Copper(II) Complexes with 1-(Isoquinolin-3-yl)heteroalkyl-2-ones: Synthesis, Structure and Evaluation of Anticancer, Antimicrobial and Antioxidant Potential DOI Open Access
Łukasz Balewski, Tomasz Plech, Izabela Korona‐Głowniak

et al.

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 25(1), P. 8 - 8

Published: Dec. 19, 2023

Four copper(II) complexes, C1–4, derived from 1-(isoquinolin-3-yl)heteroalkyl-2-one ligands L1–4 were synthesized and characterized using an elemental analysis, IR spectroscopic data as well single crystal X-ray diffraction for complex C1. The stability of complexes C1–4 under conditions mimicking the physiological environment was estimated UV-Vis spectrophotometry. antiproliferative activity both compounds evaluated MTT assay on four human cancer cell lines, A375 (melanoma), HepG2 (hepatoma), LS-180 (colon cancer) T98G (glioblastoma), a non-cancerous line, CCD-1059Sk (human normal skin fibroblasts). Complexes showed greater potency against HepG2, LS180 lines than etoposide (IC50 = 5.04–14.89 μg/mL vs. IC50 43.21–>100 μg/mL), while free remained inactive in all lines. prominent compound C2 appeared to be more selective towards cells compared with C1, C3 C4. treatment resulted sub-G1 G2/M cycle arrest, respectively, which accompanied by DNA degradation. Moreover, non-cytotoxic doses synergistically enhanced cytotoxic effects chemotherapeutic drugs, including etoposide, 5-fluorouracil temozolomide, cells. antimicrobial activities L2–4 their C2–4 different types Gram-positive bacteria, Gram-negative bacteria yeast species. No correlation found between results experiments. antioxidant determined DPPH ABTS radical scavenging methods. Antiradical tests revealed that among investigated compounds, C4 possessed strongest properties. Finally, ADME technique used determine physicochemical drug-likeness properties obtained complexes.

Language: Английский

Precision therapeutics for inflammatory bowel disease: advancing ROS-responsive nanoparticles for targeted and multifunctional drug delivery DOI
Xiangang Wan,

Caijie Zhang,

Pengyu Lei

et al.

Journal of Materials Chemistry B, Journal Year: 2025, Volume and Issue: 13(10), P. 3245 - 3269

Published: Jan. 1, 2025

This review discusses ROS-responsive nanoparticles in IBD therapy, highlighting challenges, solutions, and the “layered programmable delivery” strategy for enhanced drug delivery localized treatment.

Language: Английский

Citations

0
Drug delivery for platinum therapeutics DOI
Hui Liu, Jiahui Zou, Xiaotong Li

et al.

Journal of Controlled Release, Journal Year: 2025, Volume and Issue: 380, P. 503 - 523

Published: Feb. 11, 2025

Language: Английский

Citations

0
Advances in the Potential of Quinoline‐Derived Metal Complexes as Antimalarial Agents: A Review DOI Open Access
Carla Peron, Raoni S. B. Gonçalves, Sidnei Moura

et al.

Applied Organometallic Chemistry, Journal Year: 2025, Volume and Issue: 39(3)

Published: Feb. 11, 2025

ABSTRACT Quinolines obtained from native trees of South and Central America, the genus Cinchona , have been used since 17th century for treatment malaria. However, it was only in 1820 that quinine had its structure elucidated, subsequently, during 20th century, several synthetic derivatives were produced with superior activities. In parallel, search synthesis metal complex compounds malaria dates 1994, development ferroquine, an iron derived chloroquine, developed by Biot collaborators at Lille University. After, there are complexes synthesized various metals, such as ruthenium, gold, iridium, platinum, over last 30 years, which aims this review. This review identified 84 quinoline–metal reported across 25 studies, gold (Complex 63) showing significant potency against FcBI strain (IC 50 10 nM), outperforming chloroquine (CQ, indicating coordination enhances drug's action. The ruthenium 03) exhibited activity PFB but less effective than CQ 22.5 vs. 8.2 nM). Other complexes, Au(III) 61), Ir(I) 52), Ir(II) 50), also demonstrated promising results varying effectiveness different strains. Structural features, including linear geometry Au(I) square planar or piano stool geometries Ru(II) Ir play crucial roles influencing their biological activity. These findings highlight potential improving antimalarial efficacy.

Language: Английский

Citations

0
Substituent Effect of Superhalogens on the Metallodrug IMeAuCl: A DFT Study DOI Open Access
Xin Cheng, Bin Liu, Jinghua Chen

et al.

ChemPhysChem, Journal Year: 2025, Volume and Issue: unknown

Published: March 4, 2025

Halogens are usually involved in numerous anticancer drugs and play an important role activity. Taking the IMeAuCl, a potent drug as example, substituent effect of superhalogens X@B12N12 (X=F, Cl, Br) on structures, electronic properties, chemical reactivity with biomolecular targets this metallodrug has been investigated. Substituting for Cl atom IMeAuCl results polar covalent bonds between Au N atoms resulting Au-X derivatives. The introduction enhances polarity solubility Au-X, which enables them to directly react biological target molecules without undergoing hydrolysis. In particular, it is found that higher electron affinity (EA) lower energy barrier reaction molecules, maybe benefit its high With regard this, another complex Au-BF4 better activity also designed by replacing BF4, well-known superhalogen EA value than X@B12N12. Thus, study provides new strategy improve antitumor halogen-containing from theoretical point view.

Language: Английский

Citations

0
PEGylation Effects on Amphiphilic Platinum(IV) Complexes: Influence on Uptake, Activation, and Cytotoxicity DOI Creative Commons
Arpit Sharma,

Md Al Amin,

Man B. Kshetri

et al.

Pharmaceutics, Journal Year: 2025, Volume and Issue: 17(4), P. 440 - 440

Published: March 29, 2025

Background/Objectives: The utilization of amphiphilic Pt(IV) complexes as prodrugs offers a promising strategy to revolutionize Pt-based cancer therapy by enhancing drug delivery and activation. While PEGylation is widely used optimize properties, its impact on the biological behavior remains unclear. This study systematically investigates how varying molecular weights influences their cytotoxicity, cellular uptake, Methods: were synthesized with PEG chains different using HATU-catalyzed amide bond formation copper-free click chemistry. Their properties assessed through cell-based analyses, focusing activation reductants. Results: Small modifications retained potent cytotoxicity prodrugs, whereas large significantly reduced efficacy. decrease in potency was linked impaired uptake mitochondrial accumulation. Additionally, slowed reduction reductants, further limiting anticancer activities. Conclusions: These findings underscore critical role metallodrug design provide key insights into optimizing strategies for platinum–based therapies.

Language: Английский

Citations

0
Novel platinum(IV) prodrugs with tetraacetylriboflavin axial ligand possessing enhanced light-induced toxicity DOI
Daniil Viktorovich Spector, Roman Akasov, Dmitrii M. Mazur

et al.

Mendeleev Communications, Journal Year: 2025, Volume and Issue: 35(3), P. 282 - 284

Published: Jan. 1, 2025

Language: Английский

Citations

0
Fluorine‐Substituted Rhenium(I) Metallocycle: A New Class of Potent Anticancer Agent DOI
Reema L. Borkar,

Chandra Lekha Putta,

Bhaskaran Shankar

et al.

Chemistry - An Asian Journal, Journal Year: 2025, Volume and Issue: unknown

Published: April 14, 2025

Abstract Fluorine and nonfluorine substituted rhenium(I) metallocycles, fac ‐[{Re(CO) 3 } 2 ( μ ‐SO 4 )(L1) ] C1 ) )(L2) C2 ), respectively, were synthesized using Re (CO) 10 , sodium bisulfite, fluorobenzimidazolyl/benzimidazolyl‐based ditopic nitrogen‐donor ligands (L1/L2), toluene–acetone via coordination‐driven one‐pot solvothermal approach. The metallocycles characterized elemental analysis, ESI‐TOF‐MS, ATR‐IR, NMR, PXRD methods. molecular structures of ·9(DMSO), ·(toluene)(acetone), ·(toluene) determined SCXRD analysis. in vitro cytotoxicity study was performed against cervical (HeLa) skin (B16) cancer cells. Murine fibroblast (L929) mouse myoblast (C2C12) cells used as noncarcinogenic model cell lines for biocompatibility determination. exhibited potent anticancer activity both lines, showing greater efficacy than the commonly cisplatin. Moreover, fluorine‐substituted metallocycle significantly higher nonfluorinated metallocycle, indicating a fluorine effect. Further, in‐depth studies on HeLa showed elevated intracellular ROS generation, disruption mitochondrial membrane potential, antiproliferative properties. also revealed its ability to bind with DNA induce changes cellular morphology, thus leading damage death by apoptosis. Molecular docking B‐DNA macromolecule binding sites, affinity, type noncovalent interactions.

Language: Английский

Citations

0
Cu(ii) flavonoids as potential photochemotherapeutic agents DOI

Namisha Das,

Bidisha R. Bora,

Aarti Upadhyay

et al.

Dalton Transactions, Journal Year: 2024, Volume and Issue: 53(7), P. 3316 - 3329

Published: Jan. 1, 2024

Cu( ii ) flavonoid complexes having phenanthroline bases display significant visible-light assisted cytotoxicity in MCF-7 and A549 cancer cells with low dark toxicity via ROS mediated cell death.

Language: Английский

Citations

2
Recent Development of Transition Metal Complexes as Chemotherapeutic Hypoxia Activated Prodrug (HAP) DOI

K. Jagathesan,

Sovan Roy

ChemMedChem, Journal Year: 2024, Volume and Issue: 19(14)

Published: April 18, 2024

Hypoxia is a state characterized by low concentration of Oxygen. Hypoxic often found in the central region solid tumors. associated with abnormal neovascularization resulted poor blood flow tissues and increased proliferation tumor cells, imbalance between O

Language: Английский

Citations

2
Omeprazole-Loaded Copper Nanoparticles for Mitochondrial Damage Mediated Synergistic Anticancer Activity against Melanoma Cells DOI
Kalyani Eswar,

Sri Amruthaa Sankaranarayanan,

Rupali Srivastava

et al.

ACS Applied Bio Materials, Journal Year: 2024, Volume and Issue: 7(7), P. 4795 - 4803

Published: July 3, 2024

Metallic nanoparticles are promising candidates for anticancer therapies. Among the different metallic systems studied, copper is an affordable and biologically available metal with a high redox potential. Copper-based widely used in studies owing to their ability react intracellular glutathione (GSH) induce Fenton-like reaction. However, considering metastatic potential versatility of tumor microenvironment, modalities single therapeutic agent may not be effective. Hence, enhance efficiency chemotherapeutic drugs, repurposing them or conjugating other essential. Omeprazole FDA-approved proton pump inhibitor clinics treatment ulcers. has also been studied its sensitize cancer cells chemotherapy apoptosis. Herein, we report nanosystem comprising encapsulating omeprazole (CuOzL) against B16 melanoma cells. The developed nanoformulation exerted significant synergistic activity when compared either alone by inducing cell death through excessive ROS generation subsequent mitochondrial damage.

Language: Английский

Citations

2