title: Synthesis and biological property of carba and 20-deoxo analogues of arenastatin A.
abstract: The carba analogue, in which a methylene group is substituted for the oxygen atom linked to C-15, and 20-deoxo analogue of arenastatin A, a potent cytotoxic spongean depsipeptide, were synthesized. Both analogues lacking the 15,20-ester function, which was easily metabolized in serum, showed good stability in serum as well as moderate cytotoxic activity against KB cells and better solubility.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Murakami
authors.forename: W
authors.initials: W
authors.lastname: Wang
authors.forename: S
authors.initials: S
authors.lastname: Tamura
authors.forename: M
authors.initials: M
authors.lastname: Kobayashi
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D003500:Cyclization; D047630:Depsipeptides; D004355:Drug Stability; D006801:Humans; D007624:KB Cells; D051379:Mice; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*
chemical_list: C418103:15-carbaarenastatin A; C418104:20-deoxoarenastatin A; D000970:Antineoplastic Agents; D047630:Depsipeptides; D010456:Peptides, Cyclic; C096566:arenastatin A