2019
DOI: 10.1111/cbdd.13567
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Synthesis of novel tanshinone derivatives for treatment of castration‐resistant prostate cancer

Abstract: 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‐resistant 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‐mediated AR transactivation and cell viability assay were performed to test the synthesized compounds.… Show more

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Cited by 12 publications
(8 citation statements)
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“…Tanshinone capsules can treat FSD through the following mechanism. Firstly, tanshinone has an anti-androgen effect and estrogen activity, which can regulate skin endocrine and metabolic function, and maintain hormone balance (39,40). Secondly, tanshinone capsules have a broad-spectrum antibacterial effects, such as hydroxytanshinone and methyl tanshinate can kill and inhibit a variety of aerobic and anaerobic bacteria, especially can inhibit gram-positive bacteria (41,42).…”
Section: Discussionmentioning
confidence: 99%
“…Tanshinone capsules can treat FSD through the following mechanism. Firstly, tanshinone has an anti-androgen effect and estrogen activity, which can regulate skin endocrine and metabolic function, and maintain hormone balance (39,40). Secondly, tanshinone capsules have a broad-spectrum antibacterial effects, such as hydroxytanshinone and methyl tanshinate can kill and inhibit a variety of aerobic and anaerobic bacteria, especially can inhibit gram-positive bacteria (41,42).…”
Section: Discussionmentioning
confidence: 99%
“…毕跃峰等 [9] 为改善丹参酮 IIA 的水溶性, 运用孪药 设计原理, 将丹参水溶性酚酸类结构通过酯键引入 A 秦洪波等 [10] 胞的生长起着重要作用, 雄激素受体是治疗前列腺癌的 主要靶点. 徐德峰等 [11] 以丹参酮 IIA 为原料, 在乙酸/乙 酸铵反应体系中与取代苯甲醛进行 Debus-Radziszewski 多种致癌基因(如 c-myc、K-ras、Bcl-2 等)在转移性 三阴乳腺癌(TNBC)中过表达, 致癌基因启动子中存在 大量富含鸟嘌呤的序列, 在生理条件下可形成 G-四联 体(G4)结构, 使其成为潜在的癌症治疗靶点 [12a-12b] . Vilar…”
Section: A 环结构优化unclassified
“…However, after 18 months of treatment, the majority of the patients relapsed subsequently, an initial response to ADT, and acquired CRPC. Therefore, there is an urgent need to discover more efficacious AR-suppressing agents for the treatment of CRPC (Xu et al, 2019).…”
Section: Natural Therapeutic Products For Castration-resistant Prostate Cancer Treatment and Managementmentioning
confidence: 99%