Derivatives of iressa, a specific epidermal growth factor receptor inhibitor, are powerful apoptosis inducers in PC3 prostatic cancer cells
Derivatives of iressa, a specific epidermal growth factor receptor inhibitor, are powerful apoptosis inducers in PC3 prostatic cancer cells
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DOI：
10.1002/cmdc.200600128
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发表时间：
2007-03-01
期刊：
影响因子：
3.4
通讯作者：
Henichart, Jean-Pierre
中科院分区：
文献类型：
--
作者：
Telliez, Aurelie;Desroses, Matthieu;Henichart, Jean-Pierre
表皮生长因子受体（EGFR）的酪氨酸激酶活性广泛参与信号通路，并在癌症中经常失调。它在前列腺癌发展中的作用已经得到了很好的证实，并且已经提出了一些治疗策略，例如用小分子酪氨酸激酶抑制剂阻断细胞内酪氨酸激酶结构域。本文描述了C6-和c7 -取代的4-苯胺喹啉、易瑞沙类似物和强效促凋亡诱导剂在激素非依赖性前列腺癌PC3细胞系中的合成和体外药理学性质。
The tyrosine kinase activity of the epidermal growth factor receptor (EGFR) is widely involved in signaling pathways and often de-regulated in cancer. Its role in the development of prostate cancer is well established, and therapeutic strategies such as blockade of the intracellular tyrosine kinase domain with small-molecule tyrosine kinase inhibitors have been proposed. Herein we describe the synthesis and in vitro pharmacological properties of C6- and C7-substituted 4-anilinoquinazolines, analogues of Iressa and powerful proapoptotic inducers in hormone-independent prostate cancer PC3 cell lines.