Skip NavigationSkip to Content
Return Return to Search Results

Synthesis of Analogs of 2-Methoxyestradiol With Enhanced Inhibitory Effects On Tubulin Polymerization and Cancer Cell Growth

  1. Author:
    Cushman, M.
    He, H. M.
    Katzenellenbogen, J. A.
    Varma, R. K.
    Hamel, E.
    Lin, C. M.
    Ram, S.
    Sachdeva, Y. P.

  2. Author Address

    Cushman M PURDUE UNIV SCH PHARM & PHARMACAL SCI DEPT MED CHEM & MOL PHARMACOL W LAFAYETTE, IN 47907 USA UNIV ILLINOIS DEPT CHEM URBANA, IL 61801 USA NCI DRUG SYNTH & CHEM BRANCH DEV THERAPEUT PROGRAM DIV CANC TREATMENT DIAG & CTR ROCKVILLE, MD 20852 USA NCI FREDERICK CANC RES & DEV CTR LAB DRUG DISCOVERY RES & DEV DEV THERAPEUT PROGRAM FREDERICK, MD 21702 USA PHARM ECO LABS INC LEXINGTON, MA 02173 USA
    1. Year: 1997
  2. Journal: Journal of Medicinal Chemistry
    1. 40
    2. 15
    3. Pages: 2323-2334
  4. Type of Article: Article
  1. Abstract:

    A new series of estradiol analogs was synthesized in an attempt to improve on the anticancer activity of 2-methoxyestradiol, a naturally occurring mammalian tubulin polymerization inhibitor. The compounds were evaluated as inhibitors of tubulin polymerization and the binding of [H-3]colchicine to tubulin, as well as for in vitro cytotoxicity in human cancer cell cultures. Overall, the most potent of the new compounds were 2-(2',2',2'-trifluoroethoxy)-6-oximinoestradiol, 2-ethoxy-6-oximinoestradiol, and 2-ethoxy-6-methoximinoestradiol. These agents lacked significant affinity for the estrogen receptor. The cytotoxicities of the compounds correlated in general with their abilities to inhibit tubulin polymerization, thus supporting inhibition of tubulin polymerization as the primary mechanism causing inhibition of cell growth. [References: 46]

    See More

  1. Keywords:

External Sources

  1. No sources found.

Library Notes

  1. No notes added.
NCI at Frederick

You are leaving a government website.

This external link provides additional information that is consistent with the intended purpose of this site. The government cannot attest to the accuracy of a non-federal site.

Linking to a non-federal site does not constitute an endorsement by this institution or any of its employees of the sponsors or the information and products presented on the site. You will be subject to the destination site's privacy policy when you follow the link.

ContinueCancel