Thorsten E. Fisher

Synthesis and biological activity of ras farnesyl protein transferase inhibitors. Tetrapeptide analogs with amino methyl and carbon linkages.

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.

An efficient synthesis of γ-alkylated E-olefin dipeptide isosteres

Abstract An efficient synthetic sequence was developed for the preparation of γ-alkylated E-olefin isosteres of dipeptides.

Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.

Compound affinity for activated and resting GPIIb/IIIa receptors may differ, and comparison of those differences determines selectivity. Structural features that influence selectivity are discussed.

Synthesis of 3-Alkyl-6-bromo-4,5-E-hexenoate

Abstract Two complementary routes for the preparation of 3-alkyl-6-bromo-4,5-E-hexenoate are reported.