| 摘要 |
PURPOSE: Novel alkaloid derivatives, specifically novel colchicine derivatives having anticancer, antiproliferative and anti-inflammatory effects, and immunosuppressive function and muscle relaxation, and a pharmaceutical composition containing the same are provided. CONSTITUTION: The novel colchicine derivatives have the formula (I), wherein, if R1 is N(R6)C(X1)-A, X2C(X1)-A, N(R6)-A, N(A)2 or X2-A, R2 is X3R7 or N(R7)2, R3 and R4 are independently hydrogen or a methyl group, R5 is hydrogen, a methyl group, or CH2X4R7, wherein R6 and R7 are independently hydrogen or a lower alkyl group, and X, X1, X2, X3 and X4 are independently 0 or S; if R2 is N(R6)C(X1)-A, X2C(X1)-A, N(R6)-A, N(A)2 or X2-A, R1 is N(R6)COCH3, N(R6)COCF3, or NHC(O)OR8, R3 and R4 are independently hydrogen or a methyl group, R5 is hydrogen, a methyl group, or CH2X4R7, wherein R6 and R7 are independently hydrogen or a lower alkyl group, R8 is a lower alkyl, alkenyl, or substituted or unsubstituted aryl, and X, X1, X2 and X4 are independently 0 or S; if R3 and R4 are independently C(X1)-A or -A, R1 is N(R6)COCH3, N(R6)COCF3, or NHC(O)OR8, R2 is X3R7 or N(R-)2, R5 is hydrogen, a methyl group, or CH2X4R7, wherein R6 and R7 are independently hydrogen or a lower alkyl group, R8 is a lower alkyl, alkenyl, or substituted or unsubstituted aryl, and X, X1, X3 or X4 are independently 0 or S; and if R5 is CH2X2C(X1)-A, R1 is N(R6)COCH3, N(R6)COCF3 or NHC(O)OR8, R2 is X3R7 or N(R7)2, R3 and R4 are independently hydrogen or a methyl group, wherein R6 and R7 are independently hydrogen or a lower alkyl group, R8 is a lower alkyl, alkenyl, or substituted or unsubstituted aryl group, and X, X1, X2 and X3 are independently 0 or S, wherein A is represented by the formula (a), (b), (c), (d), (e), (g), (h), (i) or (j).
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