Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593503 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
We have developed a new series of immunosuppressant with improved pharmacokinetic properties as the second-generation of colchicine analogs, which were designed based on the privileged structure derived from our previous work. In particular, we identified an analog (14), which exhibited a potent in vitro activity (IC50: 5Â nM) in MLR and excellent in vivo efficacy in the Zymosan A-induced arthritis model, in the Carrageenan-induced edema model and in the local lymph node assay (LLNA). Analog 14 also revealed a good oral bioavailability (F: 67.3%) in BALB/c mice.
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Authors
Dong-Jo Chang, Sujin Lee, Jaebong Jang, Soon-Ok Kim, Wan-Joo Kim, Young-Ger Suh,