Design, synthesis and biological evaluation of cyclic angiotensin II analogues with 3,5 side-Chain bridges

2002 ◽  
Vol 12 (18) ◽  
pp. 2627-2633 ◽  
Author(s):  
Panagiota Roumelioti ◽  
Ludmila Polevaya ◽  
Panagiotis Zoumpoulakis ◽  
Nektarios Giatas ◽  
Ilze Mutule ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Biological Evaluation ◽  
Side Chain ◽  
Design Synthesis ◽  
Angiotensin Ii Analogues ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of novel, simplified analogues of laulimalide: modification of the side chain

2005 ◽  
Vol 15 (9) ◽  
pp. 2243-2247 ◽  
Author(s):  
Ian Paterson ◽  
Dirk Menche ◽  
Anders E. Håkansson ◽  
Adrian Longstaff ◽  
David Wong ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Side Chain ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis, and biological evaluation of novel substituted [1,2,3]triazolo[4,5-d]pyrimidines as HIV-1 Tat-TAR interaction inhibitors

2010 ◽  
Vol 82 (1) ◽  
pp. 339-347
Author(s):  
Fei Yu ◽  
Ruifang Pang ◽  
Dekai Yuan ◽  
Meizi He ◽  
Chunlei Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Side Chain ◽  
Design Synthesis ◽  
Cat Assay ◽  
Immunodeficiency Virus ◽  
Antiviral Activities ◽  
Tar Rna ◽  
Rna Interaction ◽  
Synthesis And Biological Evaluation ◽  
Hiv 1

A novel series of compounds, derived from [1,2,3]triazolo[4,5-d]pyrimidines with a guanidyl group or amino group-terminated side chain was designed and synthesized as HIV-1 trans-activator of transcription–trans-activation responsive region (Tat–TAR) interaction inhibitors. Their ability to inhibit Tat–TAR RNA interaction was determined by a Tat-dependent HIV-1 long terminal repeat (LTR)-driven chloramphenicol acetyltransferase (CAT) assay and simian immunodeficiency virus (SIV)-induced syncytium evaluation. The binding of the compounds with TAR RNA was conducted by molecular modeling and capillary electrophoresis (CE) analysis. The results showed that all the compounds could block the Tat–TAR interaction and have antiviral activities.

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