1.
Bioorg Med Chem
; 18(19): 7132-43, 2010 Oct 01.
Article
in English
| MEDLINE
| ID: mdl-20800501
ABSTRACT
The synthesis of non-peptidic helix mimetics based on a trimeric quinoline scaffold is described. The ability of these new compounds, as well as their synthetic dimeric intermediates, to bind to various members of the Bcl-2 protein anti-apoptotic group is also evaluated. The most interesting derivative of this new series (compound A) inhibited Bcl-x(L)/Bak, Bcl-x(L)/Bax and Bcl-x(L)/Bid interactions with IC(50) values around 25 µM.
Subject(s)
Proto-Oncogene Proteins c-bcl-2/antagonists & inhibitors , Quinolines/chemical synthesis , Quinolines/pharmacology , bcl-X Protein/antagonists & inhibitors , Apoptosis , Binding Sites , Dimerization , Dose-Response Relationship, Drug , Drug Discovery , Models, Molecular , Molecular Structure , Proto-Oncogene Proteins c-bcl-2/chemistry , Quinolines/chemistry , Recombinant Proteins/antagonists & inhibitors , Recombinant Proteins/chemistry , Stereoisomerism , Structure-Activity Relationship , bcl-X Protein/chemistry
2.
Eur J Med Chem
; 45(4): 1657-62, 2010 Apr.
Article
in English
| MEDLINE
| ID: mdl-20106562
ABSTRACT
The synthesis of new di- and trimeric quinoline derivatives is described as well as their in vitro antiproliferative activities toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1).
