Sm(Ⅲ), Gd(Ⅲ), and Eu(Ⅲ) complexes with 8-hydroxyquinoline derivatives as potential anticancer agents via inhibiting cell proliferation, blocking cell cycle, and inducing apoptosis in NCI-H460 cells.

Four lanthanide complexes with 8-hydroxyquinoline-2-aldehyde-2-hydrazinopyridine (H-L), 8-hydroxyquinoline-2-aldehyde-2-hydrazimidazole (H-L): [Sm(L)][Sm(L)(NO)]·CHCl·2CHOH (1), [Gd(L)][Gd(L)(NO)]·CHCl·2CHOH (2), [Sm(L)(NO)]·CHOH (3), and [Eu(L)(NO)]·CHOH (4) were synthesized and characterized. In vitro cytotoxicity evaluation showed that the ligands and four lanthanide complexes exhibited cytotoxicity to the five tested tumor cell lines. Among them, complex 1 showed the best antiproliferative activity against NCI-H460 tumor cells.

Visible-light promoted radical cascade cyclization of 3-allyl-2-arylquinazolinones for the synthesis of phosphorylated dihydroisoquinolino[1,2-]quinazolinones.

A novel visible-light promoted metal-free radical cascade cyclization reaction has been developed with 3-allyl-2-arylquinazolinones as a new class of radical acceptor. This photocatalytic protocol represents an efficient approach to construct phosphorylated dihydroisoquinolino[1,2-]quinazolinones featuring mild conditions, broad substrate scope, and gram-scale synthesis.

Sesquilignans PD from var. exerts antitumor effects the ROS/MAPK pathway in liver cancer cells.

Sesquilignans is a natural phenylpropanoid compound that was isolated from var. . In this study, we assessed the antitumor effect of on SK-Hep-1 and HepG2 cells and the underlying molecular mechanisms.

Stereoselective Solid-State Synthesis of Biologically Active Cyclobutane and Dicyclobutane Isomers via Conformation Blocking and Transference.

Conformations in the solid state are typically fixed during crystallization. Transference of "frozen" C=C conformations in 3,5-bis((E)-2-(pyridin-4-yl)vinyl)methylbenzene (CH-3,5-bpeb) by photodimerization selectively yielded cyclobutane and dicyclobutane isomers, one of which (Isomer 2) exhibited excellent in vitro anti-cancer activity towards T-24, 7402, MGC803, HepG-2, and HeLa cells.

Alkaloids from and their anti-proliferative activity against A549 cells by regulating the EGFR/AKT/mTOR pathway.

is frequently used as a traditional Chinese medicine and food supplement. Our previous study revealed that its constituent compounds were able to inhibit cancer cell proliferation. In our continuous exploration of bioactive compounds in , we isolated ten alkaloids (-), including one new natural compound (), and nine known alkaloids (), from an ethanolic extract of the whole plant.

Rhodium(III)-Picolinamide Complexes Act as Anticancer and Antimetastasis Agents via Inducing Apoptosis and Autophagy.

As a continuation of our endeavors in discovering metal-based drugs with cytotoxic and antimetastatic activities, herein, we reported the syntheses of 11 new rhodium(III)-picolinamide complexes and the exploration of their potential anticancer activities. These Rh(III) complexes showed high antiproliferative activity against the tested cancer cell lines in vitro. The mechanism study indicated that ([Rh()(CHCN)Cl]) and ([Rh()(CHCN)Cl]) inhibited cell proliferation by multiple modes of action via cell cycle arrest, apoptosis, and autophagy and inhibited cell metastasis via FAK-regulated integrin β1-mediated suppression of EGFR expression.

In vitro and in vivo antitumor activities of Ru and Cu complexes with terpyridine derivatives as ligands.

Six terpyridine ligands(L-L) with chlorophenol or bromophenol moiety were obtained to prepare metal terpyridine derivatives complexes: [Ru(L)(DMSO)Cl] (1), [Ru(L)(DMSO)Cl] (2), [Ru(L)(DMSO)Cl] (3), [Cu(L)Br]·DMSO (4), Cu(L)Br (5), and [Cu(L)Br]⋅CHOH (6). The complexes were fully characterized. Ru complexes 1-3 showed low cytotoxicity against the tested cell lines.

Copper(II) complex enhanced chemodynamic therapy through GSH depletion and autophagy flow blockade.

Three copper(II) complexes C1-C3 were synthesized and fully characterized as chemodynamic therapy (CDT) anticancer agents. C1-C3 showed greater cytotoxicity than their ligands toward SK-OV-3 and T24 cells. Particularly, C2 showed high cytotoxicity toward T24 cells and low cytotoxicity toward normal human HL-7702 and WI-38 cells.

Arene-Ruthenium(II)/Osmium(II) Complexes Potentiate the Anticancer Efficacy of Metformin via Glucose Metabolism Reprogramming.

Targeting metabolic reprogramming to treat cancer could increase overall survival and reduce side effects. Here, we put forward a strategy using arene-ruthenium(II)/osmium(II) complexes to potentiate the anticancer effect of metformin (Met.) via glucose metabolism reprogramming.

Terpyridine copper(II) complexes as potential anticancer agents by inhibiting cell proliferation, blocking the cell cycle and inducing apoptosis in BEL-7402 cells.

Four mononuclear terpyridine complexes [Cu(H-L)Cl]·CHOH (1), [Cu(H-L)Cl]ClO (2), [Cu(H-L)Cl]·CHOH (3), and [Cu(H-L)(CHOH)(DMSO)](ClO) (4) were prepared and fully characterized. Complexes 1-4 exhibited higher cytotoxic activity against several tested cancer cell lines especially BEL-7402 cells compared to cisplatin, and they showed low toxicity towards normal human liver cells. ICP-MS detection indicated that the copper complexes were accumulated in mitochondria.

Ru(III) complexes with pyrazolopyrimidines as anticancer agents: bioactivities and the underlying mechanisms.

Three ruthenium(III) complexes with pyrazolopyrimidine [Ru(L)(HO)Cl] (1-3, = 1-3) were prepared and characterized. These Ru(III) compounds show strong cytotoxicity against six cancer cell lines and low toxicity to normal human liver cells. Particularly, they exhibited stronger cytotoxicity to SK-OV-3 cells than cisplatin.

Dual-response detection of Ni and Cu ions by a pyrazolopyrimidine-based fluorescent sensor and the application of this sensor in bioimaging.

Herein, a dual-response fluorescent sensor, L, based on pyrazolopyrimidine was designed and developed for the simultaneous detection of Ni and Cu ions in the presence of other metal ions; the structural characterization of L was carried out by FTIR spectroscopy, NMR spectroscopy, HRMS and X-ray diffraction analysis. The sensor L effectively displayed fluorescence quenching towards the Ni and Cu ions with high sensitivity without interference from other metal ions. The results reveal that L binds to Ni and Cu in a 2 : 1 pattern, which matches well with the result of the Job's plot.

Platinum(ii) complexes with rutaecarpine and tryptanthrin derivatives induce apoptosis by inhibiting telomerase activity and disrupting mitochondrial function.

Four new platinum(ii) complexes, [Pt(Rut)(DMSO)Cl] (), [Pt(Try)(DMSO)Cl] (), [Pt(ITry)(DMSO)Cl] () and [Pt(BrTry)(DMSO)Cl] (), with rutaecarpine (Rut), tryptanthrin (Try), 8-iodine-tryptanthrin (ITry) and 8-bromo-tryptanthrin (BrTry) as ligands were synthesized and fully characterized. In these complexes, the platinum(ii) adopts a four-coordinated square planar geometry. The inhibitory activity evaluated by the MTT assay showed that (IC = of 0.

A pyrazolopyrimidine based fluorescent probe for the detection of Cu and Ni and its application in living cells.

A fluorescent sensor L based on a pyrazolopyrimidine core simultaneously detects Cu and Ni ions by photoluminescence quenching, even in the presence of other metal cations. Sensor L possesses high association constants of 5.24 × 10 M and 2.

New dinuclear ruthenium arene complexes containing thiosemicarbazone ligands: synthesis, structure and cytotoxic studies.

A series of mononuclear ruthenium arene complexes with thiosemicarbazone (TSC) ligands (A-type, 1-8) and their corresponding di-nuclear analogues (B-type, 9-16) were synthesized and characterized by NMR, elemental analysis and HR-ESI-mass spectrometry. The molecular structures of 1, 2, 6, 9-11 and 13-16 were determined using single-crystal X-ray diffraction analysis. The Gibbs free energy of the two examples of the two types of complexes (1 and 9) and the bonding order in their single-crystals were studied using density functional theory (DFT) calculations.

Novel Fe and Co Complexes of Natural Product Tryptanthrin: Synthesis and Binding with G-Quadruplex DNA.

Tryptanthrin is one of the most important members of indoloquinoline alkaloids. We obtained this alkaloid from . Two novel Fe and Co complexes of tryptanthrin were first synthesized.

The antitumor activity of zinc(II) and copper(II) complexes with 5,7-dihalo-substituted-8-quinolinoline.

[Zn₂(ClQ)₄(CH₃OH)₂] (1), [Zn(BrQ)₂(H₂O)₂] (2), [Zn₂(ClIQ)₄] (3) and [Cu(BrQ)₂] (4) (H-ClQ = 5,7-dichloro-8-hydroxylquinoline, H-BrQ = 5,7-dibromo-8-hydroxylquinoline, and H-ClIQ = 5-chloro-7-iodo-8-hydroxylquinoline) were synthesized. Compounds 1-4 showed high anti-proliferative cytotoxicities against BEL-7404, SK-OV-3, NCI-H460 tumor cells, and HL-7702 normal cells in vitro, with IC₅₀ values in the 1.4 nM to 32.

High antitumor activity of 5,7-dihalo-8-quinolinolato cerium complexes.

Three cerium complexes: [Ce(ClQ)4] (1) (H-ClQ=5,7-dichloro-8-hydroxylquinoline), [Ce(ClIQ)4]·CH2Cl2·0.5H2O (2) (H-ClIQ=5-chloro-7-iodo-8-hydroxylquinoline) and [Ce2(BrQ)4(H-BrQ)(H2O)3Cl2]·1.5H2O (3) (H-BrQ=5,7-dibromo-8-hydroxylquinoline) were synthesized.

High antitumor activity of 5,7-dihalo-8-quinolinolato tin(IV) complexes.

Three tin(IV) complexes [Sn(ClQ)2Cl2] (1), [Sn(BrQ)2Cl2] (2) and [Sn(ClIQ)2Cl2] (3) were prepared (H-ClQ = 5,7-dichloro-8-hydroxylquinoline, H-BrQ = 5,7-dibromo-8-hydroxylquinoline, H-ClIQ = 5-chloro-7-iodo-8-hydroxylquinoline) and their in vitro cytotoxicities against BEL7404, SKOV-3, NCI-H460, HL-7702 cell lines were evaluated. The complexes showed high anti-proliferative activity toward the tested cell lines with IC50 values ranging from 20 nM to 5.11 μM.

Synthesis, crystal structure, cytotoxicity and DNA interaction of 5,7-dichloro-8-quinolinolato-lanthanides.

Four isostructural lanthanide complexes with 5,7-dichloro-8-quinolinoline (H-ClQ): [Sm(ClQ)(3)(H(2)O)(2)]·1.33EtOH·0.33H(2)O (1), [Eu(ClQ)(3)(H(2)O)(2)]·0.

Bis[4-amino-N-(pyrimidin-2-yl)benzene-sulfonamidato](2,2'-bipyridine)manganese(II).

The title compound, [Mn(C(10)H(9)N(4)O(2)S)(2)(C(10)H(8)N(2))], contains a distorted octa-hedral [Mn(sdz)(2)(bpy)] (sdz is the sulfadiazine anion and bpy is 2,2'-bipyridine) complex mol-ecule. A three-dimensional network is generated by N-H⋯N, N-H⋯O and C-H⋯O hydrogen bonds from the sulfadiazine ligands.