Design and synthesis of highly potent fumagillin analogues from homology modeling for a human MetAP-2

New fumagillin analogues were designed through structure-based molecular modeling with a human methionine aminopeptidase-2. Among the fumagillin analogues, cinnamic acid ester derivative CKD-731 showed 1000-fold more potent proliferation inhibitory activity on endothelial cell than TNP-470.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-01, Vol.10 (1), p.39-43
Hauptverfasser:	Han, C K, Ahn, S K, Choi, N S, Hong, R K, Moon, S K, Chun, H S, Lee, S J, Kim, J W, Hong, C I, Kim, D, Yoon, J H, No, K T
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Aminopeptidases - chemistry Angiogenesis Inhibitors - chemical synthesis Angiogenesis Inhibitors - chemistry Angiogenesis Inhibitors - pharmacology Animals Antineoplastic agents Biological and medical sciences Cattle Cell Line Cinnamates - chemical synthesis Cinnamates - pharmacology Cyclohexanes Drug Design Epoxy Compounds - chemical synthesis Epoxy Compounds - pharmacology Fatty Acids, Unsaturated - chemical synthesis Fatty Acids, Unsaturated - pharmacology General aspects Growth Inhibitors - pharmacology Humans Leukemia P388 - pathology Medical sciences Metalloendopeptidases - chemistry Mice Models, Molecular Molecular Sequence Data Pharmacology. Drug treatments Sequence Homology, Amino Acid Sesquiterpenes Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	New fumagillin analogues were designed through structure-based molecular modeling with a human methionine aminopeptidase-2. Among the fumagillin analogues, cinnamic acid ester derivative CKD-731 showed 1000-fold more potent proliferation inhibitory activity on endothelial cell than TNP-470.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(99)00577-6