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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.

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.

SUBMITTER: Romagnoli R

PROVIDER: S-EPMC2762271 | biostudies-literature | 2009 Sep

REPOSITORIES: biostudies-literature

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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.

Romagnoli Romeo R Baraldi Pier Giovanni PG Carrion Maria Dora MD Cruz-Lopez Olga O Cara Carlota Lopez CL Basso Giuseppe G Viola Giampietro G Khedr Mohammed M Khedr Mohammed M Balzarini Jan J Mahboobi Siavosh S Sellmer Andreas A Brancale Andrea A Hamel Ernest E

Journal of medicinal chemistry 20090901 17

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 e ...[more]

PMID: 19663386

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