Correlation of indoleamine-2,3-dioxigenase 1 inhibitory activity of 4,6-disubstituted indazole derivatives and their heme binding affinity

[Display omitted] •4,6-Disubstituted indazoles we synthesized had stronger binding to ferrous heme than to ferric heme of IDO1.•We are the first to report a strong correlation between the heme-binding affinity and IDO1 inhibitory activity.•Good fit of the 6-substitutent of the indazole in Pocket-A o...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2019-10, Vol.29 (19), p.126607-126607, Article 126607
Hauptverfasser:	Tsujino, Hirofumi, Uno, Tadayuki, Yamashita, Taku, Katsuda, Masafumi, Takada, Kazuki, Saiki, Takeshi, Maeda, Shotaro, Takagi, Akira, Masuda, Shigeaki, Kawano, Yasuhiko, Meguro, Kanji, Akai, Shuji
Format:	Artikel
Sprache:	eng
Schlagworte:	Heme protein Indazole derivatives Indoleamine 2,3-dioxygenase 1 inhibitor Structure-based drug design
Online-Zugang:	Volltext
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