Epothilone analogs

• US 6,441,186 B1
• Filed: 09/04/1997
• Issued: 08/27/2002
• Est. Priority Date: 12/13/1996
• Status: Expired due to Fees

• Current Assignee: The Scripps Research Institute
• Original Assignee: The Scripps Research Institute
• Inventors: Sarabia, Francisco, Yang, Zhen, Roschangar, Frank, Pastor, Joaquin, Vourloumis, Dionisios, He, Yun, Ninkovic, Sacha, Winssinger, Nicolas, Nicolaou, Kyriacos C., Vallberg, Hans, Finlay, M. Ray, King, N. Paul
• Primary Examiner(s): STOCKTON, LAURA LYNNE
• Application Number:
  US08/923,869
• Time in Patent Office: 1,818 Days
• Field of Search: 549/562, 548/204, 548/236
• US Class Current: 548/204
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07D 313/00 Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
• CPC Class Codes: C07D 417/06 linked by a carbon chain containing only aliphatic carbon atoms
• CPC Class Codes: C07D 493/04 Ortho-condensed systems

Abstract

Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancer agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the anlogs are demonstrated to have a superior cytotoxic activities as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.

Claims

1. An epothilone analog represented by the following structure: