Dong-Ho Lee

Korea Research Institute of Chemical Technology

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Jong Yeon Hwang

Korea Research Institute of Chemical Technology

Chi Hoon Park

Korea University of Science and Technology

Pilho Kim

Korea Research Institute of Chemical Technology

Inn‐Kyu Kang

Kyungpook National University

Chung Hyo Kang

Korea Research Institute of Chemical Technology

Lee Soon Park

Jin-Wan Jeong

Jinwoo Jeong

Chung-Ang University

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Kwan Ho Seo

Kyungpook National University

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Seoul National University

Korea Research Institute of Chemical Technology

Korea University of Science and Technology

Yonsei University

Korea Research Institute of Bioscience and Biotechnology

Korea Advanced Institute of Science and Technology

Korea University

Chungnam National University

Daejeon University

Sungkyunkwan University

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Synthesis and Molecular Modeling Studies of N′-Hydroxyindazolecarboximidamides as Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Molecules (2017)

Dong-Ho Lee Joo‐Youn Lee Ji‐Eun Jeong Mi‐Ok Kim Kyungwon Lee

Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunosuppressive enzyme that is highly overexpressed in various cancer cells and antigen-presenting cells. It has emerged as an attractive therapeutic target for cancer immunotherapy, which has prompted high interest in the development of small-molecule inhibitors. To discover novel IDO1 inhibitors, we designed and synthesized a series of N'-hydroxyindazolecarboximidamides. Among the compounds synthesized, compound 8a inhibited both tryptophan depletion and kynurenine production through the IDO1 enzyme. Molecular docking studies revealed that 8a binds to IDO1 with the same binding mode as the analog, epacadostat (INCB24360). Here, we report the synthesis and biological evaluation of these hydroxyindazolecarboximidamides and present the molecular docking study of 8a with IDO1.

Indoleamine 2,3-dioxygenase

Dioxygenase

10.3390/molecules22111936

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Citations (8)

Mo1123 Association of Post-Treated Creatinine Level With Negative Conversion Rate of Clostridium difficile Toxin Assay

Gastroenterology (2012)

Dong Hyeon Lee Dong-Ho Lee Nayoung Kim Cheol Min Shin Jin‐Hyeok Hwang

10.1016/s0016-5085(12)62303-8

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Open-world knowledge graph completion for unseen entities and relations via attentive feature aggregation