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Synthesis and biological evaluation of triazolothienopyrimidine derivatives as novel HIV-1 replication inhibitors.

Abstract：

:We identified a novel class of triazolothienopyrimidine (TTPM) compounds as potent HIV-1 replication inhibitors during a high-throughput screening campaign that evaluated more than 200,000 compounds using a cell-based full replication assay. Herein, we report the optimization of the antiviral activity in a cell-based assay system leading to the discovery of aryl-substituted TTPM derivatives (38, 44, and 45), which exhibited significant inhibition of HIV-1 replication with acceptable safety margins. These novel and potent TTPMs could serve as leads for further development.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kim J,Kwon J,Lee D,Jo S,Park DS,Choi J,Park E,Hwang JY,Ko Y,Choi I,Ju MK,Ahn J,Kim J,Han SJ,Kim TH,Cechetto J,Nam J,Ahn S,Sommer P,Liuzzi M,No Z,Lee J

doi

10.1016/j.bmcl.2012.10.134

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

153-7

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01436-9

journal_volume

23

pub_type

杂志文章

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