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Related Concept Videos

Carbocations02:10

Carbocations

Carbocations are one of the reaction intermediates formed during several nucleophilic substitutions or elimination reactions. A carbocation is an electron-deficient species with the central carbon atom having six electrons and three bonded atoms. The central carbon in a carbocation is sp2 hybridized with trigonal planar geometry. It has an empty p orbital perpendicular to the plane of the structure that can accept electrons. Thus, carbocations act as strong electrophiles and may react with any...
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates these...
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
Complexation Equilibria: The Chelate Effect01:19

Complexation Equilibria: The Chelate Effect

In complexation reactions, metal atoms or cations interact with ligands to form donor-acceptor adducts called metal complexes. Ligands that bind through one donor site are monodentate, ligands with two donor sites are bidentate, and those with more than two donor sites are polydentate ligands. For example, ethylene diamine is a bidentate ligand that binds through two nitrogen donor atoms, forming a five-membered ring. EDTA is a polydentate ligand that binds through four oxygen and two nitrogen...
Electron Transport Chain: Complex I and II01:46

Electron Transport Chain: Complex I and II

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...
Mutagenicity and Carcinogenicity01:25

Mutagenicity and Carcinogenicity

Mutagenicity and carcinogenicity refer to the ability of drugs to cause genetic defects and induce cancer, respectively. The International Agency for Research on Cancer (IARC) classifies agents into four groups based on their carcinogenic potential. Group 1 agents are known human carcinogens; group 2A agents are probably carcinogenic to humans; group 3 agents lack data to support their role in carcinogenesis; and group 4 includes agents for which data support that they are not likely to be...

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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
07:20

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

A platinum Chugaev carbene complex as a potent anticancer agent.

Georges Alves1, Laurent Morel, Malika El-Ghozzi

  • 1CNRS, UMR 6247, GReD Laboratory, 24 Ave des Landais, F-63177, Aubière, France.

Chemical Communications (Cambridge, England)
|June 8, 2011
PubMed
Summary

A novel platinum complex demonstrates significant cytotoxic effects, acting as a cisplatin alternative by interacting with DNA and thiols. Its stability and potential therapeutic applications are highlighted.

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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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Area of Science:

  • Inorganic Chemistry
  • Medicinal Chemistry
  • Materials Science

Background:

  • Cisplatin is a widely used platinum-based chemotherapy drug.
  • Development of novel platinum complexes with improved efficacy and reduced toxicity is an ongoing area of research.
  • Carbene complexes offer unique structural and electronic properties for potential therapeutic applications.

Purpose of the Study:

  • To synthesize and characterize a novel platinum Chugaev complex.
  • To evaluate the cytotoxic activity of the synthesized complex.
  • To investigate the interaction of the complex with biological targets like DNA and thiols.

Main Methods:

  • Synthesis of the platinum Chugaev complex.
  • Characterization using multinuclear NMR spectroscopy.
  • X-ray crystallography for structural elucidation.
  • In vitro assays to assess cytotoxicity and DNA binding.

Main Results:

  • A cis bis acyclic diamino carbene platinum complex was successfully synthesized and characterized.
  • The complex exhibited significant cytotoxic activity, comparable to cisplatin.
  • Evidence of interaction with supercoiled DNA and thiols was observed.
  • Ligand stability was assessed and discussed.

Conclusions:

  • The synthesized platinum Chugaev complex shows promise as a potential chemotherapeutic agent.
  • Its mechanism of action involves interaction with DNA and thiols, similar to cisplatin.
  • Further studies are warranted to explore its therapeutic potential and optimize its structure for enhanced efficacy and safety.