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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, R., Baraldi, P. G., Carrion, M. D., Cruz-Lopez, O., Cara, C. L., Basso, G., Viola, G., Khedr, Mohammed Abdou, Balzarini, J., Mahboobi, S., Sellmer, A., Brancale, Andrea and Hamel, E. 2009. 2-Arylamino-4-Amino-5-Aroylthiazoles. "One-Pot" Synthesis and Biological Evaluation of a New Class of Inhibitors of Tubulin Polymerization. Journal of Medicinal Chemistry 52 (17) , pp. 5551-5555. 10.1021/jm9001692

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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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
Publisher: American Chemical Society
ISSN: 0022-2623
Last Modified: 04 Jun 2017 01:58
URI: http://orca.cf.ac.uk/id/eprint/6697

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