The development of sparsomycin as an anti-tumour drug
Ottenheijm, H.C.; van den Broek, L.A.
Anti-Cancer Drug Design 2(4): 333-337
1988
ISSN/ISBN: 0266-9536 PMID: 3365303 Document Number: 305743
The synthesis of sparsomycin and eight lipophilic analogues is discussed. Sparsomycin, a bacterial metabolite, is a potent inhibitor of protein biosynthesis; in addition it has anti-tumour properties. Structure-activity relationship studies indicate that the anti-tumour activity is a direct consequence of the inhibition of protein synthesis. Two of the analogues show a higher anti-tumour activity in vitro as well as in vivo, and are less toxic to mice than sparsomycin. Finally, some properties of sparsomycin are discussed: the drug potentiates the cytotoxicity of cisplatin and is selectively active on tumour cells without affecting human bone-marrow.