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Synthesis and Biological Activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyri midin-4-aminium Chloride as Potent Cytotoxic Antitubulin Agents

  1. Author:
    Ganglee, A.
    Zhao, Y.
    Hamel, E.
    Westbrook, C.
    Mooberry, S. L.

  2. Author Address

    [Ganglee, A; Zhao, Y] Duquesne Univ, Grad Sch Pharmaceut Sci, Div Med Chem, Pittsburgh, PA 15282 USA. [Hamel, E] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA. [Westbrook, C; Mooberry, SL] Univ Texas Hlth Sci Ctr San Antonio, Dept Pharmacol, San Antonio, TX 78229 USA.;Ganglee, A (reprint author), Duquesne Univ, Grad Sch Pharmaceut Sci, Div Med Chem, 600 Forbes Ave, Pittsburgh, PA 15282 USA;gangjee@duq.edu mooberry@uthscsa.edu
    1. Year: 2011
    2. Date: Sep
  2. Journal: Journal of Medicinal Chemistry
    1. 54
    2. 17
    3. Pages: 6151-6155
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    (R,S)-1 is a potent antimitotic compound. (R)-1 center dot HCl and (S)-1 center dot HCl were synthesized from (R)- and (S)-3-methyladipic acid. Both enantiomers were potent inhibitors of cell proliferation and caused cellular microtubule loss and mitotic arrest. They inhibited purified tubulin assembly and the binding of [(3)H]colchicine to tubulin, with (S)-1 being about twice as potent. Cytotoxicity against 60 tumor cell lines, however, indicated that the (S)-isomer was 10- to 88-fold more potent than the (R)-isomer.

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External Sources

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  2. DOI: 10.1021/jm2007722
  3. View record in Web of Science®
  4. WOS: 000294385700016

Library Notes

  1. Fiscal Year: FY2011-2012
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