1. Academic Validation
  2. Structure-cytotoxicity relationships of a series of natural and semi-synthetic simple coumarins as assessed in two human tumour cell lines

Structure-cytotoxicity relationships of a series of natural and semi-synthetic simple coumarins as assessed in two human tumour cell lines

  • Z Naturforsch C J Biosci. 1997 Mar-Apr;52(3-4):240-4. doi: 10.1515/znc-1997-3-416.
H Kolodziej 1 O Kayser H J Woerdenbag W van Uden N Pras
Affiliations

Affiliation

  • 1 Institut für Pharmazie II, Freie Universität Berlin, Germany.
Abstract

The cytotoxicity of 22 natural and semi-synthetic simple Coumarins was evaluated in GLC4, a human small cell lung carcinoma cell line, and in COLO 320, a human colorectal Cancer cell line, using the microculture tetrazolium (MTT) assay. With IC50 values > 100 microM, following a continuous (96 h) incubation, most Coumarins exhibited only low cytotoxicity. Several compounds, however, displayed significant potencies. As far as the structure--cytotoxicity relationship is concerned, it is conspicuous that all the potentially active natural compounds possess at least two phenolic groups in either the 6,7- or 6,8-positions. In addition, the 5-formyl-6-hydroxy substituted semi-synthetic analogue was found to be potent, reflecting the importance of at least two polar functions for high cytotoxicity.

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