Inhibitors of farnesyl protein transferase

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514357, 514399, 514562, 514450, 514459, 514461, 514432, 549271, 549293, 549295, 549 28, 549 9, 549 59, 549 65, 546268, 546283, 546284, 5483111, 5483151, 5483154, 530331, A61K 3144, A61K 31415, C07D31304

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active

054808936

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.

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Goldstein, J. L. et al., Nonfamesylated Tetrapeptide Inhibitors of Protein Farnesyltransferase*, (1991), Jour. of Biol. Chem., 266, pp. 15575-15578.
Reiss, Y., et al., Sequence requirement for peptide recognition by rat brain p21ras protein farnesyltransferase (1991), Proc. Natl. Acad. Sci., USA, 88, pp. 732-736.
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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