1.
Bioorg Med Chem Lett
; 13(2): 261-4, 2003 Jan 20.
Article
in English
| MEDLINE
| ID: mdl-12482435
ABSTRACT
A series of novel cyclopropanyl methyl hexadienoic acid retinoids was designed and prepared. These compounds exhibited either selective activity as RXR agonists or pan-agonists on one or more of each of the RAR and RXR isoforms. The most potent pan-agonist 5a (RAR's EC(50)=17-59 nM; RXR's EC(50)=6-14 nM) showed good antiproliferative properties in the in vitro cancer cell lines, ME 180 and RPMI 8226.
Subject(s)
Cyclopropanes/chemical synthesis , Cyclopropanes/pharmacology , Receptors, Retinoic Acid/drug effects , Sorbic Acid/analogs & derivatives , Binding, Competitive/drug effects , Cell Differentiation/drug effects , Cell Division/drug effects , Humans , Indicators and Reagents , Ligands , Receptors, Retinoic Acid/agonists , Receptors, Retinoic Acid/genetics , Sorbic Acid/chemical synthesis , Sorbic Acid/pharmacology , Transfection , Tumor Cells, Cultured
2.
Angew Chem Int Ed Engl
; 40(24): 4765-4769, 2001 Dec 17.
Article
in English
| MEDLINE
| ID: mdl-12404411
