| 摘要 |
The present invention relates to alkynyl-substituted camptothecins of formula (I), wherein R1 is selected from: hydrogen; an optionally substituted C1-C6 alkyl; C3-C7 cycloalkyl; C3-C7 cycloalkyl C1-C6 alkyl; phenyl C1-C6 alkyl; an optionally substituted phenyl; an optionally substituted naphthyl; -R x-NR3R4, wherein R x is C1-C4 alkylene, R3 and R4 are, each independently, hydrogen, C1-C6 alkyl, phenyl, or benzyl; -(R y)m-COOR5, wherein m is zero or 1, R y is C1-C4 alkylene, R5 is hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, or phenyl C1-C6 alkyl; -(R z)n -COR6, wherein n is zero or 1, R z is C1-C4 alkylene, R6 is C1-C6 alkyl, C3-C7 cycloalkyl, phenyl C1-C6 alkyl, an optionally substituted phenyl, or -NR7R8, wherein R7 and R8 are, each independently, hydrogen or C1-C6 alkyl; and - SiR9R10R11, wherein R9, R10 and R11 are, each independently, C1-C4 alkyl; R2 is selected from: hydrogen; C1-C6 alkyl, C3-C7 cycloalkyl; a nd phenyl C1-C6 alkyl, X is selected from: hydrogen; C1-C6 alkyl; C3-C7 cycloalkyl; C1-C6 alkoxy; C3-C7 cycloalkoxy; C1-C6 alkanoyloxy; benzoyloxy; amino; hydroxy; nitro; chlorine; and a methylene- or ethylene-dioxy group linked to positions 10 and 11 of the molecule; and the pharmaceutically acceptable salts thereof. These compounds are useful in therapy as antitumor agents.
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