[ Pharmaceutical Sciences Asia - ONLINE ]
E-ISSN 2586-8470
[ Journal Abbreviation: Pharm.Sci.Asia ]
Mahidol University Journal of Pharmaceutical Sciences
  FORMER NAME   "Mahidol University Journal of Pharmaceutical Sciences" Published Since 1974


DOI: 10.29090/psa.2023.02.22.309Pharm Sci Asia 2023; 50(2), 147-156

Design, synthesis, and evaluation of indoleamin-2,3-dioxygenase 1 inhibition activity of novel 5/6-amino indazole derivatives with amide template

Ngo Xuan Hoang1, Tam Thuy Lu Vo2, Van-Hai Hoang3,4, Tiep K. Nguyen1, Ji Hae Seo2*, Phuong-Thao Tran1*

1 Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, Vietnam
2 Department of Biochemistry, Keimyung University School of Medicine, Daegu, Korea
3 Faculty of Pharmacy, PHENIKAA University, Hanoi, Vietnam
4 PHENIKAA Institute for Advanced Study (PIAS), PHENIKAA University, Yen Nghia, Hadong, Hanoi, Vietnam

Indoleamine 2,3-dioxygenase 1 (IDO1) is an enzyme participating in tryptophan metabolism that has been implicated in numerous cancers. In the present study, a series of novel 5/6-amino indazole derivatives having amide linker were designed, synthesized, and evaluated for IDO1 inhibitory activity. The compounds were initially designed based on the known structural feature of IDO1 active site, and the important role of the indazole scaffold in interaction with IDO1 active site. Thirteen compounds exibited the moderate to excellent inhibitory activity (49% to 100% at the concentration of 1.0 mM). One of them, compound, 2-(6-amino-1H-indazol-1-yl)-N-(4-chlorophenyl) acetamide (19d), with chloro substituents group at para- position increased the activity upto 100%, equal to that value of the positive control, IDO5L. This research suggests that 5/6-amino indazole moiety combined with amide template is a potential scaffold for IDO1 inhibition as anti-cancer agents.


Aminoindazole, Amide, Indoleamine 2,3-dioxygenase 1, IDO1

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