Mixed ligand Re and 99mTc tricarbonyl complexes bearing two important pharmacophores: 2-(4′-aminophenyl)benzothiazole and curcumin

Stouraitis, Alexandros; Sagnou, Marina; Mavroidi, Barbara; Kiritsis, Christos; Shegani, Antonio; Raptopoulou, Catherine; Psycharis, Vassilis; Methenitis, Constantinos; Pirmettis, Ioannis; Papadopoulos, Minas; Pelecanou, Maria

doi:10.1016/j.ica.2024.122172

Inorganica Chimica Acta

2024

DOI: 10.1016/j.ica.2024.122172

|View full text |Cite

Mixed ligand Re and 99mTc tricarbonyl complexes bearing two important pharmacophores: 2-(4′-aminophenyl)benzothiazole and curcumin

Alexandros Stouraitis,

Marina Sagnou,

Barbara Mavroidi

et al.

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2024

2025

Publication Types

Select...

Article2

Relationship

Self Cite0

Independent2

Authors

Journals

Cited by 2 publications

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Synthesis, characterization and comparative biological activity of a novel set of Cu(II) complexes containing azole-based ligand frames

Elwell,

Stein,

Lewis

et al. 2025

Journal of Inorganic Biochemistry

View full text Add to dashboard Cite

Synthesis, characterization and comparative biological activity of a novel set of Cu(II) complexes containing azole-based ligand frames

Elwell,

Stein,

Lewis

et al. 2025

Journal of Inorganic Biochemistry

View full text Add to dashboard Cite

Synthesis and Biological Evaluation of Novel Cationic Rhenium and Technetium-99m Complexes Bearing Quinazoline Derivative for Epidermal Growth Factor Receptor Targeting

Triantopoulou,

Roupa,

Shegani

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

Background/Objectives: Epidermal growth factor receptor (EGFR) plays a vital role in cell proliferation and survival, with its overexpression linked to various malignancies, including non-small cell lung cancer (NSCLC). Although EGFR tyrosine kinase inhibitors (TKIs) are a key therapeutic strategy, acquired resistance and relapse remain challenges. This study aimed to synthesize and evaluate novel rhenium-based complexes incorporating EGFR TKIs to enhance anticancer efficacy, particularly in radiosensitization. Methods: We synthesized a rhenium tricarbonyl complex (Complex 2) and its 99mTc analog (Complex 2’) by incorporating triphenylphosphine instead of bromine as the monodentate ligand and PF6− as the counter-ion, resulting in a positively charged compound that forms cationic structures. Cytotoxicity and EGFR inhibition were evaluated in A431 cells overexpressing EGFR using MTT assays, Western blotting, and flow cytometry. Radiosensitization was tested through MTT and clonogenic assays. The 99mTc complex’s radiochemical yield, stability, and lipophilicity were also assessed. Results: Complex 2 exhibited significant cytotoxicity with an IC50 of 2.6 μM and EGFR phosphorylation inhibition with an IC50 of 130.6 nM. Both complex 1 and 2 induced G0/G1 cell cycle arrest, with Complex 2 causing apoptosis. Radiosensitization was observed at doses above 2 Gy. Complex 2’ demonstrated high stability and favorable lipophilicity (LogD7.4 3.2), showing 12% cellular uptake after 30 min. Conclusions: Complexes 2 and 2’ show promise as dual-function anticancer agents, offering EGFR inhibition, apoptosis induction, and radiosensitization. Their potential as radiopharmaceuticals warrants further in-depth investigation in preclinical models.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Mixed ligand Re and 99mTc tricarbonyl complexes bearing two important pharmacophores: 2-(4′-aminophenyl)benzothiazole and curcumin

Cited by 2 publications

References 34 publications

Synthesis, characterization and comparative biological activity of a novel set of Cu(II) complexes containing azole-based ligand frames

Synthesis, characterization and comparative biological activity of a novel set of Cu(II) complexes containing azole-based ligand frames

Synthesis and Biological Evaluation of Novel Cationic Rhenium and Technetium-99m Complexes Bearing Quinazoline Derivative for Epidermal Growth Factor Receptor Targeting

Contact Info

Product

Resources

About