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Synthesis, Docking and Biological Evaluation of a Novel Class of Imidazothiazoles as IDO1 Inhibitors

Department of Pharmaceutical Sciences, Università del Piemonte Orientale, Largo Donegani 2, 28100 Novara, Italy
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Pawel Kafarski
Molecules 2019, 24(10), 1874; https://doi.org/10.3390/molecules24101874
Received: 6 May 2019 / Revised: 13 May 2019 / Accepted: 15 May 2019 / Published: 15 May 2019
(This article belongs to the Special Issue Design and Synthesis of Bioactive Compounds)
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Abstract

IDO1, a key dioxygenase in tryptophan-kynurenine metabolism, appeared in the last 10 years at the vanguard of druggable targets in cancer therapy due to its well-established role both in immune escape and inflammatory neovascularization. Among the pool of IDO1 inhibitors that have entered clinical trials, none have reached approval. The identification of novel inhibitors endowed with better clinical profile, together with the further comprehension of the interactions with residues in IDO1 active site, are still a need. In this context, we have synthesized a novel class of imidazothiazole derivatives as IDO1 inhibitors and identified three compounds with inhibitory potency in the low micromolar range. This report strengthens the role played by pocket C in the active site of IDO1, providing novel directions in the design of IDO1 inhibitors. View Full-Text
Keywords: indoleamine 2,3-dioxygenase 1; click chemistry; imidazothiazoles; docking indoleamine 2,3-dioxygenase 1; click chemistry; imidazothiazoles; docking
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Serafini, M.; Torre, E.; Aprile, S.; Massarotti, A.; Fallarini, S.; Pirali, T. Synthesis, Docking and Biological Evaluation of a Novel Class of Imidazothiazoles as IDO1 Inhibitors. Molecules 2019, 24, 1874.

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