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Therapeutic uses of curcumin analogs for treatment of prostate cancer

机译:姜黄素类似物在治疗前列腺癌中的治疗用途

摘要

This invention relates generally to methods of treating aggressive cancers, such as hormone-refractory metastatic prostate cancer, by exposing the aggressive cancer cells to curcumin analogs having the claimed structural scaffolds and side groups. The anticancer effects of curcumin are associated with its influence on numerous growth factors within the cells. However, its clinical development has been limited by its suboptimal pharmacokinetics and poor bioavailability caused by poor solubility in water and rapid in vivo metabolism. There is the need to develop new and improved curcumin analogs with better potency, water solubility, and in vivo metabolic stability, as well as retained safety profiles. Curcumin analogs having one of the claimed four novel scaffolds with basic heteroaromatic side groups show the ability to decrease aggressive cancer cell viability and to inhibit aggressive cancer cell growth.
机译:本发明一般涉及通过将侵袭性癌细胞暴露于具有所要求保护的结构支架和侧基的姜黄素类似物来治疗侵袭性癌症,例如激素难治性转移性前列腺癌的方法。姜黄素的抗癌作用与其对细胞内众多生长因子的影响有关。然而,其临床发展受到其次佳的药代动力学和因水溶性差和体内快速代谢所引起的生物利用度差的限制。需要开发新的和改进的姜黄素类似物,其具有更好的效力,水溶性和体内代谢稳定性以及保留的安全性。具有要求保护的四个具有基本杂芳族侧基的新颖支架之一的姜黄素类似物显示出降低侵袭性癌细胞生存力和抑制侵袭性癌细胞生长的能力。

著录项

  • 公开/公告号US9499529B2

    专利类型

  • 公开/公告日2016-11-22

    原文格式PDF

  • 申请/专利权人 CALIFORNIA STATE UNIVERSITY FRESNO;

    申请/专利号US201414318295

  • 发明设计人 QIAO-HONG CHEN;

    申请日2014-06-27

  • 分类号C07D403/06;C07D413/06;C07D417/06;C07D413/14;C07D413/08;

  • 国家 US

  • 入库时间 2022-08-21 13:42:04

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