Synthesis of Analogues of Dicoumarol and Their Biological Evaluation

Julie Chineze Obi, Tagbo Emmanuel Ezenwa


Both symmetrical (1a-f) and asymmetrical (2a-f) analogues of dicoumarol were synthesized in 20 – 86% yield by using microwave assisted one-pot protocol. Their ability to inhibit NAD (P)H:oxidorectase quinone 1 (NQO1) and cytotoxicity towards A549 small lung cancer cell line were evaluated. Interestingly, (E)-3-(2-hydroxynaphthalen-1-y)chroman-2,4-dione (2d) showed not only moderate inhibitory potency (IC50 = 20 ± 6 nM) towards NQO1 but also was toxic (IC50 = 9.2 ± 0.2 µM) towards the A549 small lung cancer cell line.

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International Journal of Chemistry   ISSN 1916-9698 (Print)   ISSN 1916-9701 (Online)

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