By Tim Storr
Increasing the efficiency of healing compounds, whereas proscribing side-effects, is a standard objective in medicinal chemistry. Ligands that successfully bind steel ions and likewise contain particular gains to augment concentrating on, reporting, and total efficacy are riding innovation in components of disorder prognosis and therapy.
Ligand layout in Medicinal Inorganic Chemistry offers the cutting-edge in ligand layout for medicinal inorganic chemistry functions. each one person bankruptcy describes and explores the applying of compounds that both goal a ailment web site, or are activated through a disease-specific organic process.
Ligand layout is mentioned within the following areas:
- Platinum, Ruthenium, and Gold-containing anticancer agents
- Emissive metal-based optical probes
- Metal-based antimalarial agents
- Metal overload disorders
- Modulation of metal-protein interactions in neurodegenerative diseases
- Photoactivatable steel complexes and their use in biology and medicine
- Radiodiagnostic brokers and Magnetic Resonance Imaging (MRI) agents
- Carbohydrate-containing ligands and Schiff-base ligands in Medicinal Inorganic Chemistry
- Metalloprotein inhibitors
Ligand layout in Medicinal Inorganic Chemistry presents graduate scholars, commercial chemists and educational researchers with a launching pad for brand new examine in medicinal chemistry.
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Additional info for Ligand Design in Medicinal Inorganic Chemistry
Blood vessels in tumours are irregular in shape, leaky and dilated, and the endothelial cells are poorly aligned and characterised by large fenestrations [1, 2]. As a result, large molecules such as polymers and nanoparticles present in the blood plasma are able to leak into tumour tissue, while being largely restricted from entering normal, healthy tissue [1, 2]. In addition, these large molecules tend to be retained by the tumour mass due to poor lymphatic drainage [1, 2]. This phenomenon, dubbed the EPR effect, provides the rationale for employing high molecular weight ligands to selectively deliver platinum complexes to tumour regions.
Liu et al. have prepared a series of oxaliplatin analogues functionalised with glucose molecules (24–26) . The oxalato ligand of oxaliplatin was replaced with a malonato ligand to provide an extra carbon as an attachment point for the glucose molecule. Similarly to oxalato complexes, malonato complexes are characterised by relatively slow aquation kinetics . In view of this, the glucose targeting group was envisaged to remain bound to the platinum centre in the bloodstream, and only released once inside target cells.
In vivo evaluations in tumour-bearing mice revealed that treatment with (44) resulted in almost three-fold higher platinum accumulation in tumour tissue than the corresponding treatment with the disuccinato platinum(IV) monomer. 2). No comparisons with cisplatin were reported. 15) . Carbon nanotubes possess a number of advantages as drug delivery agents, including excellent cell membrane permeability, long circulating times and intrinsic near-infrared fluorescent properties, which allow their distribution in biological systems to be mapped [169, 170].