ROBERT W; KIM YOUNG-WOO; HACKETT JOHN C 权利人:BRUEGGEMEIER ROBERT W; KIM YOUNG-WOO; HACKETT JOHN C; UNIV OHIO STATE RES FOUND 摘要:Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: n nwherein X is selected from O, N, S, SO, SO 2 , and S(CH 2 ) n , wherein n=1-10; R 1 and R 2 may be the same or different and are selected from H, OH, OCH 3 , OCH 2 CH 3 , OCH 2 C 6 H 5 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , CH(CH 3 ) 2 , C(CH 3 ) 3 , NO 2 , F, Cl, Br, CF 3 , SH, SCH 3 , SCH 2 CH 3 , OCOCH 3 , OCOC(CH 3 ) 3 , OCOCH 2 COOH, and CN; and R 3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.
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合成参考文献
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