JLK1486, a <i>N</i>,<i>N</i>‐[(8‐hydroxyquinoline)methyl]‐substituted benzylamine analogue, inhibits melanoma proliferation and induces autophagy

Koekemoer, Trevor; Venter, Maryna van de; Kraus, Jean‐Louis

doi:10.1111/cpr.12127

Cited by 5 publications

(1 citation statement)

References 15 publications

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“…CQ and its derivative hydroxychloroquine (HCQ) are known inhibitors of autophagy, used in the clinics to treat GBM tumors, typically in combinatorial therapies together with the alkylating agent temozolomide (TMZ), and contribute, in some cases, to extend survival prognoses in patients affected by these aggressive, autophagy‐prone tumors . The N , N ‐(8‐hydroxyquinoline)methyl‐substituted benzylamine JLK1486 has been reported to inhibit cellular proliferation in B16F10 skin melanoma cells, via induction of cytodestructive autophagy . The styrylquinoline LV‐320 was found to block the autophagic flux, and thus impair cellular viability, in several breast cancer cell lines, in a dose‐dependent manner…”

Section: Introductionmentioning

confidence: 99%

Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action

et al. 2019

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The role of autophagy in cancer is often complex, ranging from tumor-promoting to -suppressing effects. In this study, two novel hybrid molecules were designed, containing a ruthenacarborane fragment conjugated with a known modulator of autophagy, namely a quinoline derivative. The complex closo-[3-(η 6 -p-cymene)-1-(quinolin-8-yl-acetate)-3,1,2-RuC 2 B 9 H 10 ](4) showed a dual mode of action against the LN229 (human glioblastoma) cell line, where it inhibited tumor-promoting autophagy, and strongly inhibited cell proliferation, de facto blocking cellular division. These results, together with the tendency to spontaneously form nanoparticles in aqueous solution, make complex 4 a very promising drug candidate for further studies in vivo, for the treatment of autophagy-prone glioblastomas. [a] Dr. . Results from flow cytometric and fluorescence microscopy analysis, and wound healing assay of MCF-7 cells incubated (72 h) with 3 and 4 at 20 μM. (A) CFSE staining (left panel) and wound healing assay (right panel); (B) AnnV/PI double staining; (C) DAPI-stained cells observed under fluorescence microscope (magnification X200). Arrows indicate apoptotic cells; (D) ApoStat staining; (E) AO staining. Experiments were run in triplicate. One representative example per each experiment is shown. For each staining protocol, the respective control (untreated cells) is also shown. (FL1, green channel; FL2, orange channel; FL3, dark red channel).

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Section: Introductionmentioning

confidence: 99%

Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action

et al. 2019

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Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer

Sharma,

Sudha Ambadipudi,

Kumar Chouhan

et al. 2024

Bioorganic & Medicinal Chemistry Letters

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New ternary Fe(III)-8-hydroxyquinoline–reduced Schiff base complexes as selective anticancer drug candidates

Ferretti

Matos

Canelas

et al. 2022

Journal of Inorganic Biochemistry

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JLK1486, a N,N‐[(8‐hydroxyquinoline)methyl]‐substituted benzylamine analogue, inhibits melanoma proliferation and induces autophagy

Abstract: JLK1486 provides a promising chemical scaffold to develop new anti-melanoma drugs or combination therapies, due to its potent inhibition of cell proliferation and induction of autophagy, at pharmacologically relevant concentrations.

Cited by 5 publications

References 15 publications

Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action

Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action

Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer

New ternary Fe(III)-8-hydroxyquinoline–reduced Schiff base complexes as selective anticancer drug candidates

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