Lipophilic analogs of sparsomycin as strong inhibitors of protein synthesis and tumor growth: a structure-activity relationship study

…, P Lelieveld, M Garzotto, DJT Wagener…

Index: Van den Broek; Lazaro; Zylicz; Fennis; Missler; Lelieveld; Garzotto; Wagener; Ballesta; Ottenheijm Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 2002 - 2015

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Citation Number: 22

Abstract

Fourteen derivatives of sparsomycin (1) were synthesized. Six of them were prepared following a novel synthetic route starting from the amino acid alanine. Some physicochemical properties, viz. lipophilicity and water solubility, of selected derivatives were measured. The biological activity was tested in vitro in cell-free protein synthesis inhibition assays, in bacterial and tumor cell growth inhibition assays, and in the L1210 ...