title: Structure--activity relationships of side-chain modified didemnins.
abstract: The synthesis and antitumor activity of a novel didemnin B analogue containing a psi[CH2NH] amide bond surrogate between N-Me-D-Leu7 and Pro8 are reported. The analogue shows activity (GI50 = 4 nM) comparable to that of didemnin B (GI50 = 13 nM) in the NCI-60 tumor cell screen. This result, along with new data from previously reported synthetic didemnin analogues, is discussed within the context of the side-chain SAR for didemnins.
authors.affiliation: Department of Chemistry, University of Pennsylvania, Philadelphia 19104-6323, USA.
authors.forename: X
authors.initials: X
authors.lastname: Ding
authors.forename: M D
authors.initials: MD
authors.lastname: Vera
authors.forename: B
authors.initials: B
authors.lastname: Liang
authors.forename: Y
authors.initials: Y
authors.lastname: Zhao
authors.forename: M S
authors.initials: MS
authors.lastname: Leonard
authors.forename: M M
authors.initials: MM
authors.lastname: Joullié
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D047630:Depsipeptides; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D018716:Molecular Mimicry; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; D010456:Peptides, Cyclic; C030051:didemnins