Skip NavigationSkip to Content
Return Return to Search Results

Design, synthesis, and biological evaluation of thiophene analogues of chalcones

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

  2. Author Address

    Romagnoli, Romeo, Baraldi, Pier Giovanni, Carrion, Maria Dora, Cara, Carlota Lopez, Cruz-Lopez, Olga, Preti, Delia] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy. [Tolomeo, Manlio, Grimaudo, Stefania, Di Cristina, Antonella] Univ Palermo, Dept Oncol, Policlin P Giaccone, Div Ematol, Palermo, Italy. [Tolomeo, Manlio, Grimaudo, Stefania, Di Cristina, Antonella] Univ Palermo, Dept Oncol, Policlin P Giaccone, AIDS Serv, Palermo, Italy. [Zonta, Nicola, Brancale, Andrea] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10, Wales. [Balzarini, Jan] Rega Inst, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium. [Sarkar, Taradas, Hamel, Ernest] NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA.
    1. Year: 2008
  2. Journal: Bioorganic & Medicinal Chemistry
    1. 16
    2. 10
    3. Pages: 5367-5376
  4. Type of Article: Article
  1. Abstract:

    Chalcones are characterized by possessing an enone moiety between two aromatic rings. A series of chalcone-like agents, in which the double bond of the enone system is embedded within a thiophene ring, were synthesized and evaluated for antiproliferative activity and inhibition of tubulin assembly and colchicine binding to tubulin. The replacement of the double bond with a thiophene maintains antiproliferative activity and therefore must not significantly alter the relative conformation of the two aryl rings. The synthesized compounds were found to inhibit the growth of several cancer cell lines at nanomolar to low micromolar concentrations. In general, all compounds having significant antiproliferative activity inhibited tubulin polymerization with an IC50 < 2 mu M. Several of these compounds caused K562 cells to arrest in the G2/M phase of the cell cycle. (C) 2008 Elsevier Ltd. All rights reserved.

    See More

  1. Keywords:

External Sources

  1. PMID: 18440234

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