Archives of Pharmacal Research

, Volume 34, Issue 3, pp 357–367 | Cite as

Structural influence of indole C5-N-substitutents on the cytotoxicity of seco-duocarmycin analogs

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Abstract

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.

Key words

Achiral duocarmycin seco-Cyclopropylindoline Cytotoxicity DNA minor groove alkylation 
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Copyright information

© The Pharmaceutical Society of Korea and Springer Netherlands 2011

Authors and Affiliations

  1. 1.College of PharmacyCatholic University of DaeguHayangKorea

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