| 摘要 |
Styryl benzylsulfones of formula I are useful as ant-proliferative agents, including, for example, anticancer agents. In formula I:
(a) (i) R 1 , R 2 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl;
(ii) R 3 is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, provided at least three of R 1 , R 2 , R 3 , R 4 and R 5 are other than hydrogen; and
(iii) R 6 , R 7 , R 8 , R 9 and R 10 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl;
or
(b) (i) R 6 , R 8 and R 10 are halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, and R 7 and R 9 are hydrogen; and
(ii) R 1 , R 2 , R 3 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy), or trifluoromethyl;
or
(c) (i) at least four of R 6 , R 7 , R 8 , R 9 and R 10 are halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, and the remainder of R 6 , R 7 , R 8 , R 9 and R 10 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl; and
(ii) R 1 , R 2 , R 3 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy), or trifluoromethyl;
or a pharmaceutically acceptable salt thereof.
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