Novel Metal Complexes As Potential Chemotherapeutic Agents

2021 ◽  
Vol 3 (1) ◽  
pp. 019
Author(s):  
Abdou S. El-Tabl ◽  
Moshira M. Abd-El Wahed ◽  
Al-Zahraa Ibrahim El-Mahsarawy ◽  
Mohamed Samy Abd El-Khalek ◽  
Sameh Anwer Zwam
Keyword(s):  
Metal Complexes ◽  
Chemotherapeutic Agents

Novel Chemotherapeutic Agents - The Contribution of Scorpionates

2020 ◽  
Vol 26 (41) ◽  
pp. 7452-7475 ◽  
Author(s):  
Marta A. Andrade ◽  
Luísa M.D.R.S. Martins
Keyword(s):  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Bioinorganic Chemistry ◽  
Chemotherapeutic Agents ◽  
Great Role ◽  
Anticancer Properties ◽  
Scorpionate Ligands

: The development of safe and effective chemotherapeutic agents is one of the uppermost priorities and challenges of medicinal chemistry and new transition metal complexes are being continuously designed and tested as anticancer agents. Scorpionate ligands have played a great role in coordination chemistry, since their discovery by Trofimenko in the late 1960s, with significant contributions in the fields of catalysis and bioinorganic chemistry. Scorpionate metal complexes have also shown interesting anticancer properties, and herein, the most recent (last decade) and relevant scorpionate complexes reported for application in medicinal chemistry as chemotherapeutic agents are reviewed. The current progress on the anticancer properties of transition metal complexes bearing homo- or hetero- scorpionate ligands, derived from bis- or tris-(pyrazol-1-yl)-borate or -methane moieties is highlighted.

scholarly journals The Platinum(II) Complexes Induced Oxidative Stress of Isolated Rat Heart

2017 ◽  
Vol 18 (2) ◽  
pp. 111-117
Author(s):  
Katarina Radonjic ◽  
Isidora Stojic ◽  
Vladimir Zivkovic ◽  
Ivan Srejovic ◽  
Nevena Jeremic ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Rat Heart ◽  
Clinical Success ◽  
Chemotherapeutic Agents ◽  
Isolated Rat Heart

AbstractInterest for the clinical application of transition metal complexes as chemotherapeutic agents initially started with discovery of cisplatin. Despite the remarkable clinical success, cisplatin treatment is limited due to its resistance and side effects. Over the last 40 years, numerous transition metal complexes were synthesized and investigated in vitro and in vivo in order to establish a metallopharmaceutical that will exert less toxicity and equal or higher potency. We have compared the cardiotoxicity of 2 platinum complexes, one ligand, and a starting salt for complex synthesis using an experimental model of an isolated, perfused rat heart according to the Langendorfftechnique. The cardiotoxicity was assessed by comparison of oxidative stress induced following the perfusion of the following compounds: Dichloro(1,2-diaminocyclohexane)platinum(II), cisplatin, potassium-tetra-chloroplatinum(II) and 1,2-diaminocyclohexane, which were perfused at increasing concentrations from 10−8to 10−4M for 30 minutes. The oxidative stress was assessed by determination of superoxide anion radical, hydrogen peroxide, thiobarbituric acid reactive substances, and nitric oxide from the coronary venous effluent. Our results showed that the levels of oxidative stress parameters were not significantly affected by perfusion with all the tested compounds and were not dose-dependent. These results could be of importance to further investigations concerning the effects of platinum-based potential anticancer drugs on the heart.

scholarly journals HYDRAZIDE SCHIFF BASES OF ACETYLACETONATE METAL COMPLEXES: SYNTHESIS, SPECTROSCOPIC AND BIOLOGICAL STUDIES

2017 ◽  
Vol 9 (12) ◽  
pp. 257 ◽  
Author(s):  
Charity W. Dikio ◽  
Ikechukwu P. Ejidike ◽  
Fanyana M. Mtunzi ◽  
Michael J. Klink ◽  
Ezekiel D. Dikio
Keyword(s):  
Staphylococcus Aureus ◽  
Schiff Base ◽  
Metal Complexes ◽  
Enterococcus Faecalis ◽  
Schiff Bases ◽  
Condensation Reaction ◽  
Chemotherapeutic Agents ◽  
Schiff Base Ligands ◽  
Biological Studies ◽  
Ft Ir

Objective: The study was focused on the synthesis and spectroscopic studies of metal acetylacetonates and their complexes using bidentate Schiff-base ligands (NO), evaluation of their in-vitro antibacterial potentials against pathogenic microorganism.Methods: Acetylacetonate salts of Cobalt(II), Manganese(II) and Magnesium(II) were prepared by reacting their metal hydroxides with acetylacetone. The metal complexes of N'-{(E)-[4-(diethylamino)-2-hydroxyphenyl]methylidene}-4-nitrobenzohydrazide (HL1), N'-{(E)-[4-(diethylamino)-2-hydroxyphenyl]methylidene}-4-methoxybenzohydrazide (HL2) obtained from the condensation reaction of 4-(diethylamino)-2-hydroxybenzaldehyde and 4-nitrobenzohydrazide/ or 4-methoxybenzohydrazide. The synthesized compounds were characterized by fourier transform infrared spectroscopy (FT-IR), proton and carbon-13 nuclear magnetic resonance (NMR), thermogravimetric analysis (TGA). The compounds were screened for their antimicrobial properties against a list of Gram-positive bacterial strains.Results: The FT-IR spectra revealed that the Schiff bases acts as bidentate chelating ligand via nitrogen of the azomethine and phenolic oxygen atoms. NMR reveal the presence of azomethine (HC=N) and aromatic hydrogens at expected chemical shifts confirming the formation of the Schiff base ligands. Thermal decomposition behaviour was studied by thermogravimetry revealing stability up to 260 °C. The compounds were evaluated for their antibacterial potentials against Staphylococcus aureus and Enterococcus faecalis. The manganese acetylacetonato(N'-{(E)-[4-(diethylamino)-2-hydroxyphenyl]methylidene}-4-methoxybenzohydrazide: Mn(acac)(L2) exhibited antimicrobial activities against both Enterococcus faecalis and Staphylococcus aureus with a minimum inhibitory concentration (MIC) of 398.0 μg/mL.Conclusion: The prepared compounds showed no inhibition against the selected pathogenic microorganisms except for Mn(acac)(L2) Standard antibacterial compounds: ampicillin and ciprofloxacin were used as positive control. The antibacterial activity of the compound depends on the kind of substituent on the benzo hydrazide rings at the para position, thereby suggesting the compound as promising chemotherapeutic agents for further structural optimization. 

scholarly journals Bioactivities of holmium(III) and gadolinium(III) complexes of thymoquinone

2021 ◽  
Vol 35 (1) ◽  
pp. 87-96
Author(s):  
N. S. Awwad ◽  
H. A. Ibrahium ◽  
A. A. Shati ◽  
M. A. Alshehri ◽  
K. M. Al-Syaad ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Functional Characterization ◽  
Radical Scavenging ◽  
Chemotherapeutic Agents ◽  
Molecular Structures ◽  
Computational Techniques ◽  
Designed Materials ◽  
Light Chain Enhancer ◽  
Free Radical Scavenging Activities

Chemotherapeutic agents which are the main stay in cancer treatment are toxic with numerous contrary side effects. A number of chemical, physical, and computational techniques were applied to synthesize and elucidate the structural and functional characterization of the new designed bioligands and their metal complexes. Besides, several biological techniques for developing therapeutics and diagnostics agents of these new designed materials were used. The trivalent holmium(III) and gadolinium(III) metal complexes of thymoquinone (TQ) were synthesized. Toxicities and other bioactivites were undertaken with existing drug combinations and more effective tumor models will be established. The molecular structures of TQ-metal complexes were elucidated based on particular spectral approaches. The NF-kB (nuclear factor kappa-light-chain enhancer of activated B Cells) luciferase, elastase release, superoxide anion (O2•−) generation, and DPPH (1,1-diphenyl-2-picryl hydrazyl) free-radical scavenging activities of TQ and its synthesized complexes were elucidated and discussed. The core research is to use coordination and organometallic chemistry to design new bioligands and binary, ternary, mixed ligand, multi metal multi ligand complexes pursing a bio target continuously with structure-activity relationships (SARS).                     KEY WORDS: Thymoquinone, Holmium, Gadolinium, Bioactivities   Bull. Chem. Soc. Ethiop. 2021, 35(1), 87-96. DOI: https://dx.doi.org/10.4314/bcse.v35i1.7

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