4386
B. Lagu et al. / Bioorg. Med. Chem. Lett. 17 (2007) 4382–4386
16. Hashimoto, H.; Ikemoto, T.; Itoh, T.; Maruyama, H.;
References and notes
Hanaoka, T.; Wakimasu, M.; Mitsudera, H.; Tomimatsu,
K. Org. Process Res. Dev. 2002, 6, 70.
1. Bachman, M. F.; Kopf, M.; Marsland, B. J. Nat. Rev.
Immunol. 2006, 103, 3733.
2. Rollins, B. J. Mol. Med. Today 1996, 2, 198.
3. Dawson, J.; Miltz, W.; Mir, A. K.; Weissner, C. Expert
Opin. Ther. Targets 2003, 7, 35.
4. Feria, M.; Diaz-Gonzalez, F. Expert Opin. Ther. Pat.
2006, 16, 49.
5. Saunders,J.;Tarby,C.M.DrugDiscoveryToday1999,4,80.
6. Boring, L.; Gosling, J.; Chensue, S. W.; Kunkel, S. L.;
Farsee, R. V.; Broxmeyer, H. E.; Charo, I. F. J. Clin.
Invest. 1997, 100, 2552.
17. THP-1 cells were incubated with 0.5 nM 125-I labeled
MCP-1 (Perkin-Elmer Life Sciences, Inc., Boston, MA) in
the presence of varying concentrations of either unlabeled
MCP-1 (R&D systems, Minneapolis, MN)or the test
compound for 2 h at 30 °C in a 96-well plate. Cells were
then harvested onto a filter plate, dried, and 20 lL of
Microscint-20 was added to each well. Plates were counted
in a TopCount NXT microplate scintillation and lumi-
nescence counter (Perkin-Elmer Life Sciences, Inc., Bos-
ton, MA). Blank values (buffer only) were subtracted from
all the values and drug treated values were compared to
vehicle treated values. One micromolar cold MCP-1 was
used for non-specific binding.
7. Kuziel, W. A.; Morgan, S. J.; Dawson, T. C.; Griffin, S.;
Smithies, O.; Ley, K.; Maeda, N. Proc. Natl. Acad. Sci.
U.S.A. 1997, 94, 12053.
18. In this model, mice are injected ip with zymosan, a
polysaccharide derived from the cell walls of yeast
(Saccharomyces cerevisiae). A rapid influx of neutro-
phils into the peritoneal cavity occurs, peaking at
8. Gao, Z.; Metz, W. A. Chem. Rev. 2003, 103, 3733.
9. Forbes, I. T.; Cooper, D. G.; Dodds, E. K.; Hickey, D. M.
B.; Ife, R. J.; Messon, M.; Stockley, M.; Berkhout, T. A.;
Gohil, J.; Groot, P. H. E.; Moores, K. Bioorg. Med. Chem.
Lett. 2000, 1803.
10. Witherington, J.; Bordas, V.; Cooper, D. G.; Forbes, I. T.;
Gribble, A. D.; Ife, R. J.; Berkhout, T. A.; Gohil, J.; Groot,
P. H. E.; Moores, K. Bioorg. Med. Chem. Lett. 2000, 1803.
11. Pasternak, A.; Marino, D.; Vicario, P. P.; Ayala, J. M.;
Casceierri, M.; Parsons, W.; Mills, S. G.; MacCoss, M.;
Yang, L. J. Med. Chem. 2006, 49, 4801.
ꢀ4 h, which is followed by
a wave of monocyte
infiltration which is maximal at 16–24 h. MCP-1
concentration in peritoneal lavage fluid peaks at
ꢀ4 h, and an antibody to MCP-1 significantly inhibits
monocyte infiltration.
19. Ajuebor, M. N.; Flower, R. J.; Hannon, R.; Christie, M.;
Bowers, K.; Verity, A.; Perretti, M. J. Leukocyte Biol.
1998, 63, 108.
20. Alam, R.; York, J.; Boyars, M.; Stafford, S.; Grant, J. A.;
Lee, J.; Forsythe, P.; Sim, T.; Ida, N. Am. J. Respir. Crit.
Care Med. 1996, 153, 1398.
12. Mirazadegan, T.; Diehl, F.; Ebi, B.; Bhakta, S.; Polsky, I.;
McCarley, D.; Mulkins, M.; Weatherhead, G. S.; Lapi-
erre, J. M.; Dankwardt, J.; Morgans, D., Jr.; Wilhelm, R.;
Jarnagin, K. J. Biol. Chem. 2000, 275, 25562.
21. Hsieh, K. H.; Chou, C. C.; Chiang, B. L. J. Allergy Clin.
Immunol. 1996, 98, 580.
22. Gonzalo, J. A.; Lloyd, C. M.; Wen, D.; Albar, J. P.; Wells,
T. N. C.; Proudfoot, A.; Martinez, A. C.; Dorf, M.;
Bjerke, T.; Coyle, A. J.; Gutierrez-Ramos, J. J. Exp. Med.
1998, 188, 157.
13. Moree, W. J.; Kataoka, K.; Ramirez-Weinhouse, M. M.;
Shiota, T.; Imai, M.; Sudo, M.; Tsutsumi, T.; Endo, N.;
Muroga, Y.; hada, T.; Tanaka, H.; Morita, T.; Greene, J.;
Barnum, D.; Saunders, J.; Kato, Y.; Meyers, P. L.; Tarby,
C. M. Bioorg. Med. Chem. Lett. 2004, 14, 5413.
14. Warner-Lambert Co. US6,184235B1.
23. Barnes, P. J. Nat. Rev. Drug Disc. 2004, 10, 831.
24. Williams, C. J.; Galli, S. J. J. Exp. Med. 2000, 192,
455.
15. Shirashi, M.; Aramaki, Y.; Seto, H.; Nishikawa, Y.;
Kanzaki, N.; Okamoto, M.; Sawda, H.; Nishimura, O.;
Baba, M.; Fujino, M. J. Med. Chem. 2000, 43, 2049.