期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 9, 页码 2679-2682出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.02.089
关键词
(+)-Lycoricidine; Heat-stress cognate 70 (Hsc70); Down-regulators; Structure-activity relationship (SAR); Anti-HCV activity
资金
- National Natural Science Foundation of China [30830114, 31270404]
- Ministry of Science and Technology [2009CB522300]
The anti hepatitis C virus (HCV) activity of (+)-lycoricidine (1) was evaluated for the first time in this letter, yielding an EC50 value of 0.55 nmol/mL and an selection index (SI) value of 12.72. Further studies indicated that 1 induced this effect by down-regulating host heat-stress cognate 70 (Hsc70) expression. In addition, 20 derivatives were designed and synthesised to investigate the basic structure-activity relationship (SAR) of the title compound. Several of these derivatives exhibit a good inhibition of HCV, such as compound 3 (EC50 = 0.68 nmol/mL, SI = 33.86), compound 2d (EC50 = 15 nmol/mL, SI = 12) and compound 5 (EC50 = 33 nmol/mL, SI > 10.91). Meanwhile, the experimental data suggest that the modification of certain groups of (+)-lycoricidine can reduce the cytotoxicity of the compounds. (C) 2013 Elsevier Ltd. All rights reserved.
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