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Semaxanib Synthesis
Semaxanib (INN, codenamed SU5416) is a tyrosine-kinase inhibitor drug designed by SUGEN as a cancer therapeutic. It is an experimental stage drug, not licensed for use on human patients outside clinical trials. Semaxanib is a potent and selective synthetic inhibitor of the Flk-1/KDR vascular endothelial growth factor (VEGF) receptor tyrosine kinase. It targets the VEGF pathway, and both ''in vivo'' and ''in vitro'' studies have demonstrated antiangiogenic potential. Research In February 2002, Pharmacia, the then-parent of Sugen, prematurely ended phase III clinical trials of semaxinib in the treatment of advanced colorectal cancer due to discouraging results. Other studies, at earlier phases, have since been conducted. However, due to the prospect of next-generation tyrosine kinase inhibitors and the inefficacy of semaxanib in clinic trials, further development of the drug has been discontinued. A related compound, SU11248 (sunitinib), was further developed by Sugen and subse ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sunitinib
Sunitinib, sold under the brand name Sutent, is an anti-cancer medication. It is a small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) in January 2006. Sunitinib was the first cancer drug simultaneously approved for two different indications. As of August 2021, sunitinib is available as a generic medicine in the US. Medical uses Gastrointestinal stromal tumor Like renal cell carcinoma, gastrointestinal stromal tumors do not generally respond to standard chemotherapy or radiation. Imatinib was the first chemotherapeutic agent proven effective for metastatic gastrointestinal stromal tumors and represented a significant development in the treatment of this rare but challenging disease. However, approximately 20% of patients do not respond to imatinib (early or primary resistance), and among those who do respond init ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Toceranib
Toceranib (INN), sold under the brand name Palladia, is a receptor tyrosine kinase inhibitor that is used in the treatment of canine mast cell tumor also called mastocytoma. It is the first medication developed specifically for the treatment of cancer in dogs. It is used as its phosphate salt, toceranib phosphate. It was developed by SUGEN as SU11654, a sister compound to sunitinib, which was later approved for human therapies. Toceranib is a tyrosine kinase inhibitor and works in two ways: by killing tumor cells and by cutting off the blood supply to the tumor. The most common side effects include diarrhea, decrease or loss of appetite, lameness, weight loss, and blood in the stool. Veterinary uses Toceranib is indicated In medicine, an indication is a valid reason to use a certain test, medication, procedure, or surgery. There can be multiple indications to use a procedure or medication. An indication can commonly be confused with the term diagnosis. A diagnosis ... to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxindole
Oxindole (2-indolone) is an aromatic heterocyclic organic compound with the formula . It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered nitrogen-containing ring. Oxindole is a modified indoline with a substituted carbonyl at the second position of the 5-member indoline ring. Classified as a cyclic amide, it is a pale yellow solid. Formation and reactions Oxindole is derived in nature from tryptophan, formed by gut bacteria ("normal flora"). It is normally metabolized and detoxified from the body by the liver. In excess, it can cause sedation, muscle weakness, hypotension, and coma. Patients with hepatic encephalopathy Hepatic encephalopathy (HE) is an altered level of consciousness as a result of liver failure. Its onset may be gradual or sudden. Other symptoms may include movement problems, changes in mood, or changes in personality. In the advanced stag ... have been recorded to have elevated serum oxindole levels. Treatmen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Knoevenagel Condensation
In organic chemistry, the Knoevenagel condensation () reaction is a type of chemical reaction named after German chemist Emil Knoevenagel. It is a modification of the aldol condensation. A Knoevenagel condensation is a nucleophilic addition of an active hydrogen compound to a carbonyl group followed by a dehydration reaction in which a molecule of water is eliminated (hence ''condensation''). The product is often an α,β-unsaturated ketone (a conjugated enone). In this reaction the carbonyl group is an aldehyde or a ketone. The catalyst is usually a weakly basic amine. The active hydrogen component has the forms: * or for instance diethyl malonate, Meldrum's acid, ethyl acetoacetate or malonic acid, or cyanoacetic acid. * , for instance nitromethane. where Z is an electron withdrawing group. Z must be powerful enough to facilitate deprotonation to the enolate ion even with a mild base. Using a strong base in this reaction would induce self-condensation of the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aldehyde
In organic chemistry, an aldehyde () (lat. ''al''cohol ''dehyd''rogenatum, dehydrogenated alcohol) is an organic compound containing a functional group with the structure . The functional group itself (without the "R" side chain) can be referred to as an aldehyde but can also be classified as a formyl group. Aldehydes are a common motif in many chemicals important in technology and biology. Structure and bonding Aldehyde molecules have a central carbon atom that is connected by a double bond to oxygen, a single bond to hydrogen and another single bond to a third substituent, which is carbon or, in the case of formaldehyde, hydrogen. The central carbon is often described as being sp2- hybridized. The aldehyde group is somewhat polar. The bond length is about 120–122 picometers. Physical properties and characterization Aldehydes have properties that are diverse and that depend on the remainder of the molecule. Smaller aldehydes such as formaldehyde and acetaldehyde are solubl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vilsmeier–Haack Reaction
The Vilsmeier–Haack reaction (also called the Vilsmeier reaction) is the chemical reaction of a substituted formamide (1) with phosphorus oxychloride and an electron-rich arene (3) to produce an aryl aldehyde or ketone (5): : HArZ + POCl3 + H2O → RC(=O)ArZ + HCl + H3PO4 The reaction is named after Anton Vilsmeier and . For example, benzanilide and dimethylaniline react with phosphorus oxychloride to produce an unsymmetrical diaryl ketone. Similarly, anthracene is formylated at the 9-position. The reaction of anthracene with ''N''-methylformanilide, also using phosphorus oxychloride, gives 9-anthracenecarboxaldehyde: : In general, the electron-rich arene (3) must be much more active than benzene for the reaction to proceed; phenols or anilines are good substrates. Reaction mechanism The reaction of a substituted amide with phosphorus oxychloride gives a substituted chloroiminium ion (2), also called the Vilsmeier reagent. The initial product i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Semaxanib Synthesis
Semaxanib (INN, codenamed SU5416) is a tyrosine-kinase inhibitor drug designed by SUGEN as a cancer therapeutic. It is an experimental stage drug, not licensed for use on human patients outside clinical trials. Semaxanib is a potent and selective synthetic inhibitor of the Flk-1/KDR vascular endothelial growth factor (VEGF) receptor tyrosine kinase. It targets the VEGF pathway, and both ''in vivo'' and ''in vitro'' studies have demonstrated antiangiogenic potential. Research In February 2002, Pharmacia, the then-parent of Sugen, prematurely ended phase III clinical trials of semaxinib in the treatment of advanced colorectal cancer due to discouraging results. Other studies, at earlier phases, have since been conducted. However, due to the prospect of next-generation tyrosine kinase inhibitors and the inefficacy of semaxanib in clinic trials, further development of the drug has been discontinued. A related compound, SU11248 (sunitinib), was further developed by Sugen and subse ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Animal Testing On Rodents
Rodents have been employed in biomedical experimentation from the 1650s. Rodent studies up to the early 19th century were mainly physiological or toxicological. The first rodent behavioral study was carried out in 1822, a purely observational study, while quantitative rodent behavioral testing began in the late 19th century. Currently, rodents are commonly used in animal testing for physiological, pathological and behavioral scientific studies, particularly laboratory mouse, mice and laboratory rat, rats, but also guinea pigs, hamsters, gerbils and others. Mice are the most commonly used vertebrate species, due to their availability, size, low cost, ease of handling, and fast Net reproduction rate, reproduction rate. __TOC__ Statistics In the UK in 2015, there were 3.33 million procedures on rodents (80% of total procedures that year). The most common species used were mice (3.03 million procedures, or 73% of the total) and rats (268,522, or 6.5%). Other rodents species included ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Laboratory Rat
Laboratory rats or lab rats are strain (biology), strains of the rat subspecies ''Rattus norvegicus domestica'' (Domestic Norwegian rat) which are bred and kept for scientific research. While Animal testing on rodents, less commonly used for research than laboratory mice, rats have served as an important animal model for research in psychology and biomedical science, and "lab rat" is commonly used as an idiom for a test subject. Origins of rat breeding In 18th-century Europe, wild brown rats (''Rattus norvegicus'') ran rampant and this infestation fueled the industry of rat-catching. Rat-catchers would not only make money by trapping the rodents, but also by selling them rat meat, for food or, more commonly, for rat-baiting. Rat-baiting was a popular sport, which involved filling a pit with rats and timing how long it took for a terrier to kill them all. Over time, breeding the rats for these contests may have produced color variations, notably the albino rat, albino and hoode ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Laboratory Mouse
The laboratory mouse or lab mouse is a small mammal of the order Rodentia which is bred and used for scientific research or feeders for certain pets. Laboratory animal sources for these mice are usually of the species ''Mus musculus''. They are the most commonly used mammalian research model and are used for research in genetics, physiology, psychology, medicine and other scientific disciplines. Mice belong to the Euarchontoglires clade, which includes humans. This close relationship, the associated high homology with humans, their ease of maintenance and handling, and their high reproduction rate, make mice particularly suitable models for human-oriented research. The laboratory mouse genome has been sequenced and many mouse genes have human homologues. Lab mice are sold at pet stores for snake food and can also be kept as pets. Other mouse species sometimes used in laboratory research include two American species, the white-footed mouse (''Peromyscus leucopus'') and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pulmonary Hypertension
Pulmonary hypertension (PH or PHTN) is a condition of increased blood pressure in the pulmonary artery, arteries of the lungs. Symptoms include dypsnea, shortness of breath, Syncope (medicine), fainting, tiredness, chest pain, pedal edema, swelling of the legs, and a fast heartbeat. The condition may make it difficult to exercise. Onset is typically gradual. According to the definition at the 6th World Symposium of Pulmonary Hypertension in 2018, a patient is deemed to have pulmonary hypertension if the pulmonary mean arterial pressure is greater than 20mmHg at rest, revised down from a purely arbitrary 25mmHg, and pulmonary vascular resistance (PVR) greater than 3 Wood units. The cause is often unknown. Risk factors include a family history, prior pulmonary embolism (blood clots in the lungs), HIV/AIDS, sickle cell disease, cocaine use, chronic obstructive pulmonary disease, sleep apnea, living at high altitudes, and problems with the mitral valve. The underlying mechanism typ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
