ANTITUMOR-ACTIVITY OF NEW SEMISYNTHETIC SAFRAMYCIN DERIVATIVES

  • 1 October 1986
    • journal article
    • research article
    • Vol. 77  (10) , 1043-1049
Abstract
Saframycins Yd-1 and Y3, which have an amino functional group in the side chain, were recently obtained by a directed biosynthesis. Twenty-eight side chain-modified chemical derivatives were prepared from these saframycins, and their in vitro and in vivo antitumor activities were studied. Among these new derivatives, three saframycins, namely, two N-acyl derivatives, pivaloyl- and n-caproylsaframycin Y3, and one water-soluble type, saframycin Yd-1 .cntdot. HCL, were sound to show marked activity against L1210 mouse leukemia cells. Further studies of these saframycin derivatives using B16-F10 melanoma and Lewis lung carcinoma indicated that all three saframycins are also active against B-16-F10 melanoma; saframycin Yd-1 .cntdot. HCl showed the greatest prolongation of survival time. Marked inhibition of spontaneous metastasis of Lewis lung carcinoma was observed in mice treated with these new derivatives. Structure-activity relationships among these semisynthetic saframycins are discussed.

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