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Synthesis and biological evaluation of triazolothienopyrimidine derivatives as novel HIV-1 replication inhibitors. 2013
Junwon Kim, and
Jeongjin Kwon, and
Doohyun Lee, and
Suyeon Jo, and
Dong-Sik Park, and
Jihyun Choi, and
Eunjung Park, and
Jong Yeon Hwang, and
Yoonae Ko, and
Inhee Choi, and
Moon Kyeong Ju, and
JiYe Ahn, and
Junghwan Kim, and
Sung-Jun Han, and
Tae-Hee Kim, and
Jonathan Cechetto, and
Jiyoun Nam, and
Sujin Ahn, and
Peter Sommer, and
Michel Liuzzi, and
Zaesung No, and
Jinhwa Lee
Medicinal Chemistry 2, Institut Pasteur Korea, Sampyeong-dong 696, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea.
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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