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Molecules 2018, 23(9), 2281;

Design, Synthesis and Biological Evaluation of Novel 4-Substituted Coumarin Derivatives as Antitumor Agents

2,* and 1,*
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 17 August 2018 / Revised: 1 September 2018 / Accepted: 4 September 2018 / Published: 6 September 2018
(This article belongs to the Special Issue Design and Synthesis of Organic Molecules as Antineoplastic Agents)
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Herein, fifteen new compounds containing coumarin, 1,2,3-triazole and benzoyl- substituted arylamine moieties were designed, synthesized and tested in vitro for their anticancer activity. The results showed that all tested compounds had moderate antiproliferative activity against MDA-MB-231, a human breast cancer cell line, under both normoxic and hypoxic conditions. Furthermore, the 4-substituted coumarin linked with benzoyl 3,4-dimethoxyaniline through 1,2,3-triazole (compound 5e) displayed the most prominent antiproliferative activities with an IC50 value of 0.03 μM, about 5000 times stronger than 4-hydroxycoumarin (IC50 > 100 μM) and 20 times stronger than doxorubicin (IC50 = 0.60 μM). Meanwhile, almost all compounds revealed general enhancement of proliferation-inhibiting activity under hypoxia, contrasted with normoxia. A docking analysis showed that compound 5e had potential to inhibit carbonic anhydrase IX (CA IX). View Full-Text
Keywords: anticancer; coumarin; hypoxia; 1,2,3-triazole anticancer; coumarin; hypoxia; 1,2,3-triazole

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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An, R.; Hou, Z.; Li, J.-T.; Yu, H.-N.; Mou, Y.-H.; Guo, C. Design, Synthesis and Biological Evaluation of Novel 4-Substituted Coumarin Derivatives as Antitumor Agents. Molecules 2018, 23, 2281.

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