B-Homoestra-1,3,5(10)-trienes as Modulators of Tubulin Polymerization
Description of Invention:
This invention relates to the general field of steroid chemistry, particularly to estrone derivatives. Specifically, this invention provides B-ring expanded estra-1,3,5(10)-triene compounds of general formula which modulate the polymerization of tubulin and/or the depolymerization of microtubules. Successful cell division, as a step of cell mitosis, depends on the proper polymerization of tubulin and the proper depolymerization of microtubules. This invention also relates to methods of using the compounds as anti-mitotic, anti-angiogenic and anti-tumor therapeutics for the treatment of cancer or other mammalian diseases characterized by undesirable angiogenesis. Additionally, the invention provides methods of preparing the compounds. The compounds of the invention are also expected to have utility as research tools.
Inventors:
Ernest Hamel et al. (NCI)
Patent Status:
DHHS Reference No. E-230-1999/0 --
U.S. Patent No. 6,696,436 issued 24 Feb 2004
Relevant Publication:
Verdier-Pinard et al., “A Steroid Derivative With Paclitaxel-Like Effects on Tubulin Polymerization,” Mol. Pharmacol. 2000 Mar, 57(3):568-575
Wang et al., “Synthesis of B-ring Homologated Estradiol Analogues that Modulate Tubulin Polymerization and Microtubule Stability,” J. Med. Chem. 2000 Jun 15, 43(12):2419-2429
Portfolios: Cancer
Cancer -Therapeutics-Conventional Chemotherapy-Hormonal Compounds Cancer -Therapeutics
For Additional Information Please Contact: Adaku Nwachukwu J.D.
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: 301 435-5560
Email: madua@mail.nih.gov
Fax: 301 402-0220
