title: Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties.
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 (IC(50): 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.
authors.affiliation: College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors.forename: Dong-Jo
authors.initials: DJ
authors.lastname: Chang
authors.forename: Sujin
authors.initials: S
authors.lastname: Lee
authors.forename: Jaebong
authors.initials: J
authors.lastname: Jang
authors.forename: Soon-Ok
authors.initials: SO
authors.lastname: Kim
authors.forename: Wan-Joo
authors.initials: WJ
authors.lastname: Kim
authors.forename: Young-Ger
authors.initials: YG
authors.lastname: Suh
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001168:Arthritis / Q000188:drug therapy; D001682:Biological Availability; D003078:Colchicine / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D004195:Disease Models, Animal; D007166:Immunosuppressive Agents / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure
chemical_list: D007166:Immunosuppressive Agents; D003078:Colchicine