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KMID : 0370220050490010068
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Yakhak Hoeji
2005 Volume.49 No. 1 p.68 ~ p.73
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Synthesis of New Semisynthetic Analogs of Epi-xanthatin by Modification of the Side Chain and Their Cytotoxic Activity
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백두종/Baek DJ
안종웅/이정옥/Ahn JW/Lee CO
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Abstract
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Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vitro antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with ED so values of 0.1-30㎍/ml, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity, weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.
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