2. Academic Validation
  3. 2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization

2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization

  • J Med Chem. 2009 Sep 10;52(17):5551-5. doi: 10.1021/jm9001692.
Romeo Romagnoli 1,  Pier Giovanni Baraldi,  Maria Dora Carrion,  Olga Cruz-Lopez,  Carlota Lopez Cara,  Giuseppe Basso,  Giampietro Viola,  Mohammed Khedr,  Jan Balzarini,  Siavosh Mahboobi,  Andreas Sellmer,  Andrea Brancale,  Ernest Hamel
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Ferrara, Italy. rmr@unife.it
PMID: 19663386 DOI: 10.1021/jm9001692
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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