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KMID : 0043319960190050416
Archives of Pharmacal Research
1996 Volume.19 No. 5 p.416 ~ p.422
Antitumor Activity of Arylacetylshikonin Analogues
Kim Seon-Hee

Song Gyu-Yong
Jin Guang Zhu
Ahn Byung-Zun
Abstract
Twenty one phenylacetylshikonin analogues were synthesized from various subsitituted phenyl acetic acids and their cytotoxicity values against A549, K562 and L1210 cell lines and antitumor action in mice bearing S-180 cells were measured. All of phenylacetylshikonin analogues expressed a potent cytotoxicity against L1210 and K562 cells. L1210 cells were the most sensitive to shikonin analogues among these cells. Except 4-methosyphenylacetylshikonin , and a-acetoxyphenylacetylshikonin , all other shikonin derivatives sshowed higher values than phenylacetylshikonin , in L1210. In K562 cell, a-substitution of phenylacetylshikonin , while other subsitutions increased it slightly; 4-methoxyphenylacetylshikonin showed a exceptionally good cytotoxicity against K562 cell. 4-Halogenation tended to decrease the cytotoxic effect on L1210 cells, while it enhanced the effect on K562; 4-bromophenylacetyl and 4-chlorophenylacetyl shikonin . In contrast, A549 cells were much less sensitive to these shikonin analogues which showed values of.Most of phenylacetylshikonin derivatives showed good antitumor activity in mice bearing S-180 cells. a-A-cetoxyphenylacetylshikonin and 4-dimethylaminophenylacetylshikonin showed highest T/C value (192-195%), implying that introduction of a-acetyl or of 4-dimethylamino group enhanced the antitumor activity as shown for 4-dimethylaminophenylacetylshikonin (T/C, 192%). It might be due to improvement of water solubility by dimethylamino group in the molecule.
KEYWORD
ARYLACETYLSHIKONIN, SYNTHESIS, CYTOTOXICITY, ANTITUMOR ACTIVITY
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