Inhibitors of farnesyl-protein transferase

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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5483381, C07D23326

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active

060282010

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 the farnesylation of the oncogene protein Ras.

REFERENCES:
patent: 4294925 (1981-10-01), Liu
patent: 4576957 (1986-03-01), Marsico, Jr. et al.
patent: 5141851 (1992-08-01), Brown et al.
patent: 5185358 (1993-02-01), Creswell
patent: 5238922 (1993-08-01), Graham et al.
patent: 5326773 (1994-07-01), Desolms et al.
patent: 5340828 (1994-08-01), Graham et al.
patent: 5352705 (1994-10-01), Deana et al.
patent: 5439918 (1995-08-01), Desolms et al.
patent: 5468733 (1995-11-01), Desolms et al.
patent: 5480893 (1996-01-01), Graham et al.
patent: 5491164 (1996-02-01), Desolms et al.
patent: 5504212 (1996-04-01), Desolms et al.
patent: 5534537 (1996-07-01), Ciccarone et al.
patent: 5571835 (1996-11-01), Anthony et al.
patent: 5585359 (1996-12-01), Breslin et al.
patent: 5593988 (1997-01-01), Tahara
Mocko, Coll. Czech. Chem. Comm. 49 190-6, 1964.
Gibbs, J.B. et al., "Selective Inhibition of Farnesyl-Protein Transferase Blocks Ras Processing in Vivo," The Journal of Biological Chemistry, vol. 268, No. 11, pp. 7617-7620 (1993).
Goldstein, J.L. et al., "Nonfarnesylated Tetrapeptide Inhibitors of Protein Farnesyltransferase," The Journal of Biological Chemistry, vol. 266, No. 24, pp. 15575-15578 (1991).
Graham, S.L., "Inhibitors of protein farnesylation: a new approach to cancer chemotheraphy," Exp. Opin. Ther. Patents vol. 5 (12), pp. 1269-1285 (1995).
James, G.L. et al., "Benzodiazepine Peptidomimetic BZA-5B Interrupts the MAP Kinase Activation Pathway in H-Ras-transformed Rat-1 Cells, but Not in Untransformed Cells," The Jour. of Biol. Chem., vol. 269, No. 44, pp. 27705-27714 (1994).
James, G.L. et al., "Benzodiazepine Peptidomimetics: Potent Inhibitors of Ras Farnesylation in Animal Cells", Science, vol. 260, pp. 1937-1942 (1993).
James, G., et al., "Polylysine and CVIM Sequences of K-RasB Dictate Specificity of Prenylation and Confer Resistance to Benzodiazepine Peptidomimetic in Vitro", The Jour. of Biol. Chem., vol. 270, No. 11, pp. 6221-6226 (1995).
Kohl, N.E. et al., "Selective Inhibition of ras-Dependent Transformation by a Farnesyltransferase Inhibitor", Science, vol. 260, pp. 1934-1937 (1993).
Kohl, N.E. et al., "Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice", Proc. Natl. Acad. Sci. USA, Med. Sciences, vol. 91, pp. 9141-9145 (1994).
Kohl, N.E. et al., "Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice," Nature Medicine, vol. 1, No. 8, pp. 792-797 (1995).
Pompliano, D.L., "Steady-State Kinetic Mechanism of Ras Farnesyl:Protein Transferase," Biochemistry, vol. 31, pp. 3800-3807 (1992).
Sepp-Lorenzino, L., et al., "A Peptidomimetic Inhibitor of Farnesyl:Protein Transferase Blocks the Anchorage-dependent and -independent Growth of Human Tumor Cell Lines," Cancer Research, vol. 55, pp. 5302-5309 (1995).
Aldrich Catalogue p 295 #14215-8, 1996.

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