Structurally simplified macrolactone analogues of halichondrin B

Structurally simplified macrolactone analogues of halichondrin B (e.g., 47, IC 50 = 0.67 nM) were identified that retain the potent cell growth inhibitory activity of the natural product in vitro. A structurally simplified macrolactone analogue of halichondrin B was identified that retains the poten...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-11, Vol.14 (22), p.5547-5550
Main Authors: Seletsky, Boris M., Wang, Yuan, Hawkins, Lynn D., Palme, Monica H., Habgood, Gregory J., DiPietro, Lucian V., Towle, Murray J., Salvato, Kathleen A., Wels, Bruce F., Aalfs, Kimberley K., Kishi, Yoshito, Littlefield, Bruce A., Yu, Melvin J.
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Biological and medical sciences
Cell Division - drug effects
Cell Line, Tumor
Ethers, Cyclic - chemical synthesis
Ethers, Cyclic - chemistry
Ethers, Cyclic - pharmacology
General aspects
Humans
Lactones - chemical synthesis
Lactones - chemistry
Lactones - pharmacology
Macrolides
Medical sciences
Molecular Conformation
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary:Structurally simplified macrolactone analogues of halichondrin B (e.g., 47, IC 50 = 0.67 nM) were identified that retain the potent cell growth inhibitory activity of the natural product in vitro. A structurally simplified macrolactone analogue of halichondrin B was identified that retains the potent cell growth inhibitory activity of the natural product in vitro.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.08.068