The essential role of microtubules in mitosis makes them a major target of compds. 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 polymn., and cell cycle effects. SAR was elucidated with various substitutions on the phenylamino and aroyl moiety at the 2- and 5-positions, resp., of the 4-aminothiazole skeleton. Tumor cell exposure to several of these compds. led to the arrest of HeLa cells in the G2/M phase of the cell cycle and induction of apoptosis.
2-Arylamino-4-Amino-5-Aroylthiazoles. "One-Pot" Synthesis and Biological Evaluation of a New Class of Inhibitors of Tubulin Polymerization.
ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;
2009
Abstract
The essential role of microtubules in mitosis makes them a major target of compds. 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 polymn., and cell cycle effects. SAR was elucidated with various substitutions on the phenylamino and aroyl moiety at the 2- and 5-positions, resp., of the 4-aminothiazole skeleton. Tumor cell exposure to several of these compds. led to the arrest of HeLa cells in the G2/M phase of the cell cycle and induction of apoptosis.File in questo prodotto:
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