Arylthioindole Tubulin Polymerization Inhibitors and Methods of Treating or Preventing Cancer Using Same
Description of Invention:
Microtubules are involved in a variety of cellular functions including motility, division, shape maintenance, and intracellular transport. Tubulin is the major protein component in microtubules, and interference with microtubule assembly leads to an increase of cells in metaphase arrest. Inhibition of microtubule function using tubulin targeted agents are widely used in the treatment of cancer.
This invention describes novel arylthioindole derivatives, 3-arylthioindole-2-carboxylic acid esters derivatives, having excellent affinity for tubulin and excellent efficacy as inhibitors of the growth of MCF-7 breast cancer cells. These new chemical compounds have the potential to result in more effective therapeutics for the treatment of neoplastic diseases.
Applications:
Therapeutic for proliferative diseases such as cancer
Market:
600,000 deaths from cancer related diseases estimated in 2006
Development Status:
The technology is currently in the pre-clinical stage of development.
Inventors:
Ernest Hamel (NCI) et al.
Patent Status:
DHHS Reference No. E-323-2004/0 --
U.S. Provisional Application No. 60/616,347 filed 05 Oct 2004
PCT Application No. PCT/US2005/035896 filed 05 Oct 2005
Relevant Publication:
G De Martino, MC Edler, G La Regina, A Coluccia, MC Barbera, D Barrow, RI Nicholson, G Chiosis, A Brancale, E Hamel, M Artico, R Silvestri. New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationship and molecular modeling studies. J Med Chem. 2006 Feb 9;49(3):947-954. [PubMed abs]
G De Martino, G La Regina, A Coluccia, MC Edler, MC Barbera, A Brancale, E Wilcox, E Hamel, M Artico, R Silvestri. Arylthioindoles, potent inhibitors of tubulin polymerization. J Med Chem. 2004 Dec 2;47(25):6120-6123. [PubMed abs]
Licensing Status: Available for exclusive or non-exclusive licensing.
Portfolios: Cancer
Cancer -Therapeutics-Biological Response Modifiers Cancer -Therapeutics-Immunomodulators and Immunostimulants Cancer -Therapeutics
For Additional Information Please Contact: Jennifer Wong
NIH Office of Technology Transfer
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Phone: (301)435-4633
Email: wongje@mail.nih.gov
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