{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,2]],"date-time":"2026-10-02T12:59:02Z","timestamp":1790945942220,"version":"4.1.0"},"reference-count":38,"publisher":"MDPI AG","issue":"21","license":[{"start":{"date-parts":[[2023,10,25]],"date-time":"2023-10-25T00:00:00Z","timestamp":1698192000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Guangdong Pharmaceutical University-Special Projects in Key Fields of General Colleges and Universities in Guangdong Province","award":["2022ZDZX2030"],"award-info":[{"award-number":["2022ZDZX2030"]}]},{"name":"Guangdong Pharmaceutical University-Special Projects in Key Fields of General Colleges and Universities in Guangdong Province","award":["2021JGXM071"],"award-info":[{"award-number":["2021JGXM071"]}]},{"name":"Guangdong Pharmaceutical University-Special Projects in Key Fields of General Colleges and Universities in Guangdong Province","award":["B20234214"],"award-info":[{"award-number":["B20234214"]}]},{"name":"Guangdong Pharmaceutical University-Special Projects in Key Fields of General Colleges and Universities in Guangdong Province","award":["20231205"],"award-info":[{"award-number":["20231205"]}]},{"name":"Guangdong Province Graduate Education Innovation Program in 2021","award":["2022ZDZX2030"],"award-info":[{"award-number":["2022ZDZX2030"]}]},{"name":"Guangdong Province Graduate Education Innovation Program in 2021","award":["2021JGXM071"],"award-info":[{"award-number":["2021JGXM071"]}]},{"name":"Guangdong Province Graduate Education Innovation Program in 2021","award":["B20234214"],"award-info":[{"award-number":["B20234214"]}]},{"name":"Guangdong Province Graduate Education Innovation Program in 2021","award":["20231205"],"award-info":[{"award-number":["20231205"]}]},{"name":"Medical Scientific Research Foundation of Guangdong Province","award":["2022ZDZX2030"],"award-info":[{"award-number":["2022ZDZX2030"]}]},{"name":"Medical Scientific Research Foundation of Guangdong Province","award":["2021JGXM071"],"award-info":[{"award-number":["2021JGXM071"]}]},{"name":"Medical Scientific Research Foundation of Guangdong Province","award":["B20234214"],"award-info":[{"award-number":["B20234214"]}]},{"name":"Medical Scientific Research Foundation of Guangdong Province","award":["20231205"],"award-info":[{"award-number":["20231205"]}]},{"name":"Guangdong Provincial Bureau of Traditional Chinese Medicine","award":["2022ZDZX2030"],"award-info":[{"award-number":["2022ZDZX2030"]}]},{"name":"Guangdong Provincial Bureau of Traditional Chinese Medicine","award":["2021JGXM071"],"award-info":[{"award-number":["2021JGXM071"]}]},{"name":"Guangdong Provincial Bureau of Traditional Chinese Medicine","award":["B20234214"],"award-info":[{"award-number":["B20234214"]}]},{"name":"Guangdong Provincial Bureau of Traditional Chinese Medicine","award":["20231205"],"award-info":[{"award-number":["20231205"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>Chalcone is a common simple fragment of natural products with anticancer activity. In a previous study, the research group discovered a series of chalcone derivatives with stronger anticancer activities. To find better anticancer drugs, novel chalcone derivatives A1\u2013A14, B1\u2013B14 have continuously been designed and synthesized. The antiproliferative activity of these compounds against breast cancer cells (MCF-7) was investigated by the Cell Counting Kit-8 (CCK-8) method with 5-fluorouracil (5-Fu) as the control drug. The results showed that compound A14 exhibited excellent antiproliferative ability compared to the control drug 5-Fu. Scratch experiments and cloning experiments further confirmed that compound A14 could inhibit the proliferation and colony formation activity of MCF-7 cells. In addition, molecular docking primarily explains the interaction between compound and protein. These results suggested that compound A14 could be a promising chalcone derivative for further anti-breast cancer research.<\/jats:p>","DOI":"10.3390\/ijms242115549","type":"journal-article","created":{"date-parts":[[2023,10,25]],"date-time":"2023-10-25T04:14:47Z","timestamp":1698207287000},"page":"15549","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":9,"title":["Design and Synthesis of Novel Chalcone Derivatives: Anti-Breast Cancer Activity Evaluation and Docking Study"],"prefix":"10.3390","volume":"24","author":[{"given":"Weihong","family":"Lai","sequence":"first","affiliation":[{"name":"School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jiaxin","family":"Chen","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xinjiao","family":"Gao","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaobao","family":"Jin","sequence":"additional","affiliation":[{"name":"Guangdong Key Laboratory of Pharmaceutical Bioactive Substances, Guangdong Pharmaceutical University, Guangzhou 510006, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gong","family":"Chen","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lianbao","family":"Ye","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2023,10,25]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","unstructured":"Akram, M., Iqbal, M., Daniyal, M., and Khan, A.U. (2017). Awareness and current knowledge of breast cancer. Biol. Res., 50.","DOI":"10.1186\/s40659-017-0140-9"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"333","DOI":"10.1007\/s12013-014-0459-6","article-title":"Breast Cancer: Epidemiology and Etiology","volume":"72","author":"Tao","year":"2015","journal-title":"Cell Biochem. Biophys."},{"key":"ref_3","doi-asserted-by":"crossref","first-page":"9S","DOI":"10.2967\/jnumed.115.157834","article-title":"Clinical Diagnosis and Management of Breast Cancer","volume":"57","author":"McDonald","year":"2016","journal-title":"J. Nucl. Med."},{"key":"ref_4","doi-asserted-by":"crossref","first-page":"102339","DOI":"10.1016\/j.ctrv.2022.102339","article-title":"Global challenges and policy solutions in breast cancer control","volume":"104","author":"Trapani","year":"2022","journal-title":"Cancer Treat. Rev."},{"key":"ref_5","first-page":"Cd011276","article-title":"Breast surgery for metastatic breast cancer","volume":"3","author":"Tosello","year":"2018","journal-title":"Cochrane Database Syst. Rev."},{"key":"ref_6","doi-asserted-by":"crossref","first-page":"100","DOI":"10.1016\/j.canlet.2020.10.016","article-title":"Triple-negative breast cancer therapeutic resistance: Where is the Achilles\u2019 heel?","volume":"497","author":"Bai","year":"2021","journal-title":"Cancer Lett."},{"key":"ref_7","doi-asserted-by":"crossref","first-page":"102375","DOI":"10.1016\/j.ctrv.2022.102375","article-title":"Adjuvant and neoadjuvant breast cancer treatments: A systematic review of their effects on mortality","volume":"105","author":"Kerr","year":"2022","journal-title":"Cancer Treat. Rev."},{"key":"ref_8","doi-asserted-by":"crossref","first-page":"2423","DOI":"10.2147\/DDDT.S253961","article-title":"Evaluation of the Efficacy of Neoadjuvant Chemotherapy for Breast Cancer","volume":"14","author":"Wang","year":"2020","journal-title":"Drug Des. Dev. Ther."},{"key":"ref_9","doi-asserted-by":"crossref","first-page":"2103","DOI":"10.2174\/1389557521666210126125200","article-title":"A Critical Review on Recent Development of Techniques and Drug Targets in the Management of Breast Cancer","volume":"21","author":"Buumba","year":"2021","journal-title":"Mini Rev. Med. Chem."},{"key":"ref_10","doi-asserted-by":"crossref","first-page":"531","DOI":"10.1038\/nchem.2479","article-title":"Counting on natural products for drug design","volume":"8","author":"Rodrigues","year":"2016","journal-title":"Nat. Chem."},{"key":"ref_11","doi-asserted-by":"crossref","first-page":"770","DOI":"10.1021\/acs.jnatprod.9b01285","article-title":"Natural Products as Sources of New Drugs over the Nearly Four Decades from 01\/1981 to 09\/2019","volume":"83","author":"Newman","year":"2020","journal-title":"J. Nat. Prod."},{"key":"ref_12","doi-asserted-by":"crossref","first-page":"65","DOI":"10.1016\/j.jsps.2022.11.006","article-title":"Design, Synthesis, anticancer evaluation and in silico studies of 2,4,6-trimethoxychalcone derivatives","volume":"31","author":"Li","year":"2023","journal-title":"Saudi Pharm. J."},{"key":"ref_13","doi-asserted-by":"crossref","first-page":"7762","DOI":"10.1021\/acs.chemrev.7b00020","article-title":"Chalcone: A Privileged Structure in Medicinal Chemistry","volume":"117","author":"Zhuang","year":"2017","journal-title":"Chem. Rev."},{"key":"ref_14","doi-asserted-by":"crossref","first-page":"348","DOI":"10.2174\/1568026620666201022143236","article-title":"Chalcone Derivatives and their Activities against Drug-resistant Cancers: An Overview","volume":"21","author":"Xiao","year":"2021","journal-title":"Curr. Top. Med. Chem."},{"key":"ref_15","doi-asserted-by":"crossref","first-page":"1265","DOI":"10.2174\/1871520623666230223112530","article-title":"Recent Progresses in Chalcone Derivatives as Potential Anticancer Agents","volume":"23","author":"Yang","year":"2023","journal-title":"Anti-Cancer Agents Med. Chem."},{"key":"ref_16","doi-asserted-by":"crossref","unstructured":"Dhaliwal, J.S., Moshawih, S., Goh, K.W., Loy, M.J., Hossain, M.S., Hermansyah, A., Kotra, V., Kifli, N., Goh, H.P., and Dhaliwal, S.K.S. (2022). Pharmacotherapeutics Applications and Chemistry of Chalcone Derivatives. Molecules, 27.","DOI":"10.3390\/molecules27207062"},{"key":"ref_17","doi-asserted-by":"crossref","unstructured":"Constantinescu, T., and Lungu, C.N. (2021). Anticancer Activity of Natural and Synthetic Chalcones. Int. J. Mol. Sci., 22.","DOI":"10.3390\/ijms222111306"},{"key":"ref_18","doi-asserted-by":"crossref","first-page":"592654","DOI":"10.3389\/fphar.2020.592654","article-title":"Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence","volume":"11","author":"Salehi","year":"2020","journal-title":"Front. Pharmacol."},{"key":"ref_19","first-page":"755","article-title":"Personal experience in the pre- and postoperative periods of biliary surgery with the preparation 1314 CB (trimethoxy-chalcone) combined with Oddi\u2019s sphincter spasmolytics","volume":"38","year":"1972","journal-title":"Rev. Esp. Enferm. Apar. Dig."},{"key":"ref_20","doi-asserted-by":"crossref","first-page":"855","DOI":"10.1161\/HYPERTENSIONAHA.114.04781","article-title":"Sofalcone upregulates the nuclear factor (erythroid-derived 2)-like 2\/heme oxygenase-1 pathway, reduces soluble fms-like tyrosine kinase-1, and quenches endothelial dysfunction: Potential therapeutic for preeclampsia","volume":"65","author":"Onda","year":"2015","journal-title":"Hypertension"},{"key":"ref_21","doi-asserted-by":"crossref","first-page":"566","DOI":"10.1016\/j.bbrc.2009.02.086","article-title":"Sofalcone, an anti-ulcer chalcone derivative, suppresses inflammatory crosstalk between macrophages and adipocytes and adipocyte differentiation: Implication of heme-oxygenase-1 induction","volume":"381","author":"Tanaka","year":"2009","journal-title":"Biochem. Biophys. Res. Commun."},{"key":"ref_22","doi-asserted-by":"crossref","unstructured":"Goodson, H.V., and Jonasson, E.M. (2018). Microtubules and Microtubule-Associated Proteins. Cold Spring Harb. Perspect. Biol., 10.","DOI":"10.1101\/cshperspect.a022608"},{"key":"ref_23","doi-asserted-by":"crossref","first-page":"1240","DOI":"10.1177\/1535370219867296","article-title":"Microtubules: Evolving roles and critical cellular interactions","volume":"244","author":"Logan","year":"2019","journal-title":"Exp. Biol. Med."},{"key":"ref_24","first-page":"147","article-title":"Microtubule involvement in regulating cell contractility and adhesion-dependent signalling: A possible mechanism for polarization of cell motility","volume":"65","author":"Elbaum","year":"1999","journal-title":"Biochem. Soc. Symp."},{"key":"ref_25","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1146\/annurev-cellbio-120420-114559","article-title":"How Microtubules Build the Spindle Branch by Branch","volume":"38","author":"Travis","year":"2022","journal-title":"Annu. Rev. Cell Dev. Biol."},{"key":"ref_26","doi-asserted-by":"crossref","first-page":"509","DOI":"10.1042\/EBC20190016","article-title":"Microtubules in cell migration","volume":"63","author":"Garcin","year":"2019","journal-title":"Essays Biochem."},{"key":"ref_27","doi-asserted-by":"crossref","first-page":"257","DOI":"10.1146\/annurev-physiol-062421-040656","article-title":"Cardiomyocyte Microtubules: Control of Mechanics, Transport, and Remodeling","volume":"84","author":"Uchida","year":"2022","journal-title":"Annu. Rev. Physiol."},{"key":"ref_28","doi-asserted-by":"crossref","first-page":"889","DOI":"10.2174\/1389450124666230731094837","article-title":"Microtubules and Cell Division: Potential Pharmacological Targets in Cancer Therapy","volume":"24","author":"Sebastian","year":"2023","journal-title":"Curr. Drug Targets"},{"key":"ref_29","doi-asserted-by":"crossref","first-page":"777","DOI":"10.1038\/s41580-021-00399-x","article-title":"Regulation of microtubule dynamics, mechanics and function through the growing tip","volume":"22","author":"Gudimchuk","year":"2021","journal-title":"Nat. Rev. Mol. Cell Biol."},{"key":"ref_30","doi-asserted-by":"crossref","first-page":"235","DOI":"10.1111\/jnc.12621","article-title":"Microtubules in neurons as information carriers","volume":"129","author":"Dent","year":"2014","journal-title":"J. Neurochem."},{"key":"ref_31","first-page":"571","article-title":"Inhibitors of microtubule polymerization- new natural compounds as potential anti-cancer drugs","volume":"69","author":"Rogalska","year":"2015","journal-title":"Postep. Hig. Med. Dosw."},{"key":"ref_32","first-page":"61","article-title":"Colchicine in Cardiovascular Disease: In-Depth Review","volume":"145","author":"Deftereos","year":"2022","journal-title":"Circulation"},{"key":"ref_33","doi-asserted-by":"crossref","first-page":"659","DOI":"10.2174\/1381612824666180123110042","article-title":"Colchicine Pharmacokinetics and Mechanism of Action","volume":"24","author":"Angelidis","year":"2018","journal-title":"Curr. Pharm. Des."},{"key":"ref_34","doi-asserted-by":"crossref","first-page":"3748","DOI":"10.2174\/0929867328666211202101641","article-title":"Recent Trends in Tubulin-Binding Combretastatin A-4 Analogs for Anticancer Drug Development","volume":"29","author":"Paidakula","year":"2022","journal-title":"Curr. Med. Chem."},{"key":"ref_35","doi-asserted-by":"crossref","first-page":"6787","DOI":"10.2174\/0929867326666191003154051","article-title":"Tubulin Inhibitors Binding to Colchicine-Site: A Review from 2015 to 2019","volume":"27","author":"Xia","year":"2020","journal-title":"Curr. Med. Chem."},{"key":"ref_36","doi-asserted-by":"crossref","first-page":"955","DOI":"10.2174\/1871520615666150526141259","article-title":"Recent advancement in discovery and development of natural product combretastatin-inspired anticancer agents","volume":"15","author":"Patil","year":"2015","journal-title":"Anticancer Agents Med. Chem."},{"key":"ref_37","doi-asserted-by":"crossref","first-page":"482","DOI":"10.1016\/j.ejmech.2018.04.011","article-title":"Recent advances in trimethoxyphenyl (TMP) based tubulin inhibitors targeting the colchicine binding site","volume":"151","author":"Li","year":"2018","journal-title":"Eur. J. Med. Chem."},{"key":"ref_38","doi-asserted-by":"crossref","first-page":"373","DOI":"10.1016\/j.bmc.2014.12.027","article-title":"Natural antitubulin agents: Importance of 3,4,5-trimethoxyphenyl fragment","volume":"23","author":"Negi","year":"2015","journal-title":"Bioorg. Med. Chem."}],"container-title":["International Journal of Molecular Sciences"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/1422-0067\/24\/21\/15549\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,10]],"date-time":"2025-10-10T21:11:14Z","timestamp":1760130674000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/1422-0067\/24\/21\/15549"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2023,10,25]]},"references-count":38,"journal-issue":{"issue":"21","published-online":{"date-parts":[[2023,11]]}},"alternative-id":["ijms242115549"],"URL":"https:\/\/doi.org\/10.3390\/ijms242115549","relation":{},"ISSN":["1422-0067"],"issn-type":[{"value":"1422-0067","type":"electronic"}],"subject":[],"published":{"date-parts":[[2023,10,25]]}}}