Design, synthesis and biological evaluation of novel, simplified analogues of laulimalide: modification of the side chain.

Abstract

Novel, simplified analogues of the microtubule-stabilizing anticancer agent laulimalide, including the first derivatives with unnatural side chains, were designed by molecular modelling, synthesized by a late-stage diversification strategy, and evaluated in vitro for growth inhibition of human ovarian carcinoma cell lines (A2780, A2780/AD10).

• Authors: Ian Paterson, Dirk Menche, Anders E Håkansson, Adrian Longstaff, David Wong, Isabel Barasoain, Rubén M Buey, J Fernando Díaz
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 15 Issue 9 Pg. 2243-7 (May 02 2005) ISSN: 0960-894X [Print] England
• PMID: 15837302 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Macrolides
• Taxoids
• laulimalide

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Division (drug effects)
• Cell Line, Tumor
• Drug Design
• Female
• Humans
• Macrolides
• Models, Molecular
• Molecular Conformation
• Molecular Structure
• Ovarian Neoplasms
• Structure-Activity Relationship
• Taxoids (chemical synthesis, chemistry, pharmacology)