Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties

DJ Chang, S Lee, J Jang, SO Kim, WJ Kim…

Index: Chang, Dong-Jo; Lee, Sujin; Jang, Jaebong; Suh, Young-Ger; Kim, Soon-Ok; Kim, Wan-Joo Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 21 p. 6750 - 6755,6

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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: 5nM) in MLR and excellent in vivo efficacy in the Zymosan A-induced arthritis model, in the Carrageenan-induced edema ...

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