Paper
Toxicity and biotransformation of the anti‐cancer agent 7‐methoxy‐4‐bromomethylcoumarin
Published Sep 1, 1998 · J. Simpson, M. Coleman, D. Rathbone
Journal of Pharmacy and Pharmacology
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Abstract
4-Bromomethylcoumarins are known antiproliferative agents with high activity against leukaemia and melanoma cells in v i m . As part of a cancer screening programme 7-methoxy-4bromomethylcoumarin (MBMC) (1) was tested against two murine adenocarcinoma cell lines, MAC13 and MAC16, which are both generally refractive to standard cytotoxic agents. For both the MAC13 and the cachexia inducing MAC16 cell lines, MBMC had a profound anti-proliferative effect with ICso values of below 1.5pM for the two cell lines. The mode of action of MBMC has not been determined, however, the lack of any anti-tumour activity shown by the related compound 7-methoxy4-methylcoumarin (MMC) (2) indicates that its activity is likely to be due to the alkylating ability of the 4-bromomethyl group.
7-methoxy-4-bromomethylcoumarin shows profound anti-proliferative activity against murine adenocarcinoma cell lines, likely due to its alkylating ability.
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