Design, synthesis and identification of novel colchicine-derived immunosuppressant

被引：26

作者：

Chang, Dong-Jo ^{[1
]}

Yoon, Eun-Young ^{[2
]}

Lee, Geon-Bong ^{[2
]}

Kim, Soon-Ok ^{[2
]}

Kim, Wan-Joo ^{[2
]}

Kim, Young-Myeong ^{[3
]}

Jung, Jong-Wha ^{[1
]}

An, Hongchan ^{[1
]}

Suh, Young-Ger ^{[1
]}

机构：

[1] Seoul Natl Univ, Coll Pharm, Seoul 151742, South Korea

[2] Suwon Univ, Chem Tech Res Inc, Team Biotech & Drug Dev, Hawseong 445743, South Korea

[3] Kangwon Natl Univ, Sch Med, Dept Mol & Cellular Biochem, Chunchon 200701, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 15期

关键词：

Immunosuppressant; Transplantation; Graft rejection; Autoimmune disease; Colchicine; Cyclosporin A; Skin-allograft; EXOGENOUS NITRIC-OXIDE; ORGAN-TRANSPLANTATION; GENE-EXPRESSION; CYCLOSPORINE-A; ALLOGRAFT; CYTOTOXICITY; HEPATOCYTES; CYCLOPHILIN; MODULATION; MECHANISM;

D O I：

10.1016/j.bmcl.2009.05.054

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4416 / 4420

页数：5

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