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.
Original language | English |
---|---|
Pages (from-to) | 4416-4420 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 19 |
Issue number | 15 |
DOIs | |
State | Published - 1 Aug 2009 |
Keywords
- Autoimmune disease
- Colchicine
- Cyclosporin A
- Graft rejection
- Immunosuppressant
- Skin-allograft
- Transplantation