期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 47, 期 10, 页码 2635-2644出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm030473r
关键词
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资金
- NCI NIH HHS [R01CA 878746, T32 CA09657] Funding Source: Medline
Splitomicin (1) and 41 analogues were prepared and evaluated in cell-based Sir2 inhibition and toxicity assays and an in vitro Sir2 inhibition assay. Lactone ring or naphthalene (positions 7-9) substituents decrease activity, but other naphthalene substitutions (positions 5 and 6) are well-tolerated. The hydrolytically unstable aromatic lactone is important for activity. Lactone hydrolysis rates were used as a measure of reactivity; hydrolysis rates correlate with inhibitory activity. The most potent Sir2 inhibitors were structurally similar to and had hydrolysis rates similar to 1.
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