Design, synthesis and bioevaluation of novel 6-substituted aminoindazole derivatives as anticancer agents

Hoang, Ngo Xuan; Hoang, Van-Hai; Luu, Thi-Thu-Trang; Luu, Hung N.; Ngo, Thien; Hieu, Duong Van; Long, Nguyen Huu; Anh, Le Viet; Ngo, Son Tung; Yen, Nguyen Thi Hai; Han, Byung Woo; Nguyen, Thanh X.; Hai, Dinh Thi Thanh; Hien, Tran Thi Thu; Tran, Phuong‐Thao

doi:10.1039/d0ra09112j

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2024

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Cited by 6 publications

(2 citation statements)

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“…41,42 Moreover, molecular docking simulations have also been utilized to interpret the experimental data, especially when the experimental structures were not available. 43…”

Section: Computational Methods and Applicationsmentioning

confidence: 99%

Characterizing the ligand-binding affinity toward SARS-CoV-2 Mproviaphysics- and knowledge-based approaches

Ngo

Nguyen

Tung

et al. 2022

Phys. Chem. Chem. Phys.

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“…41,42 Moreover, molecular docking simulations have also been utilized to interpret the experimental data, especially when the experimental structures were not available. 43…”

Section: Computational Methods and Applicationsmentioning

confidence: 99%

Characterizing the ligand-binding affinity toward SARS-CoV-2 Mproviaphysics- and knowledge-based approaches

Ngo

Nguyen

Tung

et al. 2022

Phys. Chem. Chem. Phys.

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“…Our previous study indicated that the indazole scaffold plays an important role in interaction with IDO1 active site residues at pocket A, and the 6-NH group in the 6-aminoindazole template also forms hydrogen bond (HB) with the 7-propionate of the heme ion (Figure 2B) 14 .…”

Section: Introductionmentioning

confidence: 99%

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

Hoang¹,

Vo²,

Hoang³

et al. 2023

Pharm Sci Asia

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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.

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IDO1 inhibitors are synergistic with CXCL10 agonists in inhibiting colon cancer growth

Yang,

Cao,

Zhang

et al. 2024

Biomedicine & Pharmacotherapy

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Design, synthesis and bioevaluation of novel 6-substituted aminoindazole derivatives as anticancer agents

Abstract: In the present study, a series of 6-substituted aminoindazole derivatives were designed, synthesized, and evaluated for bio-activities.

Cited by 6 publications

References 41 publications

Characterizing the ligand-binding affinity toward SARS-CoV-2 Mproviaphysics- and knowledge-based approaches

Characterizing the ligand-binding affinity toward SARS-CoV-2 Mproviaphysics- and knowledge-based approaches

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

IDO1 inhibitors are synergistic with CXCL10 agonists in inhibiting colon cancer growth

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