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

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• 作者：Romeo Romagnoli ; Pier Giovanni Baraldi ; Maria Dora Carrion ; Olga Cruz-Lopez ; Carlota Lopez Cara ; Giuseppe Basso ; Giampietro Viola ; Mohammed Khedr ; Jan Balzarini ; Siavosh Mahboobi ; Andreas Sellmer ; And
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：September 10, 2009
• 年：2009
• 卷：52
• 期：17
• 页码：5551-5555
• 全文大小：810K
• 年卷期：v.52,no.17(September 10, 2009)
• ISSN：1520-4804

文摘

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.