Abstract
Derivatives of 2- and 3-benzo[b]furancarboxylic acids were prepared and evaluated for their cytotoxic potential in the National Cancer Institute, Bethesda, USA. Six compounds: 7-acetyl-6-hydroxy-3-methyl-2-benzofurancarboxylic acid ( 2), 6-hydroxy-7-( p-methoxycinnamoyl)-3-methyl-2-benzofurancarboxylic acid ( 4), 5-bromo-7-hydroxy-6-methoxy-2-benzofurancarboxylic acid methyl ester ( 6a), 6-acetyl-5-( O-ethyl-2′-diethylamino)-2-methyl-3-benzofurancarboxylic acid methyl ester ( 1f), 6-( O-ethyl-2′-diethylamino)-7- p-methoxycinnamoyl)-3-methyl-2-benzofurancarboxylic acid methyl ester hydrochloride ( 4b), 5-bromo-7-( O-ethyl-2′-diethylamino)-6-methoxy-2-benzofurancarboxylic acid methyl ester ( 6b) showed significant cytotoxic activities against human cancer cell lines. In addition the crystal structures of 7-methoxy-2-benzofurancarboxylic acid methyl ester ( 7a) has been solved by X-ray structure analysis of single crystals.
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