Synthesis of Analogues of Dicoumarol and Their Biological Evaluation

Julie Chineze Obi and Tagbo Emmanuel Ezenwa

International Journal of Chemistry, 2018, vol. 10, issue 3, 1-7

Abstract: Both symmetrical (1a-f) and asymmetrical (2a-f) analogues of dicoumarol were synthesized in 20 ¨C 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 ¡À 6 nM) towards NQO1 but also was toxic (IC50 = 9.2 ¡À 0.2 ¦ÌM) towards the A549 small lung cancer cell line.

Keywords: asymmetrical; cytotoxicity; inhibitor; NQO1; symmetrical; synthesis (search for similar items in EconPapers)
Date: 2018
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