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Here we present the synthesis and antiproliferative activity of a series of diversely substituted 12 synthesized 4-oxycoumarin derivatives. Among all compounds the 4-hydroxy-5,7-dimethoxycoumarin showed the most potent antiproliferative effect against several human (MCF-7, U937 and HL-60) and mouse (Neuro2a) cancer cell lines with IC50 values in the range of 0.2–2 μM. Intriguingly its structural isomer where only methoxy group is changed from 5 to 8 position was inactive in MCF-7 cells, and only weakly active in HL-60, U937 and Neuro2a cells.
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