2021
DOI: 10.3390/ijms22115636
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Anticancer Activity of Two Novel Hydroxylated Biphenyl Compounds toward Malignant Melanoma Cells

Abstract: Melanoma, the deadliest form of skin cancer, is still one of the most difficult cancers to treat despite recent advances in targeted and immune therapies. About 50% of advanced melanoma do not benefit of such therapies, and novel treatments are requested. Curcumin and its analogs have shown good anticancer properties and are being considered for use in combination with or sequence to recent therapies to improve patient outcomes. Our group previously published the synthesis and anticancer activity characterizat… Show more

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Cited by 13 publications
(6 citation statements)
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References 41 publications
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“…Therefore, we analyzed some molecular markers of programmed cell death. The cleaved form of poly (ADP-ribose) polymerase 1 (cleaved-PARP1) is obtained through the activity of caspase 3 or caspase 7 in cells undergoing apoptosis [ 47 , 48 ]. After 24 h of HPF treatment, in all melanoma cell lines, immunoblots showed a decrease of bands representing full-length PARP1 expression and a correspondent increase of higher mobility band displaying cleaved-PARP1 level ( Figure 4 ).…”
Section: Resultsmentioning
confidence: 99%
“…Therefore, we analyzed some molecular markers of programmed cell death. The cleaved form of poly (ADP-ribose) polymerase 1 (cleaved-PARP1) is obtained through the activity of caspase 3 or caspase 7 in cells undergoing apoptosis [ 47 , 48 ]. After 24 h of HPF treatment, in all melanoma cell lines, immunoblots showed a decrease of bands representing full-length PARP1 expression and a correspondent increase of higher mobility band displaying cleaved-PARP1 level ( Figure 4 ).…”
Section: Resultsmentioning
confidence: 99%
“…Other potential targets revealed during the in silico “target fishing” reverse screening, including Poly(ADP-ribose)polymerase (PARP), 82, 83 phosphodiesterase type 5, 84, 85 orphan nuclear receptor LRH-1, 86, 87 nuclear receptor ROR-gamma, 88, 89 matrix metallopeptidase 9 (MMP9), 90 NAD-dependent deacetylase Sirtuin 2, 91 and cholesterol ester transfer protein, 92 all believed to play important roles in skin carcinogenesis. There is no doubt that the wealth of information gathered here will be useful in further studies towards the optimizing the hit molecules’ activity and determining their putative drug target and potential mechanism(s) of action.…”
Section: Resultsmentioning
confidence: 99%
“…78 It should also be mentioned that PI3K/RAC alpha serine/threonine protein kinase (AKT)/mTOR signaling pathway has been shown to be over-activated in some types of skin cancers, 80 with the anti-proliferative activity of some phenolic compounds against SK-MEL-2 cancer cells attributed to the downregulation of the PI3K/AKT/mTOR signaling pathway, which induces a mitochondrial-dependent apoptosis. 81 Other potential targets revealed during the in silico "target fishing" reverse screening, including Poly(ADPribose)polymerase (PARP), 82,83 phosphodiesterase type 5, 84,85 orphan nuclear receptor LRH-1, 86,87 nuclear receptor ROR-gamma, 88,89 matrix metallopeptidase 9 (MMP9), 90 NAD-dependent deacetylase Sirtuin 2, 91 and cholesterol ester transfer protein, 92 all believed to play important roles in skin carcinogenesis. There is no doubt that the wealth of information gathered here will be useful in further studies towards the optimizing the hit molecules' activity and determining their putative drug target and potential mechanism(s) of action.…”
Section: In Silico Target(s) Prediction Pharmacokinetic and Admet Stu...mentioning
confidence: 99%
“…It serves as a central building block for basic liquid crystal and fluorescent layers in OLEDs [3,4]. The ability of biphenyls to undergo chemical changes to form substituted biphenyls has many biological and pharmaceutical applications, including anti-inflammatory, antimicrobial, antifungal, antidiabetic, anti-tumor, and anticancer properties [5][6][7][8][9]. The search for new and efficient pharmaceuticals is a constant struggle for medicinal chemists, in view of the fact that the new compounds synthesized by various standard methods should be safe, effective, and have fewer side effects.…”
Section: Introductionmentioning
confidence: 99%