Skip NavigationSkip to Content
Return Return to Search Results

Synthesis and biological evaluation of 2-(3 ',4 ',5 '-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors

  1. Author:
    Romagnoli, R.
    Baraldi, P. G.
    Remusat, V.
    Carrion, M. D.
    Cara, C. L.
    Preti, D.
    Fruttarolo, F.
    Pavani, M. G.
    Tabrizi, M. A.
    Tolomeo, M.
    Grimaudo, S.
    Balzarini, J.
    Jordan, M. A.
    Hamel, E.

  2. Author Address

    Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy. Univ Palermo, Dipartimento Oncol, Policlin P Giaccone, Div Ematol, Palermo, Italy. Univ Palermo, Dipartimento Oncol, Policlin P Giaccone, Serv AIDS, Palermo, Italy. Rega Inst, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium. Univ Calif Santa Barbara, Dept Mol Cellular & Dev Biol, Santa Barbara, CA 93106 USA. Univ Calif Santa Barbara, Neurosci Res Inst, Santa Barbara, CA 93106 USA. Natl Canc Inst, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA.;Romagnoli, R, Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy.;rmr@unife.it baraldi@unife.it
    1. Year: 2006
    2. Date: Oct
  2. Journal: Journal of Medicinal Chemistry
    1. 49
    2. 21
    3. Pages: 6425-6428
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    2-(3', 4', 5'-Trimethoxybenzoyl)-3-amino-5-aryl/heteroaryl thiophene derivatives were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. SARs were elucidated with various substitutions on the aryl moiety 5-position of the thienyl ring. Substituents at the para- position of the 5-phenyl group showed antiproliferative activity in the order of F=CH3 > OCH3=Br=NO2 > CF3=I > OEt. Several of these compounds led to arrest of HL-60 cells in the G2/M phase of the cell cycle and induction of apoptosis.

    See More

  1. Keywords:

External Sources

  1. View Full Text
  2. DOI: 10.1021/jm060804a
  3. View record in Web of Science®
  4. WOS: 000241192400035

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