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STILBENOID COMPOUNDS AS SILICA CELL CARCINOMA AND HEPATOMA INHIBITORS AND THEIR APPLICATION

机译:甲硅烷基化合物作为二氧化硅细胞癌和肝癌抑制剂及其应用

摘要

1. The compound of formula I: or its stereoisomer, geometric isomer, tautomer, N-oxide, hydrate, solvate, metabolite or pharmaceutically acceptable salt or prodrug, where R ′, R are hydrogen or C1-6alkyl; R, R, R are each independently hydrogen , C1-6alkyl, or; R, R, R each independently represents hydrogen, C1-6alkyl, (CH) -CHOH or (CHOH) -CHOH, n = 0 to 3; and at least one of R, R, R is 2. A compound according to claim 1, characterized in that R, R, R each independently represents at least one of R, R, R is (CH) -CHOH, n = from 0 to 3.3. A compound according to claim 1, characterized in that R, R, R each independently represent at least one of R, R, R is (CHOH) -CHOH, n = from 0 to 3.4. A pharmaceutical composition containing a compound according to claim 1.5. The pharmaceutical composition of claim 4, further comprising a pharmaceutically acceptable carrier, excipient, diluent, adjuvant, medium, or combinations thereof. A method for treating squamous cell carcinoma / hepatoma in a subject in need thereof, comprising administering to said subject a therapeutically effective amount of a compound according to claim 1.7. A process for preparing a compound of formula I, comprising deprotecting a compound of formula II: wherein R ′, R are hydrogen or C1-6alkyl; X, X, each independently are hydrogen, C1-6alkyl, or where R and R are each independently hydrogen or C1-6alkyl; X, X, Xne are selected from hydrogen and C1-6alkyl to give a compound of formula I: wherein R ′, R are hydrogen or C1-6alkyl; R, R, R are each independently hydrogen, C1-6alkyl, or; R, R, R are each independently
机译:1.式I化合物:或其立体异构体,几何异构体,互变异构体,N-氧化物,水合物,溶剂化物,代谢产物或药学上可接受的盐或前药,其中R',R为氢或C1-6烷基; R 1,R 2和R 3各自独立地为氢,C 1-6烷基或; R 1,R 2和R 3各自独立地表示氢,C 1-6烷基,(CH)-CHOH或(CHOH)-CHOH,n = 0至3; 2.根据权利要求1的化合物,其特征在于,R 1,R 2,R 3各自独立地表示R 1,R 2和R 3的至少一个,R 3为(CH)-CHOH,n = R 1和R 2。 0至3.3。 2.根据权利要求1所述的化合物,其特征在于,R 1,R 2,R 3分别独立地表示R 1,R 2,R 3为(CHOH)-CHOH中的至少一个,n = 0〜3.4。含有权利要求1.5的化合物的药物组合物。 5.根据权利要求4所述的药物组合物,其进一步包含药学上可接受的载体,赋形剂,稀释剂,佐剂,介质或其组合。一种在有需要的受试者中治疗鳞状细胞癌/肝癌的方法,包括向所述受试者施用治疗有效量的根据权利要求1.7所述的化合物。制备式I化合物的方法,该方法包括使式II化合物脱保护:其中R',R为氢或C1-6烷基; X,X各自独立地是氢,C 1-6烷基,或其中R 1和R 2各自独立地是氢或C 1-6烷基; X,X,Xne选自氢和C 1-6烷基,得到式I化合物:其中R',R为氢或C 1-6烷基; R 1,R 2和R 3各自独立地为氢,C 1-6烷基或; R,R,R各自独立

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