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KMID : 0043320110340030357
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Archives of Pharmacal Research
2011 Volume.34 No. 3 p.357 ~ p.367
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Structural influence of indole C5-N-substitutents on the cytotoxicity of seco-duocarmycin analogs
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Choi Tae-Young
Ma Eun-Sook
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Abstract
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A series of racemic indole C5-substituted seco-cyclopropylindoline compounds (2,3 and 5?7) were prepared by coupling 1-(tert-butyloxycarbonyl)-3-(chlorocarbonyl)indoline (seg-A) with 5,6,7-trimethoxy-, 5,6-dimethoxy-, 5-amino-, 5-methylsulfonylamino- and 5-(N,N-dimethylaminosulfonylamino) indole-2-carboxylic acid as seg-B in the presence of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide. The synthetic compounds (2,3 and 5?7) were tested for cytotoxic activity against human cancer cell lines (COLO 205, SK-MEL-2, A549, and JEG-3) using the MTT assay.
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KEYWORD
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Achiral duocarmycin, seco-Cyclopropylindoline, Cytotoxicity, DNA minor groove alkylation
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