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Kansas State University

Research Foundation
Kansas State University
2005 Research Park Circle
Suite 105
Manhattan, KS 66502-5020
Tel: 785-532-5720
Fax: 785-532-3920
tech.transfer@k-state.edu

Tricyclic and Tetracylic Pyrones

Reference Number: 97-01 & 99-11

Inventors: Duy Hua and Jean-Pierre Perchellet

Description

A new class of compounds has been synthesized based on a polycyclic pyrone (PP) structure.

Performance

These compounds exhibit inhibitory properties against two major diseases.

  • Cancer
    • Preventing DNA synthesis by blockage of nucleosides cellular transport. This characteristic is reversible upon drug removal
    • Inhibiting cell growth in an irreversible and long-term fashion
    • Inhibiting cell growth in an irreversible and long-term fashion
    • Inhibiting cell growth in an irreversible and long-term fashion
    • Blocking mammalian cells in M-phase
    • Inhibiting tubulin polymerization in a similar fashion to vincristine, another microtubule-destabilizing drug
    • In vivo, water-soluble PP-HCI reduced tumor weight by up to 67% in mice inoculated with Lewis lung carcinoma cells
  • Alzheimer’s disease: Alzheimer’s disease is characterized by the deposition of the amyloid protein as plaques in certain region of the brain. KSU investigators have shown that the over expression of the amyloid protein precursor in transformed MC-65 cells induces cell death. This effect can be inhibited by addition of the PP compounds.

    In addition, the PP compounds have inhibitory properties against the enzyme acetylcholinesterase.

Application

The PP compounds have therefore some definite therapeutic potentials against cancer, Alzheimer’s disease can be of interest for the pharmaceutical industry. For that purpose, these compounds can be produced in high yield in a minimal number of reaction steps and can be adapted for drug delivery.

Patent Status

  • U.S. Patent #6,384,045 issued on May 7, 2002
  • U.S. Patent #6,828,450 issued on December 7, 2004

Interested parties should contact:

National Institute for Strategic Technology Acquisition and Commercialization (NISTAC)
2005 Research Park Circle Manhattan, KS 66502
Tel: 785-532-3900 Fax: 785-532-3909
E-Mail: nistac@ksu.edu