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KMID : 0043319970200020155
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Archives of Pharmacal Research
1997 Volume.20 No. 2 p.155 ~ p.157
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Anti-cell Adhesive Effect of Phenylacetylshikonin Analogues Related to their Cytotoxicity in A549 Cells
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Kim Seon-Hee
Song Gyu-Yong
Sok Dai-Eun
Ahn Byung-Zun
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Abstract
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An attempt to estabilish the relationship between anti-cell adhesive action of phenylacetylshikonin analogues and their cytotoxicity against A549 cells was done. In the one hour incubation with A549 cells,-methoxyphenylacetyl-(9), -acetoxyphenylacetyl-(13), 3,4-methylenedioxyphenylacetyl-(15) and 4-(N,N-dimethylamino)-phenylacetylshikonin (17) analogues showed a high anti-cell adhesive activity , while halophenylacetyl- and dimethoxy- or trimethoxyphenylacetyl analogues expressed no activity at , indicating that the presence of a bulky group at and a polar group at C-4 of phenylacetyl moiety may be important. A similar structure activity relationship exists for the 48 hr cytotoxocity of phenylacetylshikonin analogues in A 549 cells, but not in either K562 or L1210 cells. Furthermore, the difference between values for anti-cell adhesive activity and values for cytotoxicity of potent compound in A549 cells was not so great (1.5 to 3 times). Based on these observations, it is proposed that the anti-cell adhesive action of phenylacetylshikonins might be responsible for their cytotoxicity in A549 cells.
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KEYWORD
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Anti-cell adhesive effect, cytotoxicity, phenylacetylshikonin
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