{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,2]],"date-time":"2026-07-02T23:08:57Z","timestamp":1783033737703,"version":"3.54.6"},"reference-count":23,"publisher":"MDPI AG","issue":"9","license":[{"start":{"date-parts":[[2018,9,6]],"date-time":"2018-09-06T00:00:00Z","timestamp":1536192000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>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 \u03bcM, about 5000 times stronger than 4-hydroxycoumarin (IC50 &gt; 100 \u03bcM) and 20 times stronger than doxorubicin (IC50 = 0.60 \u03bcM). 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).<\/jats:p>","DOI":"10.3390\/molecules23092281","type":"journal-article","created":{"date-parts":[[2018,9,6]],"date-time":"2018-09-06T10:38:38Z","timestamp":1536230318000},"page":"2281","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":57,"title":["Design, Synthesis and Biological Evaluation of Novel 4-Substituted Coumarin Derivatives as Antitumor Agents"],"prefix":"10.3390","volume":"23","author":[{"given":"Ran","family":"An","sequence":"first","affiliation":[{"name":"School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhuang","family":"Hou","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jian-Teng","family":"Li","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hao-Nan","family":"Yu","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yan-Hua","family":"Mou","sequence":"additional","affiliation":[{"name":"Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chun","family":"Guo","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2018,9,6]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"956","DOI":"10.1016\/j.bmcl.2010.12.059","article-title":"Synthesis and evaluation of a class of new coumarin triazole derivatives as potential antimicrobial agents","volume":"21","author":"Shi","year":"2011","journal-title":"Bioorg. 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