1.
Bioorg Med Chem Lett
; 11(18): 2449-52, 2001 Sep 17.
Artículo
en Inglés
| MEDLINE
| ID: mdl-11549444
RESUMEN
A simple method for the synthesis of a rationally designed (S,S)-[Pro-Leu]-spirolactam scaffold is described. This was expanded to a small biased library of compounds mimicking the 'ZRXL' motif in order to identify E2F-1/Cyclin A antagonists. The synthesized compounds were evaluated in an E2F-1/Cyclin A binding assay and moderately active analogues were identified. In addition, the critical roles of Phe, Leu, Lys, and Arg residues of the identified motif were determined.