Structure -Cytotoxicity Relationships of a Series of Natural and Semi-Synthetic Simple Coumarins as Assessed in Two Human Tumour Cell Lines

Autor: Kolodziej, Herbert, Kayser, Oliver, Woerdenbag, Herman J., Uden, Wim van, Pras, Niesko
Zdroj: Zeitschrift für Naturforschung C; April 1997, Vol. 52 Issue: 3-4 p240-244, 5p
Abstrakt: 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 IC50values > 100 µ? , following a continuous (96h) 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.
Databáze: Supplemental Index