{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,12,19]],"date-time":"2025-12-19T08:48:25Z","timestamp":1766134105500},"reference-count":0,"publisher":"OAE Publishing Inc.","issue":"1","content-domain":{"domain":["oaepublish.com"],"crossmark-restriction":false},"short-container-title":["Cancer Drug Resist"],"abstract":"<jats:p>Aim: Efficient and readily available anticancer drugs are sought as treatment options. For this reason, chromene derivatives were prepared using the one-pot reaction and tested for their anticancer and anti-angiogenic properties.  Methods: 2-Amino-3-cyano-4-(aryl)-7-methoxy-4H-chromene compounds (2A-R) were repurposed or newly synthesized via a three-component reaction of 3-methoxyphenol, various aryl aldehydes, and malononitrile. We performed assays to study the inhibition of tumor cell growth (MTT assay), effects on microtubules (immunofluorescence), cell cycle (flow-activated cell sorting analysis), angiogenesis (zebrafish model), and MYB activity (luciferase reporter assay). Fluorescence microscopy was applied for localization studies via copper-catalyzed azide-alkyne click reaction of an alkyne-tagged drug derivative.  Results: Compounds 2A-C and 2F exhibited robust antiproliferative activities against several human cancer cell lines (50% inhibitory concentrations in the low nanomolar range) and showed potent MYB inhibition. The alkyne derivative 3 was localized in the cytoplasm after only 10 min of incubation. Substantial microtubule disruption and G2\/M cell-cycle arrest were observed, where compound 2F stood out as a promising microtubule-disrupting agent. The study of anti-angiogenic properties showed that 2A was the only candidate with a high potential to inhibit blood vessel formation in vivo.  Conclusion: The close interplay of various mechanisms, including cell-cycle arrest, MYB inhibition, and anti-angiogenic activity, led to identifying promising multimodal anticancer drug candidates.<\/jats:p>","DOI":"10.20517\/cdr.2022.90","type":"journal-article","created":{"date-parts":[[2023,2,1]],"date-time":"2023-02-01T05:11:20Z","timestamp":1675228280000},"page":"59-78","update-policy":"http:\/\/dx.doi.org\/10.20517\/oae.crossmark.policy","source":"Crossref","is-referenced-by-count":4,"title":["Multimodal 4-arylchromene derivatives with microtubule-destabilizing, anti-angiogenic, and MYB-inhibitory activities"],"prefix":"10.20517","volume":"6","author":[{"given":"Leonhard H. F.","family":"K\u00f6hler","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sebastian","family":"Reich","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maria","family":"Yusenko","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Karl-Heinz","family":"Klempnauer","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Gerrit","family":"Begemann","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rainer","family":"Schobert","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Bernhard","family":"Biersack","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"8410","published-online":{"date-parts":[[2023]]},"container-title":["Cancer Drug Resistance"],"original-title":[],"deposited":{"date-parts":[[2024,1,18]],"date-time":"2024-01-18T08:46:25Z","timestamp":1705567585000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.oaepublish.com\/articles\/cdr.2022.90"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2023]]},"references-count":0,"journal-issue":{"issue":"1","published-online":{"date-parts":[[2023]]}},"URL":"https:\/\/doi.org\/10.20517\/cdr.2022.90","relation":{},"ISSN":["2578-532X"],"issn-type":[{"value":"2578-532X","type":"electronic"}],"subject":[],"published":{"date-parts":[[2023]]}}}