Skip NavigationSkip to Content
Return Return to Search Results

Synthesis and biological evaluation of 1-methyl-2-(3 ',4 ',5 '-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors

  1. Author:
    Romagnoli, R.
    Baraldi, P. G.
    Sarkar, T.
    Carrion, M. D.
    Cara, C. L.
    Cruz-Lopez, O.
    Preti, D.
    Tabrizi, M. A.
    Tolomeo, M.
    Grimaudo, S.
    Di Cristina, A.
    Zonta, N.
    Balzarini, J.
    Brancale, A.
    Hsieh, H. P.
    Hamel, E.

  2. Author Address

    Romagnoli, Romeo, Baraldi, Pier Giovanni, Carrion, Maria Dora, Cara, Carlota Lopez, Cruz-Lopez, Olga, Preti, Delia, Tabrizi, Mojgan Aghazadeh] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy. [Tolomeo, Manlio, Grimaudo, Stefania, Di Cristina, Antonella] Univ Palermo, Dipartimento Oncol, Policlin P Giaccone, Div Ematol & Serv AIDS, Palermo, Italy. [Balzarini, Jan] Catholic Univ Louvain, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium. [Zonta, Nicola, Brancale, Andrea] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales. [Hsieh, Hsing-Pang] Natl Hlth Res Inst, Div Biotechnol & Pharmaceut Res, Miaoli, Taiwan. [Sarkar, Taradas, Hamel, Ernest] NCI Frederick, Div Canc Treatment & Diag, NIH, Dev Therapeut Program,Toxicol & Pharmacol Branch, Frederick, MD 21702 USA.
    1. Year: 2008
  2. Journal: Journal of Medicinal Chemistry
    1. 51
    2. 5
    3. Pages: 1464-1468
  4. Type of Article: Article
  1. Abstract:

    The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compounds modified with respect to positions C-4 to C-7 with different moieties (chloro, methyl, or methoxy). Additional structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as methyl or ethyl. We have identified 1-methyl-2-(3,4,5-trimethoxybenzoyl)-3-amino-7-methoxyindole as a new highly potent anti proliferative agent that targets tubulin at the colchicine binding site and leads to apoptotic cell death.

    See More

  1. Keywords:

External Sources

  1. PMID: 18260616

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