Synthesis of sparsomycin analogs as potential antitumor agents.
No information is available on the structural requirements for the antitumor activity of sparsomycin, an antibiotic obtained from the fermentation broth of Streptomyces sparsogenes. Its high in vivo and in vitro activity, novel structure, and uncommon mode of action have, therefore, suggested the synthesis of analogs. This report describes the preparation and screening of a series of N-substituted 3-aryl acrylamides which are closely related to sparsomycin. Three compounds exhibited some tumor inhibition but insufficient to warrant further testing.
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000031:analogs & derivatives*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D002279:Carcinoma 256, Walker / Q000188:drug therapy; D004353:Drug Evaluation, Preclinical; D007939:Leukemia L1210 / Q000188:drug therapy; D007942:Leukemia, Experimental / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D013033:Sparsomycin / Q000031:analogs & derivatives* / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000903:Antibiotics, Antineoplastic; D000970:Antineoplastic Agents; D013033:Sparsomycin