Pharmacological Properties of Pt(II) and Pt(IV) Complexes with 2,2′-Dipyridylamine; the Comparative In Vitro Thereof

Aghmasheh, Simin; Ostad, SN; Abedi, Anita

doi:10.1007/s12013-020-00937-y

“…The antiproliferative activity of the compounds was tested by the MTT assay on a panel of human cancer cell lines, including non‐small cell lung cancer A549, CDDP‐resistant A549/CDDP, CDDP‐resistant ovarian cancer A2780/CDDP, breast cancer MDA‐MB‐231, pancreatic cancer PANC‐1 cell lines, and the normal human liver L‐02 cell line. DMSO (<1 %) harmless to cells was used as a vehicle [27] . The half maximal inhibitory concentrations (IC 50 ) of the compounds towards these cell lines at 48 h are listed in Table 1.…”

Section: Resultsmentioning

confidence: 99%

“…DMSO (< 1 %) harmless to cells was used as a vehicle. [27] The half maximal inhibitory concentrations (IC 50 ) of the compounds towards these cell lines at 48 h are listed in Table 1. FP and DFP exhibited higher activity than CDDP against all the tested cell lines.…”

Section: Antiproliferative Activitymentioning

confidence: 99%

Overcoming Cancer Resistance to Platinum Drugs by Inhibiting Cholesterol Metabolism

Wang,

Cai,

Li

et al. 2023

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Drug resistance is a serious challenge for platinum anticancer drugs. Platinum complexes may get over the drug resistance via a distinct mechanism of action. Cholesterol is a key factor contributing to the drug resistance. Inhibiting cellular cholesterol synthesis and uptake provides an alternative strategy for cancer treatment. Platinum(IV) complexes FP and DFP with fenofibric acid as axial ligand(s) were designed to combat the drug resistance through regulating cholesterol metabolism besides damaging DNA. In addition to producing reactive oxygen species and active platinum(II) species to damage DNA, FP and DFP inhibited cellular cholesterol accumulation, promoted cholesterol efflux, upregulated peroxisome proliferator‐activated receptor alpha (PPARα), induced caspase‐1 activation and gasdermin D (GSDMD) cleavage, thus leading to both apoptosis and pyroptosis in cancer cells. The reduction of cholesterol significantly relieved the drug resistance of cancer cells. The double‐acting mechanism gave the complexes strong anticancer activity in vitro and vivo, particularly against cisplatin‐resistant cancer cells.

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“…It has the ability to bind to different metal centers through variable coordination modes, which includes monodentate, bidentate, , and also as a bridging ligand . According to Brogden and Berry, dpa adopts nine possible coordination modes which makes it adaptive to different environments and has several uses in catalysis, , pharmaceutical, , photochemistry, and cancer chemotherapy. , This N -heterocyclic compound has two pyridine rings bonded to an sp 3 -hybridized amine group, as shown in Figure a.…”

Section: Introductionmentioning

confidence: 99%

Geometric Analysis and DFT Study of 2,2′-Dipyridylamine-Stabilized First-Row Transition-Metal Complexes

Tetteh

2023

Crystal Growth & Design

0

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A geometric analysis of first-row transition-metal complexes bearing 2,2′-dipyridylamine (dpa) and halogen ligands has been performed using crystallographic data retrieved from the Cambridge Structural Database. The mononuclear complexes were found to exist in octahedral, square-planar, and tetrahedral geometries. Analysis of the bite angles shows clear deviations from the expected 109.5°for tetrahedral complexes which have observable consequences on the geometry and reactivity of these complexes. A density functional theoretical (DFT) study at the B3LYP/6-31+G(d,p) level on a series of tetrahedrally coordinated cobalt(II), nickel(II), copper(II), and zinc(II) complexes bearing dpa and halogen ligands shows that the computed gas phase geometric parameters are remarkably close to those of the experimental values. DFT calculated global chemical reactivity descriptors (chemical hardness, chemical potential, electrophilicity, electron affinity, and ionization energy) show that the energy and reactivity of the tetrahedrally coordinated complexes can be fine-tuned with an appropriate halogen ligand for various applications.

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Overcoming Cancer Resistance to Platinum Drugs by Inhibiting Cholesterol Metabolism

Wang,

Cai,

Li

et al. 2023

Angewandte Chemie

0

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Drug resistance is a serious challenge for platinum anticancer drugs. Platinum complexes may get over the drug resistance via a distinct mechanism of action. Cholesterol is a key factor contributing to the drug resistance. Inhibiting cellular cholesterol synthesis and uptake provides an alternative strategy for cancer treatment. Platinum(IV) complexes FP and DFP with fenofibric acid as axial ligand(s) were designed to combat the drug resistance through regulating cholesterol metabolism besides damaging DNA. In addition to producing reactive oxygen species and active platinum(II) species to damage DNA, FP and DFP inhibited cellular cholesterol accumulation, promoted cholesterol efflux, upregulated peroxisome proliferator‐activated receptor alpha (PPARα), induced caspase‐1 activation and gasdermin D (GSDMD) cleavage, thus leading to both apoptosis and pyroptosis in cancer cells. The reduction of cholesterol significantly relieved the drug resistance of cancer cells. The double‐acting mechanism gave the complexes strong anticancer activity in vitro and vivo, particularly against cisplatin‐resistant cancer cells.

show abstract

Pharmacological Properties of Pt(II) and Pt(IV) Complexes with 2,2′-Dipyridylamine; the Comparative In Vitro Thereof

Cited by 5 publications

References 34 publications

Overcoming Cancer Resistance to Platinum Drugs by Inhibiting Cholesterol Metabolism

Overcoming Cancer Resistance to Platinum Drugs by Inhibiting Cholesterol Metabolism

Geometric Analysis and DFT Study of 2,2′-Dipyridylamine-Stabilized First-Row Transition-Metal Complexes

Overcoming Cancer Resistance to Platinum Drugs by Inhibiting Cholesterol Metabolism

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