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  • Title: Synthesis and biological activity of ras farnesyl protein transferase inhibitors. Tetrapeptide analogs with amino methyl and carbon linkages.
    Author: Wai JS, Bamberger DL, Fisher TE, Graham SL, Smith RL, Gibbs JB, Mosser SD, Oliff AI, Pompliano DL, Rands E.
    Journal: Bioorg Med Chem; 1994 Sep; 2(9):939-47. PubMed ID: 7712129.
    Abstract:
    Replacement of the central amino methylene linkage of C[psi CH2NH]A[psi CH2NH]AX tetrapeptide inhibitors with carbon tethers led to compounds with potency in the nanomolar range. Some of the more potent olefinic compounds inhibit Ras processing in intact v-ras transformed NIH 3T3 cells with IC50 values in the 0.1 to 1 microM range, and inhibit selectively the anchorage-independent growth of H-ras transformed Rat1 cells at 10 microM.
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