Inhibitory activity on HIV-1 reverse transcriptase and integrase of a carmalol derivative from a brown Alga,Ishige okamurae

2006 ◽  
Vol 20 (8) ◽  
pp. 711-713 ◽  
Author(s):  
M.-J. Ahn ◽  
K.-D. Yoon ◽  
C. Y. Kim ◽  
J. H. Kim ◽  
C.-G. Shin ◽  
...  
2013 ◽  
Vol 170 (1) ◽  
pp. 219-230 ◽  
Author(s):  
Mengjuan Zhu ◽  
Lijing Xu ◽  
Xiao Chen ◽  
Zengqiang Ma ◽  
Hexiang Wang ◽  
...  

2008 ◽  
Vol 26 (2) ◽  
pp. 379-387 ◽  
Author(s):  
Jiraporn UNGWITAYATORN ◽  
Chanpen WIWAT ◽  
Chutima MATAYATSUK ◽  
Jutarat PIMTHON ◽  
Suratsawadee PIYAVIRIYAKUL

2014 ◽  
Vol 14 (S3) ◽  
Author(s):  
Rajendra Prasad Gujjeti ◽  
Sainath Namthabad ◽  
Estari Mamidala

1994 ◽  
Vol 57 (7) ◽  
pp. 896-904 ◽  
Author(s):  
Agnes M. Rimando ◽  
John M. Pezzuto ◽  
Norman R. Farnsworth ◽  
Thawatchai Santisuk ◽  
Vichai Reutrakul ◽  
...  

1995 ◽  
Vol 6 (2) ◽  
pp. 98-108 ◽  
Author(s):  
T. Antonucci ◽  
J. S. Warmus ◽  
J. C. Hodges ◽  
D. G. Nickell

As a result of mass screening of the Parke-Davis Pharmaceutical compound library for inhibitors of HIV-1 reverse transcriptase (RT) activity, a novel class of inhibitor, the pyrroles, was identified. Subsequently, a series of analogues was screened for inhibitory activity against HIV-1 and some structure-activity relationships were identified. Further characterization of the most potent pyrrole involved comparing its effects in peripheral blood lymphocytes (PBLs) with its effects in transformed cell lines; the pyrrole had the same efficacy (EC50 = approximately 2 μM) but was less toxic in PBLs (IC50 = 175 μM) than in the cell lines CEM-SS and MT-2 (IC50 = 60-70 μM). The pyrrole was active against a strain of HIV-1 resistant to AZT (strain G9106) but lost activity against both HIV-2 (strain ROD) and a strain of HIV-1 resistant to a non-nucleoside reverse transcriptase inhibitor (the pyridinone-resistant strain A17). Moreover, in direct enzymatic testing against HIV-1 RT purified from virus particles and against RT expressed recombinantly, the pyrrole showed potent inhibitory activity. We conclude that the pyrroles present a novel class of HIV-1 non-nucleoside reverse transcriptase inhibitor.


Sign in / Sign up

Export Citation Format

Share Document