{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,1,28]],"date-time":"2026-01-28T11:05:10Z","timestamp":1769598310573,"version":"3.49.0"},"reference-count":29,"publisher":"Wiley","issue":"3","license":[{"start":{"date-parts":[[2019,6,19]],"date-time":"2019-06-19T00:00:00Z","timestamp":1560902400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81603152"],"award-info":[{"award-number":["81603152"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Chem Biol Drug Des"],"published-print":{"date-parts":[[2019,9]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>Prostate cancer is the second leading cause of death in USA and has developed serious resistance to current drugs. Thus, development of new drugs for the treatment of castration\u2010resistant prostate cancer (CRPC) is urgently needed. In this study, 25 novel derivatives of tanshinone IIA as potential androgen receptor (AR) suppression reagents for the treatment of CRPC have been synthesized. The inhibition on DHT\u2010mediated AR transactivation and cell viability assay were performed to test the synthesized compounds. The results showed that among 25 new compounds, seven methoxy\u2010substituted tanshinone IIA derivatives showed significant inhibition effect on DHT\u2010mediated AR transactivation. In particular, TAN\u201024 that contains three methoxy groups showed the strongest inhibition effect on DHT\u2010mediated AR transactivation. In addition, TAN\u201024 also suppressed DHT\u2010AR transactivation more effectively than those of tanshinoneIIA and enzalutamide. In cytotoxicity against human prostate cancer cell lines assay, TAN\u201024 exhibited the most potent in vitro cytotoxicity against LNCaP and CWR22Rv1 cells, with IC<jats:sub>50<\/jats:sub> values 20\u2010 and 19\u2010times lower than those of tanshinone IIA and comparable to enzalutamide. TAN\u201024 reported in the present work represents a novel and effective AR suppression drug, showing great potential for the treatment of CRPC.<\/jats:p>","DOI":"10.1111\/cbdd.13567","type":"journal-article","created":{"date-parts":[[2019,5,20]],"date-time":"2019-05-20T17:34:22Z","timestamp":1558373662000},"page":"1656-1663","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":12,"title":["Synthesis of novel tanshinone derivatives for treatment of castration\u2010resistant prostate cancer"],"prefix":"10.1111","volume":"94","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-0506-1876","authenticated-orcid":false,"given":"Defeng","family":"Xu","sequence":"first","affiliation":[{"name":"School of Pharmaceutical Engineering and Life Science Changzhou University Changzhou Jiangsu China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hang","family":"Hu","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering and Life Science Changzhou University Changzhou Jiangsu China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jing","family":"Guan","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering and Life Science Changzhou University Changzhou Jiangsu China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jun","family":"Da","sequence":"additional","affiliation":[{"name":"Department of Urology and Andrology Shanghai Ninth People's Hospital School of Medicine Shanghai Jiao Tong University Shanghai China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yipeng","family":"Xie","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering and Life Science Changzhou University Changzhou Jiangsu China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yalin","family":"Liu","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering and Life Science Changzhou University Changzhou Jiangsu China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9010-1750","authenticated-orcid":false,"given":"Ren","family":"Kong","sequence":"additional","affiliation":[{"name":"School of Mechanical Engineering Jiangsu University of Technology Changzhou Jiangsu China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Guoqiang","family":"Song","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Engineering and Life Science Changzhou University Changzhou Jiangsu China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Huan","family":"Zhou","sequence":"additional","affiliation":[{"name":"School of Mechanical Engineering Jiangsu University of Technology Changzhou Jiangsu China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2019,6,19]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.1155\/2016\/4797102"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1002\/med.21304"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1002\/jcp.25099"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1039\/c0np00035c"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.2174\/1389450111314040004"},{"key":"e_1_2_8_7_1","doi-asserted-by":"publisher","DOI":"10.1158\/1940-6207.CAPR-13-0408"},{"key":"e_1_2_8_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.jep.2014.07.058"},{"key":"e_1_2_8_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.pharmthera.2007.09.008"},{"key":"e_1_2_8_10_1","first-page":"1","article-title":"Anticancer drug targets of Salvia phytometabolites: Chemistry, biology, and omics","volume":"18","author":"Hao D. 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