First generation design, synthesis, and evaluation of azepine-based cryptophycin analogues.
[structure: see text] Azepine-based cryptophycin mimics (+)-4 and (+)-5 have been designed and synthesized. Biological evaluation revealed modest in vitro activity against several human tumor cell lines, thereby supporting the utility of novel scaffolds for the design and synthesis of cryptophycin analogues.
Smith
A B
AB
Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
Cho
Y S
YS
Zawacki
L E
LE
Hirschmann
R
R
Pettit
G R
GR
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001381:Azepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D000458:Cyanobacteria / Q000737:chemistry; D047630:Depsipeptides; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D001381:Azepines; D047630:Depsipeptides; D010456:Peptides, Cyclic; C088419:cryptophycin