期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 17, 页码 5551-5555出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm9001692
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资金
- Intramural NIH HHS [Z99 CA999999] Funding Source: Medline
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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