Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596140 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
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.
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Authors
Junwon Kim, Jeongjin Kwon, Doohyun Lee, Suyeon Jo, Dong-Sik Park, Jihyun Choi, Eunjung Park, Jong Yeon Hwang, Yoonae Ko, Inhee Choi, Moon Kyeong Ju, JiYe Ahn, Junghwan Kim, Sung-Jun Han, Tae-Hee Kim, Jonathan Cechetto, Jiyoun Nam, Sujin Ahn, Jinhwa Lee,