Download MendeleyAryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
Gwaltney II, S.L., O'Connor, S.J., Nelson, L.T., Sullivan, G.M., Imade, H., Wang, W., Hasvold, L., Li, Q., Cohen, J., Gu, W.Z., Tahir, S.K., Bauch, J., Marsh, K., Ng, S.C., Frost, D.J., Zhang, H., Muchmore, S., Jakob, C.G., Stoll, V., Hutchins, C., Rosenberg, S.H., Sham, H.L.(2003) Bioorg Med Chem Lett 13: 1359-1362
- PubMed: 12657282
- DOI: https://doi.org/10.1016/s0960-894x(03)00095-7
- Primary Citation of Related Structures:
1N94, 1N95 - PubMed Abstract:
Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.
Organizational Affiliation:
Pharmaceutical Discovery, R47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. stephen.gwaltney@syrrx.com
