Farnesyl protein transferase inhibitors

Kaminski, J.J., Rane, D.F., Snow, M.E., Weber, L, and Rothofsky, M.L Identification of novel farnesyl protein transferase inhibitors using three-dimensional database searching methods./. Med. Chem. 1997, 40, 4103-4112. 

Horvath D. (2001b) ComPharm—Automated comparative analysis of phar-macophoric patterns and derived QSAR approaches, novel tools in high throughput drug discovery. A proof-of-concept study applied to farnesyl protein transferase inhibitor design. In M Diudea (ed), QSPR/QSAR Studies by Molecular Descriptors, pp. 395-439, Nova Science Publishers, New York, USA. 

Fig. 4 CAAX competitive heterocyclic farnesyl protein transferase inhibitors. The inhibitors shown in the first row are reported to be in phase I, II, or III clinical development...

Patnaik A, Rowinsky EK (2001) Early clinical experience with farnesyl protein transferase inhibitors. In Sebti SM, Hamilton AD (eds) Farnesyltransferase inhibitors in cancer therapy. Humana, Totowa, NJ, pp 233-249... 

End DW, Mevellec L, Angibaud P (2007) Farnesyl Protein Transferase Inhibitors Medicinal Chemistry, Molecular Mechanisms, and Progress in the Clinic. 1 115-150... 

S Omura, D Van der Pyl, J Inokoshi, Y Takahashi, H Takeshima. Pepticinnamins, new farnesyl-protein transferase inhibitors produced by an actinomycete. I. Producing strain, fermentation, isolation and biological activity. J Antibiot 46 222-228, 1993. 

Disubstituted-2,3,4,5-tetrahydro-lH-l,4-benzodiazepine derivatives, (VI), prepared by Kronenthal (4) were effective as farnesyl protein transferase inhibitors and used in the treatment of colon cancer and other proliferative diseases. 

Whyte, D.B., et al. (1997). K- and N-Ras are geranylgeranylated in cells trated with farnesyl protein transferase inhibitors. J Biol Chem 272 14459-14464. 

Mangues, R., Corral, T., Kohl, N.E., Symmans, W.F., Lu, S., Malumbres, M., Gibbs, J.B., Oliff, A., and Pellicer, A. (1998). Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice. Cancer Res 58 1253-1259. 

Adjei, A.A., Croghan, G.A., Erlichman, C., Marks, R.S., Reid, J.M., Sloan, J.A., Pitot, H. C., Alberts, S.R., Goldberg, R.M., Hanson, L.J., Bruzek, L.M., Atherton, P., etal. (2003). A Phase I trial of the farnesyl protein transferase inhibitor R115777 in combination with gemcitabine and cisplatin in patients with advanced cancer. Clin Cancer Res 9 2520-2526. 

Mangues, R., et at. (1998). Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice. Cancer Res 58 1253-1259. 

Omer, C.A., et at. (2000). Mouse mammary tumor virus-Ki-rasB transgenic mice develop mammary carcinomas that can be growth-inhibited by a farnesyl protein transferase inhibitor. Cancer Res 60 2680-2688. 

Rubin E, Abbruzzese JL, Morrison BW, Mazina K, Lee Y. 2000. Phase I trial of the farnesyl protein transferase inhibitor L-778,123 on a 14- or 28-day dosing schedule. Proc. Am. Soc. Clin. Oncol. 19 718... 

Liu M, Bryant MS, Chen J, Lee S, Yaremko B, et al. 1999. Effects of SCH 59228, an orally bioavailable farnesyl protein transferase inhibitor, on the growth of oncogene-transformed fibroblasts and a human colon carcinoma xenograft in nude mice. Cancer Chemother. Pharmacol. 43 50-58... 

TL, Fuery CJ, et al. 2001. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 61 131-37... 

I and pharmacokinetic study of farnesyl protein transferase inhibitor R115777 in advanced cancer. J. Clin. Oncol. 18 927-41... 

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