SAR study of niclosamide derivatives in the human glioblastoma U-87 MG cells

Mito, Shizue; Cheng, Benxu; Garcia, Benjamin A.; Gonzalez, Daniela; Ooi, Xin Yee; Ruiz, Tess C.; Elisarraras, Francisco; Tsin, Andrew; Chew, Sue Anne; Arriaga, Marco A.

doi:10.1007/s00044-022-02907-w

Cited by 3 publications

(3 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The inhibition of NF-kB activity could be utilized to overcome the resistance to TMZ, at least in NFKBIA ± GBM genotypes . In a recent study Mito et al designed and synthesized niclosamide derivatives to define structure–activity relations on U87 human GBM cells …”

Section: Introductionmentioning

confidence: 99%

“…84 In a recent study Mito et al designed and synthesized niclosamide derivatives to define structure−activity relations on U87 human GBM cells. 86 Novel salicylanilide derivatives were identified with antiproliferative effects against human cancer cell lines (pulmonary carcinoma cell line A549 and squamous cell carcinoma cell line A431) that overexpress EGFR. 87 A salicylanilide derivative [N-(4-ethoxyphenyl)-2-hydroxybenzoic-acid amide, SUCI02, efuamide] reportedly inhibits phosphorylation and signaling of erbB-2 tyrosine kinase receptor, resulting in cell cycle blockage in breast cancer cells.…”

Section: ■ Introductionmentioning

confidence: 99%

“… 84 In a recent study Mito et al designed and synthesized niclosamide derivatives to define structure–activity relations on U87 human GBM cells. 86 …”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

New Salicylanilide Derivatives and Their Peptide Conjugates as Anticancer Compounds: Synthesis, Characterization, and In Vitro Effect on Glioblastoma

Horváth,

Biri-Kovács,

Baranyai

et al. 2024

ACS Omega

View full text Add to dashboard Cite

Pharmacologically active salicylanilides (2-hydroxy-N-phenylbenzamides) have been a promising area of interest in medicinal chemistry-related research for quite some time. This group of compounds has shown a wide spectrum of biological activities, including but not limited to anticancer effects. In this study, substituted salicylanilides were chosen to evaluate the in vitro activity on U87 human glioblastoma (GBM) cells. The parent salicylanilide, salicylanilide 5-chloropyrazinoates, a 4-aminosalicylic acid derivative, and the new salicylanilide 4-formylbenzoates were chemically and in vitro characterized. To enhance the internalization of the compounds, they were conjugated to delivery peptides with the formation of oxime bonds. Oligotuftsins ([TKPKG] n , n = 1−4), the ligands of neuropilin receptors, were used as GBM-targeting carrier peptides. The in vitro cellular uptake, intracellular localization, and penetration ability on tissue-mimicking models of the fluorescent peptide derivatives were determined. The compounds and their peptide conjugates significantly decreased the viability of U87 glioma cells. Salicylanilide compoundinduced GBM cell death was associated with activation of autophagy, as characterized by immunodetection of autophagy-related processing of light chain 3 protein.

show abstract

Section: Introductionmentioning

confidence: 99%

Section: ■ Introductionmentioning

confidence: 99%

See 1 more Smart Citation

New Salicylanilide Derivatives and Their Peptide Conjugates as Anticancer Compounds: Synthesis, Characterization, and In Vitro Effect on Glioblastoma

Horváth,

Biri-Kovács,

Baranyai

et al. 2024

ACS Omega

View full text Add to dashboard Cite

show abstract

SAR study of niclosamide derivatives for neuroprotective function in SH-SY5Y neuroblastoma

Mito,

Cheng,

Garcia

et al. 2023

Bioorganic & Medicinal Chemistry Letters

View full text Add to dashboard Cite

Optimizing Niclosamide for Cancer Therapy: Improving Bioavailability via Structural Modification and Nanotechnology

Wiggins,

Woo,

Mito

2024

Cancers

View full text Add to dashboard Cite

Inhibition of multiple cancer-related pathways has made niclosamide a promising candidate for the treatment of various cancers. However, its clinical application has been significantly limited by poor bioavailability. This review will discuss current findings on improving niclosamide bioavailability through modification of its chemical structure and utilization of novel nanotechnologies, like electrospraying and supercritical fluids, to improve drug delivery. For example, niclosamide derivatives, such as o-alkylamino-tethered niclosamide derivates, niclosamide ethanolamine salt, and niclosamide piperazine salt, have demonstrated increased water solubility without compromising anticancer activity in vitro. Additionally, this review briefly discusses recent findings on the first pass metabolism of niclosamide in vivo, the role of cytochrome P450-mediated hydroxylation, UDP-glucuronosyltransferase mediated glucuronidation, and how enzymatic inhibition could enhance niclosamide bioavailability. Ultimately, there is a need for researchers to synthesize, evaluate, and improve upon niclosamide derivatives while experimenting with the employment of nanotechnologies, such as targeted delivery and nanoparticle modification, as a way to improve drug administration. Researchers should strive to improve drug-target accuracy, its therapeutic index, and increase the drug’s efficacy as an anti-neoplastic agent.

show abstract

SAR study of niclosamide derivatives in the human glioblastoma U-87 MG cells

Cited by 3 publications

References 34 publications

New Salicylanilide Derivatives and Their Peptide Conjugates as Anticancer Compounds: Synthesis, Characterization, and In Vitro Effect on Glioblastoma

New Salicylanilide Derivatives and Their Peptide Conjugates as Anticancer Compounds: Synthesis, Characterization, and In Vitro Effect on Glioblastoma

SAR study of niclosamide derivatives for neuroprotective function in SH-SY5Y neuroblastoma

Optimizing Niclosamide for Cancer Therapy: Improving Bioavailability via Structural Modification and Nanotechnology

Contact Info

Product

Resources

About