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5-Imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors

The evaluation of structure–activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described. The synthesis and inhibiting potency of farnesyltransferase inhibitors closely related to R115777 is reported.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-05, Vol.13 (9), p.1543-1547
Main Authors: Angibaud, Patrick, Bourdrez, Xavier, Devine, Ann, End, David W, Freyne, Eddy, Ligny, Yannick, Muller, Philippe, Mannens, Geert, Pilatte, Isabelle, Poncelet, Virginie, Skrzat, Stacy, Smets, Gerda, Van Dun, Jacky, Van Remoortere, Pieter, Venet, Marc, Wouters, Walter
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Language:English
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Summary:The evaluation of structure–activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described. The synthesis and inhibiting potency of farnesyltransferase inhibitors closely related to R115777 is reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00180-X