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2-Arylamino-4-Amino-5-Aroylthiazoles. "One-Pot" Synthesis and Biological Evaluation of a New Class of Inhibitors of Tubulin Polymerization

  1. Author:
    Romagnoli, R.
    Baraldi, P. G.
    Carrion, M. D.
    Cruz-Lopez, O.
    Cara, C. L.
    Basso, G.
    Viola, G.
    Khedr, M.
    Balzarini, J.
    Mahboobi, S.
    Sellmer, A.
    Brancale, A.
    Hamel, E.

  2. Author Address

    Romagnoli, Romeo, Baraldi, Pier Giovanni, Carrion, Maria Dora, Cruz-Lopez, Olga, Cara, Carlota Lopez] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy. [Basso, Giuseppe, Viola, Giampietro] Univ Padua, Dipartimento Pediat, Lab Oncoematol, I-35131 Padua, Italy. [Balzarini, Jan] Catholic Univ Louvain, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium. [Khedr, Mohammed, Brancale, Andrea] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3NB, S Glam, Wales. [Mahboobi, Siavosh, Sellmer, Andreas] Univ Regensburg, Fac Chem & Pharm, D-93040 Regensburg, Germany. [Hamel, Ernest] NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA.
    1. Year: 2009
  2. Journal: Journal of Medicinal Chemistry
    1. 52
    2. 17
    3. Pages: 5551-5555
  4. Type of Article: Article
  1. Abstract:

    The essential role of microtubules in mitosis makes them a major target of compounds useful for cancer therapy. In our search for potent antitumor agents, a novel series of 2-anilino-4-amino-5-aroylthiazoles was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. SAR was elucidated with various substitutions on the phenylamino and aroyl moiety at the 2- and 5-positions, respectively, of the 4-aminothiazole skeleton. Tumor cell exposure to several of these compounds led to the arrest of HeLa cells in the G2/M phase of the cell cycle and induction of apoptosis.

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  2. DOI: 10.1021/jm9001692
  3. PMID: 19663386

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