Diarylether inhibitors of farnesyl-protein transferase

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 10, 1997, Pages 1345-1348

  Dinsmore, Christopher J ^a   Williams, Theresa M ^a   Hamilton, Kelly ^a   O'Neill, Timothy J ^a   Rands, Elaine ^a   Koblan, Kenneth S ^a   Kohl, Nancy E ^a   Gibbs, Jackson B ^a   Graham, Samuel L ^a   Hartman, George D ^a   Oliff, Allen I ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYSTEINE DERIVATIVE; ENZYME INHIBITOR; ETHER DERIVATIVE; FARNESYL TRANS TRANSFERASE; TRANSFERASE INHIBITOR;

ARTICLE; DRUG DESIGN; DRUG SYNTHESIS; ENZYME INHIBITION; IN VITRO STUDY; STRUCTURE ACTIVITY RELATION;

EID: 0031579949     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00225-4     Document Type: Article

References (16)

1. (a) Barbacid, M. Annu. Rev. Biochem. 1987, 56, 779.
2. (b) Kato, K.; Cox, A.D.; Hisaka, M.M.; Graham, S.M.; Buss, J.E.; Der, C.J. Proc. Natl. Acad. Sci. U.S.A. 1992, 89, 6403.
3. Rodenhuis S. Semin. Cancer Biol. 3:1992;241.
4. (a) CaaX; 'C' = cysteine, 'a' = any aliphatic amino acid, 'X' = a prenylation specificity residue
5. (b) Reiss, Y.; Goldstein, J.L.; Seabra, M.C.; Casey, P.J.; Brown, M.S.; Cell 1990, 62, 81.
6. (a) Gibbs, J.B. Cell 1991, 65, 1.
7. (b) Gibbs, J.B.; Oliff, A.I.; Kohl, N.E. Cell 1994, 77, 175.
8. (a) Moores, S.L.; Shaber, M.D.; Mosser, S.D.; Rands, E.; O'Hara, M.B.; Garsky, V.M.; Marshall, M.S.; Pompliano, D.L.; Gibbs, J.B. J. Biol. Chem. 1991, 266, 14603.
9. (b) Kohl, N.E.; Mosser, S.D.; deSolms, S.J.; Giuliani, E.A.; Pompliano, D.L.; Graham, S.L.; Smith, R.L.; Scolnick, E.M.; Oliff, A.I.; Gibbs, J.B. Science 1993, 260, 1934.
10. (a) Kohl, N.E.; Wilson, F.R.; Mosser, S.D.; Giuliani, E.A.; deSolms, S.J.; Conner, M.W.; Anthony, N.J.; Holtz, W.J.; Gomez, R.P.; Lee, T.-J.; Smith, R.L.; Graham, S.L.; Hartman, G.D.; Gibbs, J.B.; Oliff, A.I. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 9141.
11. (b) Kohl, N.E.; Omer, C.A.; Conner, M.W.; Anthony, N.J.; Davide, J.P.; deSolms, S.J.; Giuliani, E.A.; Gomez, R.P.; Graham, S.L.; Hamilton, K.; Handt, L.K.; Hartman, G.D.; Koblan, K.S.; Kral, A.M.; Miller, P.J.; Mosser, S.D.; O'Neill, T.J.; Shaber, M.D.; Gibbs, J.B.; Oliff, A.I. Nature Med. 1995, 1, 792.
12. (a) Graham, S.L. Exp. Opin. Ther. Patents 1995, 5, 1269.
13. (b) Vogt, A.; Quian, Y.; Blaskovich, M.A.; Fossum. R.D.; Hamilton, A.D.; Sebti, S.M. J. Biol. Chem. 1995, 270, 660.
14. (c) Quian, Y.; Vogt, A.; Sebti, S.M.; Hamilton, A.D. J. Med. Chem. 1996, 39, 217.
15. (d) deSolms, S.J.; Deana, A.A.; Giuliani, E.A.; Graham, S.L.; Kohl, N.E.; Mosser, S.D.; Oliff, A.I.; Pompliano, D.L.; Rands, E.; Scholz, T.H.; Wiggins, J.M.; Gibbs, J.B.; Smith, R.L. J. Med. Chem. 1995, 38, 3967.
16. (e) Williams, T.M.; Ciccarone, T.M.; MacTough, S.C.; Bock, R.L.; Conner, M.W.; Davide, J.P.; Hamilton, K.; Koblan, K.S.; Kohl, N.E.; Kral, A.M.; Mosser, S.D.; Omer, C.A.; Pompliano, D.L.; Rands, E.; Shaber, M.D.; Shah, D.; Wilson, F.R.; Gibbs, J.B.; Graham, S.L.; Hartman, G.D.; Oliff, A.I.; Smith, R.L. J. Med. Chem. 1996, 39, 1345.