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

Zeitschrift Für Naturforschung. C, a Journal of Biosciences
H KolodziejN Pras

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.

Citations

Sep 14, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Krešimir BenciMladen Mintas
Jan 30, 2015·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Yang-Liu XiaLing Yang
May 15, 2007·Bioinorganic Chemistry and Applications·Irena KostovaMargarita Karaivanova
May 24, 2019·The Journal of Physical Chemistry. a·Zhivko VelkovAlia Tadjer

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