INHIBITOR OF INDOLEAMINE 2,3-DIOXYGENASE-1 AND METHODS OF MANUFACTURE AND USE THEREOF
Inhibition of indoleamine 2,3-dioxygenase (IDOl) is an attractive immunotherapeutic approach for the treatment of a variety of cancers. Dysregulation of this enzyme has also been implicated in other severe diseases such as Alzheimer's disease and arthriti
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Paragraph 00104; 00139; 00147-00149
(2019/08/06)
Identification of Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors Based on a Phenylimidazole Scaffold
Inhibition of indoleamine 2,3-dioxygenase (IDO1) is an attractive immunotherapeutic approach for the treatment of a variety of cancers. Dysregulation of this enzyme has also been implicated in other disorders including Alzheimer's disease and arthritis. Herein, we report the structure-based design of two related series of molecules: N1-substituted 5-indoleimidazoles and N1-substituted 5-phenylimidazoles. The latter (and more potent) series was accessed through an unexpected rearrangement of an imine intermediate during a Van Leusen imidazole synthesis reaction. Evidence for the binding modes for both inhibitor series is supported by computational and structure-activity relationship studies.
Brant, Michael G.,Goodwin-Tindall, Jake,Stover, Kurt R.,Stafford, Paul M.,Wu, Fan,Meek, Autumn R.,Schiavini, Paolo,Wohnig, Stephanie,Weaver, Donald F.
supporting information
p. 131 - 136
(2018/02/19)
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