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Related Concept Videos

Metal-Ligand Bonds02:51

Metal-Ligand Bonds

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The hemoglobin in the blood, the chlorophyll in green plants, vitamin B-12, and the catalyst used in the manufacture of polyethylene all contain coordination compounds. Ions of the metals, especially the transition metals, are likely to form complexes.
In these complexes, transition metals form coordinate covalent bonds, a kind of Lewis acid-base interaction in which both of the electrons in the bond are contributed by a donor (Lewis base) to an electron acceptor (Lewis acid). The Lewis acid in...
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Coordination Number and Geometry02:57

Coordination Number and Geometry

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For transition metal complexes, the coordination number determines the geometry around the central metal ion. Table 1 compares coordination numbers to molecular geometry. The most common structures of the complexes in coordination compounds are octahedral, tetrahedral, and square planar.
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Crystal Field Theory - Octahedral Complexes02:58

Crystal Field Theory - Octahedral Complexes

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Crystal Field Theory
To explain the observed behavior of transition metal complexes (such as colors), a model involving electrostatic interactions between the electrons from the ligands and the electrons in the unhybridized d orbitals of the central metal atom has been developed. This electrostatic model is crystal field theory (CFT). It helps to understand, interpret, and predict the colors, magnetic behavior, and some structures of coordination compounds of transition metals.
CFT focuses on...
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Colors and Magnetism03:02

Colors and Magnetism

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Color in Coordination Complexes
When atoms or molecules absorb light at the proper frequency, their electrons are excited to higher-energy orbitals. For many main group atoms and molecules, the absorbed photons are in the ultraviolet range of the electromagnetic spectrum, which cannot be detected by the human eye. For coordination compounds, the energy difference between the d orbitals often allows photons in the visible range to be absorbed and emitted, which is seen as colors by the human...
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Electron Transport Chain: Complex I and II01:46

Electron Transport Chain: Complex I and II

11.9K
The mitochondrial electron transport chain (ETC) is the main energy generation system in the eukaryotic cells. However, mitochondria also produce cytotoxic reactive oxygen species (ROS) due to the large electron flow during oxidative phosphorylation. While Complex I is one of the primary sources of superoxide radicals, ROS production by Complex II is uncommon and may only be observed in cancer cells with mutated complexes.
ROS generation is regulated and maintained at moderate levels necessary...
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Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
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Related Experiment Video

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Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
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Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay

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Mixed-ligand mononuclear copper(II) complex: crystal structure and anticancer activity.

Xiu-Ying Qin1, Ya-Nan Liu, Qian-Qian Yu

  • 1Department of Chemistry, Jinan University, Guangzhou 510632, China; College of Pharmacy, Guilin Medical University, Guilin 541004 (China).

Chemmedchem
|May 21, 2014
PubMed
Summary

A novel copper(II) complex shows promise as an anticancer drug candidate. It effectively induces apoptosis, inhibits angiogenesis, and reduces proliferation by targeting G-quadruplex structures and key cancer-related proteins.

Keywords:
VEGF G-quadruplexesanti-angiogenesisantitumor agentsapoptosiscopper(II) complexes

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Ion Mobility-Mass Spectrometry Techniques for Determining the Structure and Mechanisms of Metal Ion Recognition and Redox Activity of Metal Binding Oligopeptides
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Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
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Ion Mobility-Mass Spectrometry Techniques for Determining the Structure and Mechanisms of Metal Ion Recognition and Redox Activity of Metal Binding Oligopeptides
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Ion Mobility-Mass Spectrometry Techniques for Determining the Structure and Mechanisms of Metal Ion Recognition and Redox Activity of Metal Binding Oligopeptides

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Area of Science:

  • Inorganic Chemistry
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • Copper(II) complexes are explored for their therapeutic potential.
  • Targeting angiogenesis and apoptosis are key strategies in cancer therapy.
  • G-quadruplex structures in promoter regions are emerging therapeutic targets.

Purpose of the Study:

  • To synthesize and characterize a novel copper(II) mixed-ligand complex.
  • To evaluate the in vitro anticancer properties of the complex.
  • To investigate the complex's mechanism of action, including G-quadruplex interaction and protein modulation.

Main Methods:

  • Synthesis and crystal structure characterization of the copper(II) complex.
  • In vitro assays for apoptosis induction, anti-angiogenesis, and antiproliferative activity.
  • Human serum albumin (HSA) binding studies at physiological pH.
  • G-quadruplex induction and stabilization assays using VEGF promoter G-rich sequences.
  • Western blot analysis for p-Akt and p-Erk1/2 protein expression.
  • Reactive oxygen species (ROS) level measurements.

Main Results:

  • The novel copper(II) complex was successfully synthesized and structurally characterized.
  • The complex demonstrated significant in vitro apoptosis-inducing, anti-angiogenic, and antiproliferative effects.
  • It binds to human serum albumin (HSA) under physiological conditions.
  • The complex effectively induces and stabilizes G-quadruplex structures in the VEGF promoter.
  • Uptake was strong, with inhibition of p-Akt and p-Erk1/2 phosphorylation and increased ROS levels observed.

Conclusions:

  • The synthesized copper(II) complex exhibits potent anticancer activities through multiple mechanisms.
  • Its ability to interact with G-quadruplex structures offers a novel therapeutic avenue for anti-angiogenesis.
  • The complex shows potential as a candidate for anticancer drug development.