| 摘要 |
3-Aryl-1,2-benzisoxazole compound (I) or its racemic isomer, enantiomer, diastereoisomer or salt with mineral or organic acids or bases is new. 3-Aryl-1,2-benzisoxazole compound of formula (I) or its racemic isomer, enantiomer, diastereoisomer or salt with mineral or organic acids or bases is new. A1, A2CH or N; X : CRa or N; Y1CRb or N; R1-R4alkyl, alkenyl, alkynyl, (hetero)aryl, (hetero)aralkyl (all optionally substituted), H, halo, CN, NO2, trifluoromethyl, OR5, SR5, NR5R6, C(O)R5, C(O)OR5, C(O)NR5R6, S(O)R5, S(O)2R5, S(O)NR5R6, S(O)2NR5R6, NR6C(O)R5 or NR6C(O)OR5; RbH, halo, CN, NO2, trifluoromethyl or (1-3C alkyl)n-W1-(1-3C alkyl)m-R5; R5, R6H, alkyl, alkenyl, alkynyl, (hetero)aryl, (hetero)aralkyl (all optionally substituted); n, M : 0-1; and W1simple bond, O, S, 1-3C alkyl, 2-3C alkenyl, 2-3C alkynyl, 3-7C (hetero)cycloalkyl, (hetero)aryl, NH, N(1-3C alkyl), C(O), C(O)-O, C(O)-NH, C(O)-N(1-3C alkyl), O-C(O), OC(O)-NH, NH-C(O), NH-C(O)-O, N(1-3C alkyl)-C(O), NH-O, N(1-3C alkyl)-O, S(O)-NH, S(O)2-NH, S(O)-N(1-3C alkyl), S(O)2-N (1-3C alkyl), NH-S(O), NH-S(O)2, N(1-3C alkyl)-S(O), N(1-3C alkyl)-S(O)2, OS(O), OS(O)2, S(O)-O, S(O)2-O, O-P(1-3C alkyl) (O), O-P(O)2, NH-P(1-3C alkyl)(O), NH-P(O)2, P(1-3C alkyl)(O)-NH or P(O)2-NH. Provided that: Ra is halogen, hydroxy or nitro when Rb is hydrogen; and Ra is hydrogen or halogen, hydroxyl, methyl, ethyl, methoxy, hydroxymethyl, nitro, carboxy or cyano when Rb is other than hydrogen atom. An independent claim is included for a pharmaceutical composition (A) comprising (I). [Image] - ACTIVITY : Cytostatic. - MECHANISM OF ACTION : Heat shock protein 90 inhibitor. The ability of (I) to inhibit heat shock protein activity was tested in vitro. The result showed that (I) exhibited a median inhibitory concentration value of 1-10 mu M.
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