Synthesis and biological activity of spergualin analogues. I.

Publisher Website
Google Scholar
Abstract
Stable spergualin analogues were synthesized by substitutions of the .alpha.-hydroxyglycine residue of spergualin with various .alpha.- or .omega.-amino acids. The antitumor activity of these analogues against L1210 and their immunosppressive effects on delayed-type hypersensitivity and antibody formation was then examined. Analogues substituted with glycine and L-serine showed significant biological activity but were less potent than 15-deoxyspergualin. Among the analogues synthesized so far, 10-[N-4-(4-guanidinophenyl)butyryl-L-seryl]-1,5,10-triazadecane has possessed the strongest antitumor and immunosuppressive activities.