44804-88-8Relevant academic research and scientific papers
Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties
Chang, Dong-Jo,Lee, Sujin,Jang, Jaebong,Suh, Young-Ger,Kim, Soon-Ok,Kim, Wan-Joo
, p. 6750 - 6755,6 (2012)
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: 5 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.
