Skip NavigationSkip to Content
Return Return to Search Results

Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides

  1. Author:
    Raffa, D.
    Maggio, B.
    Plescia, F.
    Cascioferro, S.
    Plescia, S.
    Raimondi, M. V.
    Daidone, G.
    Tolomeo, M.
    Grimaudo, S.
    Di Cristina, A.
    Pipitone, R. M.
    Bai, R.
    Hamel, E.

  2. Author Address

    [Raffa, D; Maggio, B; Plescia, F; Cascioferro, S; Plescia, S; Raimondi, MV; Daidone, G] Dipartimento Sci & Tecnol Mol & Biomol, I-90123 Palermo, Italy [Tolomeo, M; Grimaudo, S; Di Cristina, A; Pipitone, RM] Univ Palermo, Ctr Interdipartimentale Ric Oncol Clin, Palermo, Italy [Tolomeo, M; Grimaudo, S; Di Cristina, A; Pipitone, RM] Univ Palermo, Dipartimento Biomed Med Interna & Specialist, Palermo, Italy [Bai, R; Hamel, E] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA;Raffa, D (reprint author), Dipartimento Sci & Tecnol Mol & Biomol, Via Archirafi 32, I-90123 Palermo, Italy;demraffa@unipa.it
    1. Year: 2011
    2. Date: Jul
  2. Journal: European Journal of Medicinal Chemistry
    1. 46
    2. 7
    3. Pages: 2786-2796
  4. Type of Article: Article
  5. ISSN: 0223-5234
  1. Abstract:

    Several new 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides 12a-s and 17t-v were synthesized by stirring in pyridine the (E)-3-(2-R1-3-R2-4-R3-phenyl)acrylic acid chlorides 11c-k and 11t-v with the appropriate anthranilamide derivatives 10a-c or the 5-iodoanthranilic acid 13. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). COMPARE analysis, effects on tubulin polymerization in cells and with purified tubulin, and effects on cell cycle distribution for 17t, the most active of the series, indicate that these new antiproliferative compounds act as antitubulin agents. (C) 2011 Elsevier Masson SAS. All rights reserved.

    See More

  1. Keywords:

External Sources

  1. View Full Text
  2. DOI: 10.1016/j.ejmech.2011.03.067
  3. View record in Web of Science®
  4. WOS: 000291895200015

Library Notes

  1. Fiscal Year: FY2010-2011
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