title: A concise route to the macrocyclic core of the rakicidins.
abstract: An efficient synthesis of the macrolactone core of the rakicidins is described. The rakicidins are cytotoxic lipopeptides with interesting cancer cell selectivities including HIF-1-independent hypoxia-selective cytotoxicity and anti-invasive activity. Access to the core may now allow establishment of preliminary SAR and exploration of routes to several members of rakicidins.
authors: Department of Chemistry, Aarhus University, Langelandsgade 140, 8000 Aarhus C, Denmark. thpou@chem.au.dk
authors: Thomas B
authors: TB
authors: Poulsen
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D015687:Cell Hypoxia / Q000187:drug effects; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D051793:Hypoxia-Inducible Factor 1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D055666:Lipopeptides / Q000737:chemistry*; D047028:Macrocyclic Compounds / Q000737:chemistry*; D010456:Peptides, Cyclic / Q000737:chemistry*; D047630:Depsipeptides
chemical_list: D000970:Antineoplastic Agents; D051793:Hypoxia-Inducible Factor 1; D055666:Lipopeptides; D047028:Macrocyclic Compounds; D010456:Peptides, Cyclic; C000723972:rakicidins; D047630:Depsipeptides