Synthesis and Biological Evaluation of 7-Azaisoindigo Derivatives

被引：7

作者：

Wang, Zhao-Hui ^{[1
]}

Wang, Tao ^{[2
]}

Yao, Shi-Ning ^{[3
]}

Chen, Jing-cai ^{[3
]}

Hua, Wei-Yi ^{[1
]}

Yao, Qi-Zheng ^{[1
]}

机构：

[1] China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China

[2] China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210009, Peoples R China

[3] Wuxi JC Pharmaceut Technol Inc, Wuxi, Peoples R China

来源：

ARCHIV DER PHARMAZIE | 2010年 / 343卷 / 03期

关键词：

Antitumor activity; 7-Azaisoindigo; CDK2/cyclin A assay; Synthesis; CYCLIN-DEPENDENT KINASES; CHRONIC MYELOGENOUS LEUKEMIA; INDIRUBINS; MEISOINDIGO; INHIBITORS; CHINA;

D O I：

10.1002/ardp.200900268

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 7-azaisoindigo derivatives 3-14 were designed, synthesized, and structurally characterized by IR, (1)H-NMR, (13)C-NMR, mass spectra, and elemental analyses. Their antiproliferative activities were evaluated in a hormone-independent prostate cancer cell line DU145. Among them, compounds 8, 9, 14 showed the highest activities. Our study also showed that compounds 7, 11, 12 exhibited higher inhibitory activities on CDK2/cyclin A than that of the positive control meisoindigo. Western blot analysis on DU145 cells treated with compounds 7 and 9 demonstrated that 7-azaisoindigo derivatives could decrease the level of CDK2 activity (phosphorylation) and the expression of cyclin D1, and increase the expression of endogenous cyclin-dependent inhibitor p27.

引用

页码：160 / 166

页数：7

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