کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1393062 1501175 2011 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors
چکیده انگلیسی

Indoleamine 2,3-dioxygenase (IDO) is an important new therapeutic target for the treatment of cancer. With the aim of discovering novel IDO inhibitors, a virtual screen was undertaken and led to the discovery of the keto-indole derivative 1a endowed with an inhibitory potency in the micromolar range. Detailed kinetics were performed and revealed an uncompetitive inhibition profile. Preliminary SARs were drawn in this series and corroborated the putative binding orientation as suggested by docking.

Figure optionsDownload as PowerPoint slideHighlights
► Indoleamine 2,3-dioxygenase (IDO) involved in anticancer immunosuppression.
► Keto-indoles are novel IDO inhibitors.
► Substitution in the 5-position allows to enhance IDO inhibition.
► Keto-indoles act as uncompetitive inhibitors.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 46, Issue 7, July 2011, Pages 3058–3065
نویسندگان
, , , , , , , , , , , , , , ,