[Hemisynthesis of antineoplastic conjugates with nitrogen-mustard proteins].
The synthesis of new conjugates with inhibitory action on tumour growth is investigated by linking amino functions of proteins compounds (lysozyme and alpha s-casein) through an amide linkage at the carboxylic function of nitrogen mustards (chlorambucil and melphalan). The polychlorambucil amides of lysozyme and alpha s-casein derivatives prepared showed experimental antitumour activity when these conjugates were screened against the experimental P388 leukemia. In the case of the conjugates lysozyme-melphalan, an antitumour activity is observed when the amino function of the drug is combined with the carboxylic functions of the protein contrary to the situation of the free amino function of the drug described into the literature.
Comité pour la Promotion de la Recherche, Scientifique au CERIA, Service des Substances Naturelles, Bruxelles.
R R
RR
Smolders
F
F
Jacquemotte
S
S
Godart
I
I
Legentil
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002364:Caseins; D007941:Leukemia P388 / Q000188:drug therapy; D008466:Mechlorethamine / Q000031:analogs & derivatives / Q000138:chemical synthesis*; D051379:Mice; D009113:Muramidase; D011506:Proteins / Q000032:analysis
D000970:Antineoplastic Agents; D002364:Caseins; D011506:Proteins; D008466:Mechlorethamine; D009113:Muramidase
Hémisynthèse de conjugués oncostatiques du type moutardes azotées-protéines.