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Benzoylphenylurea sulfur analogues with potent antitumor activity

  1. Author:
    Hallur, G.
    Jimeno, A.
    Dalrymple, S.
    Zhu, T.
    Jung, M. K.
    Hidaleo, M.
    Isaacs, J. T.
    Sukumar, S.
    Hamel, E.
    Khan, S. R.
  2. Author Address

    Sidney Kimmel Comprehens Canc Ctr Johns Hopkins, Div Chem Therapeut, Baltimore, MD 21231 USA. NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diagnosis,NIH, Frederick, MD 21702 USA. SAIC Frederick Inc, NCI, Frederick, MD 21702 USA.;Khan, SR, Sidney Kimmel Comprehens Canc Ctr Johns Hopkins, Div Chem Therapeut, Baltimore, MD 21231 USA.;khansa@jhmi.edu
    1. Year: 2006
    2. Date: Apr
  1. Journal: Journal of Medicinal Chemistry
    1. 49
    2. 7
    3. Pages: 2357-2360
  2. Type of Article: Article
  3. ISSN: 0022-2623
  1. Abstract:

    A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to10-fold increased potency, when compared to I (NSC-639829), against cancer cell lines. 6n was more effective than I in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 mu M.

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External Sources

  1. DOI: 10.1021/jm051261s
  2. WOS: 000236593300025

Library Notes

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