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  • Title: Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.
    Author: Njoroge FG, Vibulbhan B, Shi X, Strickland C, Kirschmeier P, Bishop R, Nomeir A, Girijavallabhan V.
    Journal: Bioorg Med Chem Lett; 2004 Dec 06; 14(23):5899-902. PubMed ID: 15501065.
    Abstract:
    Modification of the ethano bridge of the core structure of the antitumor agent, SARASAR (SCH66336) with concomitant introduction of a sulfonamide moiety off the distal piperidine afforded inhibitor 9-(S-), a compound with greatly improved PK profile. Other compounds with enhanced FPTase inhibitory activity were obtained as exemplified by amide 10-(S-) and urea 11-(S-): these compounds demonstrated activity in picomolar range.
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