Design and synthesis of indoline thiohydantoin derivatives based on enzalutamide as antiproliferative agents against prostate cancer

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• 作者：Minzan Zuo¹ ; Xi Xu¹ ; Zhouling Xie ; Raoling Ge ; Ziyu Zhang ; Zhiyu Li ; ^{zhiyuli@cpu.edu.cn} ; Jinlei Bian
• 关键词：Prostate cancer ; Androgen receptor ; Antagonist ; Indoline thiohydantoin derivatives
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：1002-1022
• 全文大小：2586 K
• 卷排序：125

文摘

A series of indoline thiohydantoin derivatives were synthesized and evaluated in vitro. The most potent compound 48c shows comparable ability with enzalutamide in proliferation inhibition of LNCaP cells. Compound 48c has less cytotoxic to AR-negative cells compared with Enzalutamide. The bicalutamide-resistant mechanism was clarified and overcome by compound 48c.