POLYMER-BOUND CAMPTOTHECIN DERIVATIVES.

摘要

A POLYMERIC CONJUGATE CONSISTS ESSENTIALLY OF:@i) FROM 60 TO 99 MOL OF N-(2-HYDROXYPROPYL) METHACRYLOYLAMIDE UNITS REPRESENTED BY FORMULA 1: ii) FROM 1 TO 40 MOL OF 20-0-(N-METHACRYLOYLGLYCYL-AMINOACYL) CAMPTOTHECIN UNITS REPRESENTED BY FORMULA 2 WHEREIN [A] IS A SPACER GROUP HAVING RESPECTIVE TERMINAL AMINO AND CARBONYL GROUPS WHICH ARE SEPARATED BY AT LEAST THREE ATOMS AND O-CPT REPRESENTS A RESIDUE OF A CAMPTOTHECIN, THE C-20 HYDROXY GROUP OF THE CAMPTOTHECIN BEING LINKED TO THE TERMINAL CARBONYL GROUP OF THE SPACER GROUP [A]; AND @iii) FROM 0 TO 10 MOL OF N-METHACRYLOYLGLYCINE OR N-(2-HYDROXY-PROPYL)METHACRYLOYLGLYCINAMIDE UNITS REPRESENTED BY FORMULA 3: WHEREIN Z REPRESENTS HYDROXY OR A RESIDUE OF FORMULA -NH-CH2-CH(OH)-CH3.