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. 2001 Sep 17;11(18):2449-52.
doi: 10.1016/s0960-894x(01)00486-3.

Identification of E2F-1/Cyclin A antagonists

S K Sharma  1 , T M Ramsey, Y N Chen, W Chen, M S Martin, K Clune, M Sabio, K W Bair
Affiliations

Identification of E2F-1/Cyclin A antagonists

S K Sharma et al. Bioorg Med Chem Lett. .

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.

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