| 摘要 |
The invention relates to novel radioactively labeled pharmacologically effective epothilone derivatives of general formula (I), wherein: R<1> represents O-PG and hydroxyl, wherein PG is a protective group; R<2a>, R<2b> are the same or different and represent, independent of one another, hydrogen C1-C10 alkyl, aryl, C7-C20 aralkyl or, together, represent a (CH2)m group, wherein m is equal to 1, 2, 3, 4 or 5; R<3> represents a C2-C10 alkyl group, a C2-C10 alkenyl group or a C8-C20 aralkyl each containing 2n tritium atoms, wherein n equals 1 or 2; R<4> represents O-PG and hydroxyl; R<5> represents hydrogen C1-C10 alkyl, aryl, C7-C20 aralkyl and halogen; W-Z represents a CH2-CH2, CH2-O or O-CH2 group; R<6> represents hydrogen, C1-C10 alkyl, aryl, C7-C20 aralkyl, (CH2)s-V and halogen, wherein s equals 1, 2, 3 or 4 and V represents O-PG, hydroxyl or halogen; R<7>, R<8> each represent a hydrogen atom and, together, represent an additional bond or an oxygen atom; A represents aryl, C7-C20 aralkyl, and a group R<10>-CH=C<9>-, wherein R<9> represents hydrogen, halogen, CN, C1-C20 alkyl, aryl, and C7-C20 aralkyl, and R<10> represents hydrogen, C1-C20 alkyl-, aryl-, C7-C20 aralkyl, and; X-Y represents an O-C(=O), an O-CH2, a CH2-C(=O), an NR<11>-C(=O) and an NR<11>-SO2 group, wherein R<11> represents hydrogen and C1-C10 alkyl. The novel compounds of formula (I) are valuable pharmaceuticals and valuable diagnostic probes for elucidating, for example, active mechanisms and biochemical, pharmacocinketic and/or pharmacodynamic processes. |
