Investigations of SCIO-469-like compounds for the inhibition of p38 MAP kinase

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 5, 2009, Pages 1461-1464

  Laufer, Stefan ^a   Lehmann, Frank ^a  

^a UNIVERSITY OF TÜBINGEN   (Germany)

Author keywords

Indoles; p38 MAPK; SAR

Indexed keywords

[4 (4 FLUOROBENZYL)PIPERAZIN 1 YL] (1H INDOL 2 YL)METHANONE; MITOGEN ACTIVATED PROTEIN KINASE P38; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; SCIO 469; UNCLASSIFIED DRUG;

ARTICLE; DRUG ACTIVITY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; INHIBITION KINETICS; STRUCTURE ACTIVITY RELATION;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; HUMANS; INDOLES; P38 MITOGEN-ACTIVATED PROTEIN KINASES; PROTEIN KINASE INHIBITORS;

EID: 60449110119     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.01.023     Document Type: Article

References (14)

1. Kumar S., Boehm J., and Lee J.C. Nat. Rev. Drug Discov. 2 (2003) 717
2. Ono K., and Han J. Cell Signalling 12 (2000) 1
3. Wagner G., and Laufer S. Med. Res. Rev. 26 (2006) 1
4. Hynes Jr. J., and Jeftheris K. Curr. Top. Med. Chem. 5 (2005) 967
5. Murali Dhar T.G., Wrobelski S.T., Lin S., Furch J.A., Nirschl D.S., Fan Y., Todderud G., Pitt S., Doweyko A.M., Sack J.S., Mathur A., McKinnon M., Barrish J.C., Dodd J.H., Schieven G.L., and Jeftheris K. Bioorg. Med. Chem. Lett. 17 (2007) 5019
6. Mavunkel B.J., Chakravarty S., Perumattam J.J., Luedtke G.R., Liang X., Lim D., Xu Y.-j., Laney M., Liu D.Y., Schreiner G.F., Lewicki J.A., and Dugar S. Bioorg. Med. Chem. Lett. 13 (2003) 3087
7. Jiang X., Tiwari A., Thompson M., Chen Z., Clearly T.P., and Lee T.B.K. Org. Process Res. Dev. 5 (2001) 604
8. 13C NMR, MS, IR, mp and HPLC. All experimental procedures and analytical data are given in Supporting Information.
9. Henn L., Hickey D.M.B., Moody C.J., and Rees C.W. J. Chem. Soc., Perkin Trans. 1 (1984) 2189
10. Ashram M. J. Chem. Soc., Perkin Trans. 2 (2002) 1662
11. Kaizerman J.A., Gross M.I., Ge Y., White S., Hu W., Duan J.X., Baird E.E., Johnson K.W., Tanaka R.D., Moser H.E., and Buerli R.W. J. Med. Chem. 46 (2003) 3914
12. Venable J.D., Cai H., Chai W., Dvorak C.A., Grice C.A., Jablonowski J.A., Shah C.R., Kwok A.K., Ly K.S., Pio B., Wei J., Desai P.J., Jiang W., Nguyen S., Ling P., Wilson S.J., Dunford P.J., Thurmond R.L., Lovenberg T.W., Karlsson L., Carruthers N.I., and Edwards J.P. J. Med. Chem. 48 (2005) 8289
13. Laufer S., Thuma S., Peifer C., Greim Y., Herweh Y., Albrecht A., and Dehner F. Anal. Biochem. 344 (2005) 135
14. Morris G.M., Goodsell D.S., Halliday R.S., Huey R., Hart W.E., Belew R.K., and Olson A.J. J. Comput. Chem. 19 (1998) 1639