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Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors |
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| Authors: | Angibaud Patrick Bourdrez Xavier End David W Freyne Eddy Janicot Michel Lezouret Patricia Ligny Yannick Mannens Geert Damsch Siegrid Mevellec Laurence Meyer Christophe Muller Philippe Pilatte Isabelle Poncelet Virginie Roux Bruno Smets Gerda Van Dun Jacky Van Remoortere Pieter Venet Marc Wouters Walter |
| Affiliation: | a Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&JPRD), Campus de Maigremont BP615, 27106, Val de Reuil, France b Oncology Drug Discovery, J&JPRD L.L.C. Welsh and McKean Roads, Spring-House PA 19477-0776, USA c Oncology Drug Discovery, J&JPRD, Turnhoutseweg 30, B-2340, Belgium d Preclinical Pharmacokinetics, J&JPRD, Turnhoutseweg 30, B-2340, Belgium e Drug Evaluation, J&JPRD, Turnhoutseweg 30, B-2340, Belgium |
| Abstract: | A series of (4-chlorophenyl)--(1-methyl-1H-imidazol-5-yl)azoloquinolines and -quinazolines was prepared. 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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