Phase I study of beta-alanyl-melphalan as a potent anticancer drug.
The dipeptide beta-alanyl-melphalan was synthesized and tested for its potential anticancer activity. It is shown to possess considerable toxicity toward Ehrlich ascites tumor cells and 3T3 mouse embryo cells in in vitro toxicity assays and is a potent anticancer agent when used in vivo in traditional phase I chemotherapy assays. The potential role for small peptide transport mechanisms in transportation of anticancer agents is discussed.
D000818:Animals; D000970:Antineoplastic Agents; D002286:Carcinoma, Ehrlich Tumor / Q000473:pathology; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004151:Dipeptides / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D008558:Melphalan / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D051379:Mice
D000970:Antineoplastic Agents; D004151:Dipeptides; C052608:beta-alanylmelphalan; D008558:Melphalan