Inhibitory effect of curcumin analogs on tissue factor procoagulant activity and their preliminary structure-activity relationships

被引：4
作者：
Ge, Hai-Xia [1 ]
Chen, Ling [3 ]
Zhang, Jian [2 ]
Kou, Jun-Ping [3 ]
Yu, Bo-Yang [3 ]
机构：
[1] Huzhou Teachers Coll, Dept Pharm, Huzhou 313000, Peoples R China
[2] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
[3] China Pharmaceut Univ, Dept Complex Prescript Tradit Chinese Med, Nanjing 211198, Jiangsu, Peoples R China
来源：
MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 07期
关键词：
Curcumin analogs; Tissue factor; Structure-activity relationships (SAR); MONO-CARBONYL ANALOGS; POTENTIAL ANTIOXIDANT; CELL; PROLIFERATION;
D O I：
10.1007/s00044-012-0330-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
With the aim to explore the multifunctional behaviors of curcumin analogs and to discover new small molecular tissue factor inhibitors, twelve mono carbonyl curcumin analogs of three classes were synthesized and their effect on tissue factor procoagulant activity was evaluated in the human monoblastic leukemia THP-1 cells stimulated by LPS. The most potent compounds 2a exhibited the dramatically enhanced activity with the IC50 values of 0.053 nM. Their preliminary structure-activity relationship was also discussed.
引用
收藏
页码：3242 / 3246
页数：5
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