PMID- 23017885
OWN - NLM
STAT- MEDLINE
DCOM- 20130320
LR  - 20131121
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Linking)
VI  - 22
IP  - 21
DP  - 2012 Nov 1
TI  - Part II. Development of novel colchicine-derived immunosuppressants with improved 
      pharmacokinetic properties.
PG  - 6750-5
LID - S0960-894X(12)01079-7 [pii]
LID - 10.1016/j.bmcl.2012.08.068 [doi]
AB  - 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.
CI  - Copyright (c) 2012 Elsevier Ltd. All rights reserved.
FAU - Chang, Dong-Jo
AU  - Chang DJ
AD  - College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 
      151-742, Republic of Korea.
FAU - Lee, Sujin
AU  - Lee S
FAU - Jang, Jaebong
AU  - Jang J
FAU - Kim, Soon-Ok
AU  - Kim SO
FAU - Kim, Wan-Joo
AU  - Kim WJ
FAU - Suh, Young-Ger
AU  - Suh YG
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20120825
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Immunosuppressive Agents)
RN  - SML2Y3J35T (Colchicine)
SB  - IM
MH  - Administration, Oral
MH  - Animals
MH  - Arthritis/drug therapy
MH  - Biological Availability
MH  - Colchicine/*chemistry/*pharmacokinetics/pharmacology
MH  - Disease Models, Animal
MH  - Immunosuppressive Agents/*chemistry/*pharmacokinetics/pharmacology
MH  - Inhibitory Concentration 50
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - Molecular Structure
EDAT- 2012/09/29 06:00
MHDA- 2013/03/21 06:00
CRDT- 2012/09/29 06:00
PHST- 2012/07/30 00:00 [received]
PHST- 2012/08/15 00:00 [revised]
PHST- 2012/08/17 00:00 [accepted]
PHST- 2012/09/29 06:00 [entrez]
PHST- 2012/09/29 06:00 [pubmed]
PHST- 2013/03/21 06:00 [medline]
AID - S0960-894X(12)01079-7 [pii]
AID - 10.1016/j.bmcl.2012.08.068 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2012 Nov 1;22(21):6750-5. doi: 10.1016/j.bmcl.2012.08.068. 
      Epub 2012 Aug 25.