Discovery of tricyclic HIV-1 integrase-LEDGF/p75 allosteric inhibitors by intramolecular direct arylation reaction

[Display omitted] We have been conducting exploratory research to develop human immunodeficiency virus type-1 (HIV-1) integrase-LEDGF/p75 allosteric inhibitors (INLAIs). Here, we report on a newly designed compound with a tricyclic scaffold that shows promise as an inhibitor. Various scaffolds were...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2022-05, Vol.64, p.128664-128664, Article 128664
Hauptverfasser:	Taoda, Yoshiyuki, Akiyama, Toshiyuki, Tomita, Kenji, Fujiwara-Kitamura, Misato, Tamura, Yoshinori, Kawasuji, Takashi, Matsuoka, Eriko, Akihisa, Erika, Seki, Takahiro, Yoshinaga, Tomokazu
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric inhibitor Dihydrophenanthridine Direct arylation HIV Integrase - chemistry HIV Integrase Inhibitors - chemistry HIV Integrase Inhibitors - pharmacology HIV-1 Humans INLAIs Integrase Intercellular Signaling Peptides and Proteins LEDGF/p75
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