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Discovery of dimeric inhibitors by extension into the entrance channel of HIV-1 reverse transcriptase

  作者 Ekkati, AR; Bollini, M; Domaoal, RA; Spasov, KA; Anderson, KS; Jorgensen, WL  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-4;  页码  1565-1568  
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[摘要]Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase is being pursued with computational guidance. Extension of azine-containing inhibitors into the entrance channel between Lys103 and Glu138 has led to the discovery of potent and structurally novel derivatives including dimeric inhibitors in an NNRTI-linker-NNRTI motif. (C) 2012 Elsevier Ltd. All rights reserved.

 
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