476494-04-9

Upstream product

• 23147-58-2 glycolaldehyde dimer 
• 476494-03-8 methanesulfonic acid 8-{2-[2-(1-trityl-1H-imidazol-4-yl)-ethylamino]-acetylamino}-naphthalen-2-yl ester 
• 312937-01-2 2,2,2-trifluoro-N-(2-(1-trityl-1H-imidazol-4-yl)ethyl)acetamide 
• 267659-67-6 methanesulfonic acid 8-(2-chloroacetylamino)naphthalen-2-yl ester 
• 50580-77-3 2,2,2-trifluoro-N-[2-(1H-imidazol-4-yl)ethyl]acetamide 
• 51-45-6 histamine 
• 195053-92-0 1-(Triphenylmethyl)-4-(2-amino-1-ethyl)imidazole 

Downstream Products

• 254108-75-3 1-[7-((Methanesulfonyl)oxy)naphthyl]-4-[2-(1-(4-cyano-3-fluorobenzyl)-5-imidazolyl)-ethyl]-2-piperazinone 
• 254108-76-4 methanesulfonic acid 8-(4-{2-[3-(4-bromo-3-fluoro-benzyl)-3H-imidazol-4-yl]-ethyl}-2-oxo-piperazin-1-yl)-naphthalen-2-yl ester 

Relevant academic research and scientific papers

INHIBITORS OF PRENYL-PROTEIN TRANSFERASE

The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras

Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I

Compound 1 has been shown to be a dual prenylation inhibitor with FPTase (IC50=2 nM) and GGPTase-I (IC50=95 nM). Analogues of 1, which replaced the cyanophenyl group with various biaryls, led to the discovery of highly potent dual FPTase/GGPTase-I inhibitors. 4-Trifluoromethylphenyl, trifluoropentynyl, and trifluoropentyl were identified as good p-cyano replacements.