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Tirapazamine Synthesis
Tirapazamine (SR-4233, WIN 59075) is an experimental anticancer drug that is activated to a toxic radical only at very low levels of oxygen ( hypoxia). Such levels are common in human solid tumors, a phenomenon known as tumor hypoxia. Thus, tirapazamine is activated to its toxic form preferentially in the hypoxic areas of solid tumors. Cells in these regions are resistant to killing by radiotherapy and most anticancer drugs. Thus the combination of tirapazamine with conventional anticancer treatments is particularly effective. , tirapazamine is undergoing phase III testing in patients with head and neck cancer and gynecological cancer, and similar trials are being undertaken for other solid tumor types. Chemically it is an aromatic heterocycle di-N-oxide. Its full chemical name is 3-amino-1,2,4-benzotriazine-1,4 dioxide. Originally it was prepared in a program screening for new herbicides in 1972. Its clinical use was first described by Zeman ''et al.'' in 1986. While tirapazami ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SR-4233
Tirapazamine ( SR-4233, WIN 59075) is an experimental anticancer drug that is activated to a toxic radical only at very low levels of oxygen ( hypoxia). Such levels are common in human solid tumors, a phenomenon known as tumor hypoxia. Thus, tirapazamine is activated to its toxic form preferentially in the hypoxic areas of solid tumors. Cells in these regions are resistant to killing by radiotherapy and most anticancer drugs. Thus the combination of tirapazamine with conventional anticancer treatments is particularly effective. , tirapazamine is undergoing phase III testing in patients with head and neck cancer and gynecological cancer, and similar trials are being undertaken for other solid tumor types. Chemically it is an aromatic heterocycle di-N-oxide. Its full chemical name is 3-amino-1,2,4-benzotriazine-1,4 dioxide. Originally it was prepared in a program screening for new herbicides in 1972. Its clinical use was first described by Zeman ''et al.'' in 1986. While tirapazam ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cytotoxic Agents
Cytotoxicity is the quality of being toxic to cells. Examples of toxic agents are toxic metals, toxic chemicals, microbe neurotoxins, radiation particles and even specific neurotransmitters when the system is out of balance. Also some types of drugs, e.g alcohol, and some venom, e.g. from the puff adder (''Bitis arietans'') or brown recluse spider (''Loxosceles reclusa'') are toxic to cells. Cell physiology Treating cells with the cytotoxic compound can result in a variety of prognoses. The cells may undergo necrosis, in which they lose membrane integrity and die rapidly as a result of cell lysis. The cells can stop actively growing and dividing (a decrease in cell viability), or the cells can activate a genetic program of controlled cell death (apoptosis). Cells undergoing necrosis typically exhibit rapid swelling, lose membrane integrity, shut down metabolism, and release their contents into the environment. Cells that undergo rapid necrosis in vitro do not have sufficient tim ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amine Oxides
In chemistry, an amine oxide, also known as an amine ''N''-oxide or simply ''N''-oxide, is a chemical compound that has the chemical formula . It contains a nitrogen-oxygen coordinate covalent bond with three additional hydrogen and/or substituent-groups attached to nitrogen. Sometimes it is written as or, alternatively, as . In the strict sense, the term ''amine oxide'' applies only to oxides of tertiary amines. Sometimes it is also used for the analogous derivatives of primary and secondary amines. Examples of amine oxides include pyridine-''N''-oxide, a water-soluble crystalline solid with melting point 62–67 °C, and ''N''-methylmorpholine ''N''-oxide, which is an oxidant. Applications Amine oxides are surfactants commonly used in consumer products such as shampoos, conditioners, detergents, and hard surface cleaners. Alkyl dimethyl amine oxide (chain lengths C10–C16) is the most commercially used amine oxide. They are considered a high production volume class o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SRI International
SRI International (SRI) is a nonprofit organization, nonprofit scientific research, scientific research institute and organization headquartered in Menlo Park, California, United States. It was established in 1946 by trustees of Stanford University to serve as a center of innovation to support economic development in the region. The organization was founded as the Stanford Research Institute. SRI formally separated from Stanford University in 1970 and became known as SRI International in 1977. SRI performs client-sponsored research and development for government agencies, commercial businesses, and private foundations. It also licenses its technologies, forms strategic partnerships, sells products, and creates Research spin-off, spin-off companies. SRI's headquarters are located near the Stanford University campus. SRI's annual revenue in 2014 was approximately $540 million, which tripled from 1998 under the leadership of Curtis Carlson. In 1998, the organization was on the ver ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Cancer Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydrogen Peroxide
Hydrogen peroxide is a chemical compound with the formula . In its pure form, it is a very pale blue liquid that is slightly more viscosity, viscous than Properties of water, water. It is used as an oxidizer, bleaching agent, and antiseptic, usually as a dilute solution (3%–6% by weight) in water for consumer use and in higher concentrations for industrial use. Concentrated hydrogen peroxide, or "high-test peroxide", decomposes explosively when heated and has been used as both a monopropellant and an oxidizer in rocketry. Hydrogen peroxide is a reactive oxygen species and the simplest peroxide, a compound having an oxygen–oxygen single bond. It decomposes slowly into water and elemental oxygen when exposed to light, and rapidly in the presence of organic or reactive compounds. It is typically stored with a Stabilizer (chemistry), stabilizer in a weakly acidic solution in an opaque bottle. Hydrogen peroxide is found in biological systems including the human body. Enzymes that u ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrogen
Nitrogen is a chemical element; it has Symbol (chemistry), symbol N and atomic number 7. Nitrogen is a Nonmetal (chemistry), nonmetal and the lightest member of pnictogen, group 15 of the periodic table, often called the Pnictogen, pnictogens. It is a common element in the universe, estimated at Abundance of the chemical elements, seventh in total abundance in the Milky Way and the Solar System. At standard temperature and pressure, two atoms of the element chemical bond, bond to form N2, a colourless and odourless diatomic molecule, diatomic gas. N2 forms about 78% of Atmosphere of Earth, Earth's atmosphere, making it the most abundant chemical species in air. Because of the volatility of nitrogen compounds, nitrogen is relatively rare in the solid parts of the Earth. It was first discovered and isolated by Scottish physician Daniel Rutherford in 1772 and independently by Carl Wilhelm Scheele and Henry Cavendish at about the same time. The name was suggested by French chemist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyanamide
Cyanamide is an organic compound with the formula C N2 H2. This white solid is widely used in agriculture and the production of pharmaceuticals and other organic compounds. It is also used as an alcohol-deterrent drug. The molecule features a nitrile group attached to an amino group. Derivatives of this compound are also referred to as cyanamides, the most common being calcium cyanamide (CaCN2). Tautomers and self-condensations Containing both a nucleophilic and electrophilic site within the same molecule, cyanamide undergoes various reactions with itself. Cyanamide exists as two tautomers, one with the connectivity N≡C–NH2 and the other with the formula HN=C=NH (" carbodiimide" tautomer). The N≡C–NH2 form dominates, but in a few reactions (e.g. silylation) the diimide form appears to be important. Cyanamide dimerizes to give 2-cyanoguanidine (dicyandiamide). This dimerization is hindered or reversed by acids and is inhibited by low temperatures. The cyclic trime ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2-nitroaniline
2-Nitroaniline is an organic compound with the formula H2NC6H4NO2. It is a derivative of aniline, carrying a nitro functional group in position 2. It is mainly used as a precursor to o-phenylenediamine. Synthesis 2-Nitroaniline is prepared commercially by the reaction of 2-nitrochlorobenzene with ammonia: :ClC6H4NO2 + 2 NH3 → H2NC6H4NO2 + NH4Cl Many other methods exist for the synthesis of this compound. Direct nitration of aniline is inefficient since anilinium is produced instead. Nitration of acetanilide gives only traces of 2-nitro isomer is obtained due to the great steric effect of the amide. Sulfonation is usually used to block the 4 position and increases the effectiveness to 56%. Uses and reactions 2-Nitroaniline is the main precursor to phenylenediamines, which are converted to benzimidazoles, a family of heterocycles that are key components in pharmaceuticals. Aside from its reduction to phenylenediamine, 2-nitroaniline undergoes other reactions anticipated for a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tirapazamine Synthesis
Tirapazamine (SR-4233, WIN 59075) is an experimental anticancer drug that is activated to a toxic radical only at very low levels of oxygen ( hypoxia). Such levels are common in human solid tumors, a phenomenon known as tumor hypoxia. Thus, tirapazamine is activated to its toxic form preferentially in the hypoxic areas of solid tumors. Cells in these regions are resistant to killing by radiotherapy and most anticancer drugs. Thus the combination of tirapazamine with conventional anticancer treatments is particularly effective. , tirapazamine is undergoing phase III testing in patients with head and neck cancer and gynecological cancer, and similar trials are being undertaken for other solid tumor types. Chemically it is an aromatic heterocycle di-N-oxide. Its full chemical name is 3-amino-1,2,4-benzotriazine-1,4 dioxide. Originally it was prepared in a program screening for new herbicides in 1972. Its clinical use was first described by Zeman ''et al.'' in 1986. While tirapazami ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitroxide
Aminoxyl denotes a radical functional group with general structure R2N–O•. It is commonly known as a nitroxyl radical or a nitroxide, however IUPAC discourages the use of these terms, as they erroneously suggest the presence of a nitro group. Aminoxyls are structurally related to hydroxylamines and ''N''-oxoammonium salts, with which they can interconvert via a series of redox steps. Aminoxyl radical.svg, The general structure of the aminoxyl radical 2,2,6,6-Tetramethylpiperidinyloxyl.svg, TEMPO, a commonly encountered organic aminoxyl radical Kaliumnitrosodisulfonat.svg, Fremy's salt, an inorganic aminoxyl radical Sterically unhindered aminoxyls bearing α-hydrogens are unstable and undergo rapid disproportionation to nitrones and hydroxylamines. Sterically hindered aminoxyls without α-hydrogens, such TEMPO and TEMPOL, and are persistent (stable) radicals and find use in a range of applications, both on the laboratory scale and in industry. Their ability to reversibly ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
