| 摘要 |
Novel bridged vinca dimers are described, of the following formula;… R-NH-CH2-(CH2)n-X-(CH2)n-CH2-NH-R… wherein each R is the same or different residue of an indole-dihydroindole alkaloid of the general formula: …<CHEM>… wherein… R<1> is OH or O-CO-CH3;… R<2> is CH3, H or CHO:… when taken singly, one of R<3> and R<4> is H or OH, and the other is C2H5, and R<5> is H; and when R<4> and R<5> are taken together, they form an alpha -epoxide ring and R<3> is C2H5;… X is S, O, Se-Se, NH, N-[(CH2)m -CH2-NH-R] or (CH2)p wherein p and each n are 0, 1, 2, 3 or 4; and m is 1 or 2; and… pharmaceutically-acceptable acid addition salts thereof. …<??>The compounds are useful pharmaceuticals especially as oncolytic agents. They are prepared by reacting the corresponding azide of an indole-dihydronidole alkaloid with an appropriate diamine or triamine. Some of the intermediates employed in this preparation are novel, namely those having the structure:… R<6>-NH-CH2-(CH2)n-Q min -(CH2)n-CH2-NH2 where R<6> is the group R defined above in which R<1> is OH and R<2> is CH3 or H, and Q min is S, S-S, Q, Se-Se, or (CH2)p where n and p is 0, 1, 2, 3 or 4. |
