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초록
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.
키워드
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
- 제목
- Design, synthesis and identification of novel colchicine-derived immunosuppressant
- 저자
- Chang, Dong-Jo; Yoon, Eun-Young; Lee, Geon-Bong; Kim, Soon-Ok; Kim, Wan-Joo; Kim, Young-Myeong; Jung, Jong-Wha; An, Hongchan; Suh, Young-Ger
- 발행일
- 2009-08-01
- 유형
- Article
- 권
- 19
- 호
- 15
- 페이지
- 4416 ~ 4420