• Archives of Pharmacal Research
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• v.26 no.5
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• pp.345-350
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• 2003

5,7-Dihydroxyflavones and their Ο-methylated flavone analogs were prepared and evaluated their anti-inflammatory activity to decipher the structure-activity relationships. Most of the analogs were achieved from 2,4,6-trihydroxyacetophenone in 4 steps. 5,7-Dihydroxy-4 -methoxyflavone (4c) and 7-hydroxy-4 ,5-dimethoxyflavone(6c) were prepared following a different synthetic pathway. Among the synthetic flavones tested, 5-hydroxy-7-methoxyflavone analogs (3a-3e) showed moderate inhibitory activities of $PGE_2$ production from LPS-induced RAW 264.7 cells.

• YAKHAK HOEJI
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• v.43 no.5
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• pp.559-565
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• 1999

The two gericudranin E derivatives, GER-I & II, were synthesized and evaluated their antitumour activities for the elucidation of structure-activity relationship. 2,4,6-Trihydroxyacetophenone was converted to target molecules GER-I and GER-B in 5 steps via sequential protection, aldol condensation, Michael type-cyclization, regioselective C-benzylation. The cellular growth inhibition of compounds GER-I and GER-II were investigated against P388, L1210, K562, HCT-15, SK-HepG-1, MCF-7 as cancer cell lines and mouse splenocytes as a normal cell by MTT assay.

• YAKHAK HOEJI
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• v.41 no.1
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• pp.14-17
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• 1997

(${\pm}$)-3-Deoxygericudranin A was designed and synthesized for the development of novel antitumour agent and for the elucidation of the effect of 3-hydroxyl group in gericudranin A on antitumour activity. 2,4.6-Trihydroxyacetophenone was converted to 3-deoxygericudranin A in 5 steps via sequential protection, aldol condensation, Michael tvpe-cyclization, regioselective, C-benzylation and deprotection.