Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-03-14
1995-08-08
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514212, 514315, 514419, 514423, 540608, 546147, 546245, 548492, 548531, 548536, C07D21712
Patent
active
054399181
ABSTRACT:
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.
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Kohl, N. E. et al., "Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice", Proc. Natl. Acad. Sci. USA, vol. 91, pp. 9141-9145 (1994).
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Goldstein, J. S., et al. Journal of Biological Chemistry, vol. 266, No. 24, pp. 15575-15578 (1991).
James, G. L. et al., Benzodiazepine Peptidomimetics: Potent Inhibitors of Ras Farnesylation in Animal Cells, (1993), Science, 260, pp. 1937-1942.
Kohl, N. E. et al., Selective Inhibition of ras-Dependent Transformation by a Farnesyltransferase Inhibitor, (1993), Science, 260, pp. 1934-1937.
Leftheris, K. et al., Peptide Based P21RAS Famesyl Transferase Inhibitors: Systematic Modification of the Tetrapepttide CA1A2X Motif, (1994), Bioorganic & Medicinal Chemistry Letters, 4, No. 7, pp. 887-892.
Pompliano, D. L. et al., Steady-State Kinetic Mechanism of Ras Farnesyl: Protein Transferase, (1992), Biochemistry, 31, pp. 3800-3807.
Qian, Y. et al., Design and Structural Requirements of Potent Peptidomimetic Inhibitors of p21ras Farnesyltransferase, (1994), The Journal of Biological Chemistry, 269, No. 17, pp. 12410-12413.
Reiss, Y. et al., Inhibition of Purified p21ras Farnesyl: Protein Transferase by Cys-AAX Tetrapeptides, (1990), Cell, 62, pp. 81-88.
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deSolms S. Jane
Graham Samuel L.
Daniel Mark R.
Davis Zinna N.
DiPrima Joseph F.
Ivy C. Warren
Merck & Co. , Inc.
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