• Bulletin of the Korean Chemical Society
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• v.32 no.4
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• pp.1293-1297
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• 2011

To improve the biological activities of rupestonic acid, 21 new rupestonic acid fatty ester derivatives (2a-2h) and aromatic ester derivatives (2i-2u) were synthesized and preliminarily evaluated for their anti-influenza activity in vitro by the national center for drug screening of China, using the Oseltamivir and Ribavirin as reference drugs. The results showed that 2l ($IC_{50}=0.5{\mu}mol/L$) exhibited potent anti-influenza $A_3$ viral activity among the synthesized compounds and was 10-fold more potent than that of the reference drug Oseltamivir ($IC_{50}=5.1{\mu}mol/L$).

• Bulletin of the Korean Chemical Society
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• v.30 no.2
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• pp.435-440
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• 2009

19 Aromatic ring and L-amino acid ester contained rupestonic acid amide derivatives 2a~2l, 3a~3g were synthesized and preliminarily evaluated in vitro against influenza virus $A_3$,B and herpes simplex virus type 1 (HSV-1), 2(HSV-2) by the national center for drug screening of China. The rusults showed that 2i possessed the highest inhibition against both influenza virus $A_3\;(TC_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;19.2\;{\mu}$mol/L, SI = 6.3) and B (T$C_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;29.9\;{\mu}$mol/L, SI = 4.0); 2g was more active against influenza $A_3$ virus at very low cytotoxicity ($TC_{50}\;>\;2092.1\;{\mu}mol/L,\;IC_{50}=\;143.7\;{\mu}mol/L,$ SI > 14.6) than the parent compound; Compounds 2b, 2c, 2f showed higher activities both against HSV-1 and HSV-2 than that of the parent compound, and 2f was the most potent inhibitor of HSV-1 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;11.3\;{\mu}mol$/L, SI = 17.7 ) and HSV-2 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;20.7\;{\mu}mol$/L , SI = 9.7).