Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 17, Pages 5551-5555Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm9001692
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- Intramural NIH HHS [Z99 CA999999] Funding Source: Medline
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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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