Abstract: The present invention relates to anti-tumor-conjugation agent-protein compounds of the general formula I: ##STR1## wherein, R.sub.1 and R.sub.2 are each independently selected from hydrogen atom, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-6 carboxyalkyl, phenyl, or phenyl substituted by at least one of hydroxy, halogen, lower alkyl, lower alkoxy, or nitro, with the proviso that R.sub.1 and R.sub.2 cannot be simultaneously a hydrogen, and when one of R.sub.1 or R.sub.2 is a hydrogen, the other one cannot be --CH.sub.2 COOH;A is the residue of an anti-tumor agent containing at least one amino group available to form an amide bound; andB is a free .epsilon.-lysine containing residue selected from a peptide or a protein.