Leptostatin: a synthetic hybrid of the cytotoxic polyketides callystatin A and leptomycin B.
Four stereoisomeric hybrids of the polyketide natural products callystatin A and leptomycin B have been prepared by parallel synthetic routes involving chiral allenylstannane methodology. Like their natural counterparts, these hybrids exhibit nanomolar levels of cytotoxicity toward HCT-116 human colon cancer cells.
Marshall
James A
JA
Department of Chemistry, University of Virginia, Charlottesville, VA 22904, USA. jam5x@virginia.edu
Mikowski
Ann M
AM
Bourbeau
Matthew P
MP
Schaaf
Gregory M
GM
Valeriote
Frederick
F
D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D005231:Fatty Acids, Unsaturated / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008968:Molecular Conformation; D013237:Stereoisomerism
D005231:Fatty Acids, Unsaturated; C421091:callystatin A; C508200:leptostatin; C038753:leptomycin B