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Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO-1) Inhibitors Based on Ortho-Naphthaquinone-Containing Natural Product.


ABSTRACT: There is great interest in developing small molecules agents capable of reversing tumor immune escape to restore the body's immune system. As an immunosuppressive enzyme, indoleamine 2,3-dioxygenase 1 (IDO-1) is considered a promising target for oncology immunotherapy. Currently, none of IDO-1 inhibitors have been launched for clinical practice yet. Thus, the discovery of new IDO-1 inhibitors is still in great demand. Herein, a series of diverse ortho-naphthaquinone containing natural product derivatives were synthesized as novel IDO-1 inhibitors. Among them, 1-ene-3-ketone-17-hydroxyl derivative 12 exhibited significantly improved enzymatic and cellular inhibitory activity against IDO-1 when compared to initial lead compounds. Besides, the molecular docking study disclosed that the two most potent compounds 11 and 12 have more interactions within the binding pocket of IDO-1 via hydrogen-bonding, which may account for their higher IDO-1 inhibitory activity.

SUBMITTER: Zhao H 

PROVIDER: S-EPMC6471201 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature

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Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO-1) Inhibitors Based on <i>Ortho</i>-Naphthaquinone-Containing Natural Product.

Zhao Hongchuan H   Sun Pu P   Guo Wei W   Wang Yi Y   Zhang Ao A   Meng Linghua L   Ding Chunyong C  

Molecules (Basel, Switzerland) 20190318 6


There is great interest in developing small molecules agents capable of reversing tumor immune escape to restore the body's immune system. As an immunosuppressive enzyme, indoleamine 2,3-dioxygenase 1 (IDO-1) is considered a promising target for oncology immunotherapy. Currently, none of IDO-1 inhibitors have been launched for clinical practice yet. Thus, the discovery of new IDO-1 inhibitors is still in great demand. Herein, a series of diverse <i>ortho</i>-naphthaquinone containing natural pro  ...[more]

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