Synthesis and Evaluation of Indole Aspartyl Ketones as Novel Caspase-3 Inhibitors

被引：0

作者：

Sengupta, S. ^{[1
]}

Rao, G. Venkateshwar ^{[1
]}

Dubey, P. K. ^{[2
]}

机构：

[1] Aurigene Discovery Technol Ltd, Div Med Chem, Bangalore 560100, Karnataka, India

[2] Jawaharlal Nehru Technol Univ, Coll Engn, Dept Chem, Hyderabad 500085, Andhra Pradesh, India

来源：

ASIAN JOURNAL OF CHEMISTRY | 2011年 / 23卷 / 12期

关键词：

Caspase inhibitors; Cysteine proteases; IDN-6556; Indole-N-acetic acid; IN-VIVO; POTENT; FLUOROMETHYLKETONES; APOPTOSIS; INTERLEUKIN-1-BETA; ACTIVATION; DIPEPTIDES; DISCOVERY; SAR;

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Synthesis, biological evaluation and structure-activity relationships for a series of novel nonpeptide small molecule inhibitors of caspase-3 are described. Among the synthesized compounds, 2,3,5,6-tetrafluorophenoxymethyl ketone derivatives of indole-N-acetamides have been identified as potent inhibitors of caspase-3. The most active compound within this series (9a) inhibited caspase-3 with an IC50 = 0.64 mu M.

引用

页码：5517 / 5520

页数：4

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