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  • Title: Synthesis and biological activity of spergualin analogues. I.
    Author: Nishizawa R, Takei Y, Yoshida M, Tomiyoshi T, Saino T, Nishikawa K, Nemoto K, Takahashi K, Fujii A, Nakamura T.
    Journal: J Antibiot (Tokyo); 1988 Nov; 41(11):1629-43. PubMed ID: 3242505.
    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 immunosuppressive 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.
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