| 摘要 |
PURPOSE: To obtain a conjugate which is active for therapy by bonding therapeutic active medicine molecules through a thioether-contg. linker to the ligand which can recognize selected objective cell groups. CONSTITUTION: This conjugate compd. is expressed by formula I (D is the medicine component, (n) is 1 to 10, (p) is 1 to 6, Y is O or NH Cl<-> , (z) is 0 or 1, (q) is 1 to 10, X is a ligand, A is a Michael addition adduct). This compd. is obtd., for example, by the reaction of a compd. expressed by formula II (R is a Michael addition receptor) and a compd. expressed by formula III. In the conjugate compd. above described, the medicine component is bonded to the linker through acylhydrazone, and therefore, the medicine to be used should have carbonyl groups which can form hydrazone bonds. As for the medicine component, anthracycline antibiotics, vinca alkaloids, mitomycin and cytotoxic nucleoside can be used. As for the linker, immunoglobulin, EGF, insulin, steroid, lectin, etc., can be used. |
