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New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies

  1. Author:
    La Regina, G.
    Sarkar, T.
    Bai, R. L.
    Edler, M. C.
    Saletti, R.
    Coluccia, A.
    Piscitelli, F.
    Minelli, L.
    Gatti, V.
    Mazzoccoli, C.
    Palermo, V.
    Mazzoni, C.
    Falcone, C.
    Scovassi, A. I.
    Giansanti, V.
    Campiglia, P.
    Porta, A.
    Maresca, B.

  2. Author Address

    La Regina, Giuseppe, Piscitelli, Francesco, Minelli, Lara, Gatti, Valerio, Mazzoccoli, Carmela, Silvestri, Romano] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farmaco, Inst Pasteur, Fdn Cenci Bolognetti, I-00185 Rome, Italy. [Saletti, Roberto, Coluccia, Antonio, Brancale, Andrea] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3NB, S Glam, Wales. [Sarkar, Taradas, Bai, Ruoli, Edler, Michael C.; Hamel, Ernest] NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA. [Novellino, Ettore] Univ Naples Federico 2, Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy. [Scovassi, Anna Ivana, Giansanti, Vincenzo] CNR, Ist Genet Mol, I-27100 Pavia, Italy. [Palermo, Vanessa, Mazzoni, Cristina, Falcone, Claudio] Univ Roma La Sapienza, Dipartimento Biol Cellulare & Sviluppo, I-00185 Rome, Italy. [Campiglia, Pietro] Univ Salerno, Dipartimento Sci Farmaceut, Sez Chim Tecnol, I-84084 Salerno, Italy. [Porta, Amalia, Maresca, Bruno] Univ Salerno, Dipartimento Sci Farmaceut, Sez Biomed, I-84084 Salerno, Italy. [Mazzoccoli, Carmela] Ctr Riferimento Oncol Basilicata, Ist Ricovero & Cura Carattere Sci, I-85028 Potenza, Italy.
    1. Year: 2009
  2. Journal: Journal of Medicinal Chemistry
    1. 52
    2. 23
    3. Pages: 7512-7527
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    New arylthioindoles along with the corresponding ketone and methylene compounds were potent tubulin assembly inhibitors. As growth inhibitors of MCF-7 cells, sulfur derivatives were superior or sometimes equivalent to the ketones, while methylene derivatives were substantially less effective. Esters 24, 27-29, 36, 39, and 41 showed similar to 50% of inhibition oil human HeLa and HCT116/chr3 cells at 0.5 mu M, and these compounds inhibited the growth of HEK, M 14, and U937 cells with IC50'S ill the 78220 nM range. While murine macrophage J744.1 cell growth was significantly less affected (20% at higher concentrations), four other nontransformed cell lines remained sensitive to these esters. The effect of drug treatment oil cell morphology was examined by time-lapse microscopy. In a protocol set up to evaluate toxicity on the Saccharomyces cerevisiae BY4741 wild type strain, compounds 24 and 54 strongly reduced cell growth, and 29, 36, and 39 also showed significant inhibition.

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  2. DOI: 10.1021/jm900016t
  3. PMID: 19601594

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