In recent years a 3D-pharmacophore model has allowed us to rationally design potent INSTIs. On this basis we synthesized a series of new benzylindole derivatives through efficient solution-phase parallel and microwave-assisted syntheses. Biological evaluation of compounds obtained pointed to a potent IN strand-transfer inhibitory activity.
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Akiyama, Toshiyuki
Johns, Brian A.
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GlaxoSmithKline Res & Dev Ltd, Infect Dis Therapeut Area Unit, Five Moore Dr, Res Triangle Pk, NC 27709 USAShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Johns, Brian A.
Taoda, Yoshiyuki
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Taoda, Yoshiyuki
Yoshida, Hiroshi
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Yoshida, Hiroshi
Taishi, Teruhiko
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Taishi, Teruhiko
Kawasuji, Takashi
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Kawasuji, Takashi
Murai, Hitoshi
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Murai, Hitoshi
Yoshinaga, Tomokazu
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Yoshinaga, Tomokazu
Sato, Akihiko
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Sato, Akihiko
Seki, Takahiro
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Seki, Takahiro
Koyama, Mikiko
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Koyama, Mikiko
Miki, Shigeru
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Miki, Shigeru
Kawauchi-Miki, Shinobu
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Kawauchi-Miki, Shinobu
Kagitani-Suyama, Akemi
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
Kagitani-Suyama, Akemi
Fujiwara, Tamio
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Shionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, JapanShionogi & Co Ltd, Shionogi Pharmaceut Res Ctr, 3-1-1 Futaba cho, Toyonaka, Osaka 5610825, Japan
机构:
UPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Hop La Pitie Salpetriere, AP HP, Dept Virol, Paris, FranceUPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Malet, Isabelle
Subra, Frederic
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Univ Paris Saclay, CNRS, ENS Cachan, LBPA,UMR 8113,IDA,FR3242, Cachan, FranceUPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Subra, Frederic
Charpentier, Charlotte
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INSERM, IAME, UMR1137, Paris, France
Univ Paris Diderot, Sorbonne Paris Cite, IAME, UMR1137, Paris, France
Hop Bichat Claude Bernard, AP HP, Lab Virol, Paris, FranceUPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Charpentier, Charlotte
Collin, Gilles
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INSERM, IAME, UMR1137, Paris, France
Univ Paris Diderot, Sorbonne Paris Cite, IAME, UMR1137, Paris, France
Hop Bichat Claude Bernard, AP HP, Lab Virol, Paris, FranceUPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Collin, Gilles
Descamps, Diane
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INSERM, IAME, UMR1137, Paris, France
Univ Paris Diderot, Sorbonne Paris Cite, IAME, UMR1137, Paris, France
Hop Bichat Claude Bernard, AP HP, Lab Virol, Paris, FranceUPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Descamps, Diane
Calvez, Vincent
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UPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Hop La Pitie Salpetriere, AP HP, Dept Virol, Paris, FranceUPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Calvez, Vincent
Marcelin, Anne-Genevieve
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UPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Hop La Pitie Salpetriere, AP HP, Dept Virol, Paris, FranceUPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France
Marcelin, Anne-Genevieve
Delelis, Olivier
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Univ Paris Saclay, CNRS, ENS Cachan, LBPA,UMR 8113,IDA,FR3242, Cachan, FranceUPMC Univ Paris 06, Sorbonne Univ, INSERM, IPLESP UMRS 1136, Paris, France