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KMID : 0043319960190050416
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Archives of Pharmacal Research
1996 Volume.19 No. 5 p.416 ~ p.422
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Antitumor Activity of Arylacetylshikonin Analogues
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Kim Seon-Hee
Song Gyu-Yong
Jin Guang Zhu
Ahn Byung-Zun
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Abstract
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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.
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KEYWORD
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ARYLACETYLSHIKONIN, SYNTHESIS, CYTOTOXICITY, ANTITUMOR ACTIVITY
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