title: Improved total synthesis and structure-activity relationship of arenastatin A, a potent cytotoxic spongean depsipeptide.
abstract: An efficient asymmetric synthesis of a cyclic depsipeptide arenastatis A (1) is described. 1, isolated from the marine sponge Dysidea arenaria, exhibited extremely potent cytotoxicity with IC50 of pg/ml for KB cells, and in this context the structure-activity relationship among several stereoisomers of 1 and allied compounds has also been examined.
authors.affiliation: Faculty of Pharmaceutical Sciences, Osaka University, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Kobayashi
authors.forename: W
authors.initials: W
authors.lastname: Wang
authors.forename: N
authors.initials: N
authors.lastname: Ohyabu
authors.forename: M
authors.initials: M
authors.lastname: Kurosu
authors.forename: I
authors.initials: I
authors.lastname: Kitagawa
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D047630:Depsipeptides; D006801:Humans; D007624:KB Cells; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D011161:Porifera / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; D010456:Peptides, Cyclic; C096566:arenastatin A