Author/Authors :
Sushil K. Sharma، نويسنده , , Timothy M. Ramsey، نويسنده , , Ying-Nan P. Chen، نويسنده , , Weichun Chen، نويسنده , , Mary S. Martin، نويسنده , , Kenneth Clune، نويسنده , , Michael Sabio، نويسنده , , Kenneth W. Bair، نويسنده ,
Abstract :
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.
