3 Papers
55 Citations
Bruno Roux is an academic researcher from Johnson & Johnson Pharmaceutical Research and Development. The author has contributed to research in topics: Farnesyltransferase & In vitro. The author has an hindex of 3, co-authored 3 publications.
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Papers
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
Patrick Rene Angibaud,Xavier Bourdrez,David William End,Eddy Jean Edgard Freyne,Michel Janicot,Patricia Lezouret,Yannick Aimé Eddy Ligny,Geert Mannens,Siegrid Damsch,Laurence Mevellec,Christophe Meyer,Philippe Muller,Isabelle Noëlle Constance Pilatte,Virginie Sophie Poncelet,Bruno Roux,Gerda Smets,Jacky Van Dun,Pieter Van Remoortere,Marc Venet,Wouters Walter Boudewijn Leopo +19 more
TL;DR: These compounds displayed potent Farnesyl Protein Transferase inhibitory activity and tetrazolo[1,5-a]quinazolines are promising agents for oral in vivo inhibition.
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4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.
Patrick Rene Angibaud,Ashis K. Saha,Xavier Bourdrez,David William End,Eddy Jean Edgard Freyne,Patricia Lezouret,Geert Mannens,Laurence Mevellec,Christophe Meyer,Isabelle Noëlle Constance Pilatte,Virginie Sophie Poncelet,Bruno Roux,Gerda Smets,Jacky Van Dun,Marc Venet,Wouters Walter Boudewijn Leopo +15 more
TL;DR: Replacement of the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA series by a 4-methyl-1,2,4-triazol3-yl group gave compounds with similar structure-activity relationship profiles showing that this triazole is potentially a good surrogate to imidazole for farnesytransferase inhibition.
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Impact on farnesyltransferase inhibition of 4-chlorophenyl moiety replacement in the Zarnestra® series
Patrick Rene Angibaud,Laurence Mevellec,Christophe Meyer,Xavier Bourdrez,Patricia Lezouret,Isabelle Noëlle Constance Pilatte,Virginie Sophie Poncelet,Bruno Roux,Sophie Merillon,David W. End,Jacky Van Dun,Walter Wouters,Marc Venet +12 more
TL;DR: Based on the structure of R115777 (tipifarnib, Zarnestra), a series of farnesyltransferase inhibitors have been synthesized by modification of the 2-quinolinone motif and transposition of the 4-chlorophenyl ring to the imidazole or its replacement by 5-membered rings.
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