1. Academic Validation
  2. Design, synthesis and identification of novel colchicine-derived immunosuppressant

Design, synthesis and identification of novel colchicine-derived immunosuppressant

  • Bioorg Med Chem Lett. 2009 Aug 1;19(15):4416-20. doi: 10.1016/j.bmcl.2009.05.054.
Dong-Jo Chang 1 Eun-Young Yoon Geon-Bong Lee Soon-Ok Kim Wan-Joo Kim Young-Myeong Kim Jong-Wha Jung Hongchan An Young-Ger Suh
Affiliations

Affiliation

  • 1 College of Pharmacy, Seoul National University, San 56-1, Sillim-dong, Gwanak-gu, Seoul 151-742, Republic of Korea.
Abstract

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.

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