期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 2, 页码 179-182出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm701228e
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资金
- NCI NIH HHS [P50 CA102701] Funding Source: Medline
A series of substituted 9-aminoacridines is evaluated for antiproliferative activity toward pancreatic cancer cells. The results indicate that the compounds inhibit cell proliferation by inducing a G1-S phase arrest. A model is also developed that explains the molecular basis to inhibition through a DNA threading mechanism. We conclude that the drug-DNA complex formed blocks topoisomerase II binding and activity leading to catalytic inhibition of the enzyme and the induction of apoptosis and programmed cell death.
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