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Nitrosourea
Nitrosourea is both the name of a molecule, and a class of compounds that include a nitroso (R-NO) group and a urea. Examples Examples include: * Arabinopyranosyl-''N''-methyl-''N''-nitrosourea (Aranose) * Carmustine (BCNU, BiCNU) * Chlorozotocin * Ethylnitrosourea (ENU) * Fotemustine * Lomustine (CCNU) * Nimustine * ''N''-Nitroso-''N''-methylurea (NMU) * Ranimustine (MCNU) * Semustine * Streptozocin (Streptozotocin) Nitrosourea compounds are DNA alkylating agents and are often used in chemotherapy. They are lipophilic and thus can cross the blood–brain barrier, making them useful in the treatment of brain tumors such as glioblastoma multiforme. File:Aranose (Haworth).svg, Arabinopyranosyl-''N''-methyl-''N''-nitrosourea File:Carmustine.svg, Carmustine File:Chlorozotocin (Haworth).svg, Chlorozotocin File:ENU.svg, Ethylnitrosourea File:Fotemustine.svg, Fotemustine File:Lomustine.svg, Lomustine File:N-Nitroso-N-methylurea.svg, ''N''-Nitroso-''N''-methylurea File:N ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arabinopyranosyl-N-methyl-N-nitrosourea
Arabinopyranosyl-''N''-methyl-''N''-nitrosourea, also known as Aranose (Араноза) is a cytostatic anticancer chemotherapeutic drug of an alkylating type. Chemically it is a nitrosourea derivative. It was developed in the Soviet Union in the 1970s. It was claimed by its developers that its advantages over other nitrosoureas are a relatively low hematological toxicity (compared to other nitrosoureas available at that time) and a wider therapeutic index, which allows for its outpatient administration. History It was first synthesized in late 1970s in the Laboratory of Organic Synthesis of Soviet Cancer Research Institute (which belonged to Academy of Medical Sciences of the USSR). Its first clinical trials in USSR were conducted in the late 1980s. Those trials confirmed its potential clinical efficacy in melanoma and better relative safety & improved tolerability over other nitrosourea antineoplastic compounds available at that time. In 1996 the compound obtained a Russia ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ethylnitrosourea
ENU, also known as ''N''-ethyl-''N''-nitrosourea (chemical formula C3H7N3O2), is a highly potent mutagen. For a given gene in mice, ENU can induce 1 new mutation in every 700 loci. It is also toxic at high doses. The chemical is an alkylating agent, and acts by transferring the ethyl group of ENU to nucleobases (usually thymine) in nucleic acids. Its main targets are the spermatogonial stem cells, from which mature sperm are derived. Background of discovery of ENU as a mutagen Bill Russell (1951) created a landmark in the field of mouse genetics by creating a specifically designed mouse strain, the ''T'' (test) stock that was used in genetic screens for testing mutagens such as radiations and chemicals. The ''T''-stock mouse harbors 7 recessive, viable mutations affecting easily recognizable traits. At the Oak Ridge National Laboratory, Russell's initial goal was to determine the rate of inheritable gene mutations in the germ line induced by radiations. Thus he decided to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Semustine
Semustine (1- (2-Chloroethyl)-3-(trans-4-methylcyclohexyl)- 1-nitrosourea, MeCCNU) is an alkylating nitrosourea compound used in chemotherapy treatment of various types of tumours. Due to its lipophilic property, semustine can cross the blood-brain barrier for the chemotherapy of brain tumours, where it interferes with the cellular DNA of the highly dividing cells. Semustine, just as lomustine, is administered orally. It has been reported that semustine can perform the main mechanism of action at molecular level via the alkylation of DNA nitrogenous bases in duplex by results of inhibition of DNA replication, transcription, and translation by way of alkylation of DNA, under pH-dependent conditions by hydrolysis, forming chloro-carbonium ions. Sufficient evidence was found that treatment with semustine can cause acute leukaemia as a delayed effect in very rare cases. History During the past two decades, massive developments of various categories of anti-cancer drugs have been obs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carmustine
Carmustine, sold under the brand name BiCNU among others, is a medication used mainly for chemotherapy. It is a nitrogen mustard β-chloro- nitrosourea compound used as an alkylating agent. Description Carmustine is an orange-yellow solid medication used mainly for chemotherapy. It is a nitrogen mustard β-chloro- nitrosourea compound. Mechanism of action As an alkylating agent, carmustine can form interstrand crosslinks in DNA, which prevents DNA replication and DNA transcription. Uses Carmustine is used as an alkylating agent to treat several types of brain cancer including glioma, glioblastoma multiforme, medulloblastoma and astrocytoma), multiple myeloma, and lymphoma (Hodgkin's and non-Hodgkin). Carmustine is sometimes used in conjunction with alkyl guanine transferase (AGT) inhibitors, such as ''O''6-benzylguanine. The AGT-inhibitors increase the efficacy of carmustine by inhibiting the direct reversal pathway of DNA repair, which will prevent formation of the inters ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lomustine
Lomustine (INN); abbreviated as CCNU; original brand name CeeNU, now marketed as Gleostine) is an alkylating nitrosourea compound used in chemotherapy. It is closely related to semustine and is in the same family as streptozotocin. It is a highly lipid-soluble drug, thus it crosses the blood–brain barrier. This property makes it ideal for treating brain tumors, which is its primary use, although it is also used to treat Hodgkin lymphoma as a second-line option. Lomustine has a long time to nadir (the time when white blood cells reach their lowest number). Unlike carmustine, lomustine is administered orally. It is a bifunctional alkylating agent, alkylates both DNA and RNA, has the ability to created interstrand cross-links (ICLs) in DNA. As with other nitrosoureas, it may also inhibit several key enzymatic processes by carbamoylation of amino acids in proteins. Lomustine is cell-cycle nonspecific. It has also been used in veterinary practice as a treatment for mast cell tum ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N-Nitroso-N-methylurea
''N''-Nitroso-''N''-methylurea (NMU) is a highly reliable carcinogen, mutagen, and teratogen. NMU is an alkylating agent, and exhibits its toxicity by transferring its methyl group to nucleobases in nucleic acids, which can lead to AT:GC transition mutations. NMU is the traditional precursor in the synthesis of diazomethane. It has the potentially advantageous property that the stoichiometric byproducts formed are water, carbon dioxide, and ammonia, which are innocuous or easily removed. However, because it is unstable at temperatures beyond 20 °C and somewhat shock-sensitive, it has become obsolete for this purpose and replaced by other N-nitroso compounds: (''N''-methyl)nitrosamides and nitrosamines. Most chemical supply houses have stopped carrying it. Acute exposure to NMU in humans can result in skin and eye irritation, headache, nausea, and vomiting. [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Streptozocin
Streptozotocin or streptozocin (INN, USP) (STZ) is a naturally occurring alkylating antineoplastic agent that is particularly toxic to the insulin-producing beta cells of the pancreas in mammals. It is used in medicine for treating certain cancers of the islets of Langerhans and used in medical research to produce an animal model for hyperglycemia and Alzheimer's in a large dose, as well as type 2 diabetes or type 1 diabetes Type 1 diabetes (T1D), formerly known as juvenile diabetes, is an autoimmune disease that originates when cells that make insulin (beta cells) are destroyed by the immune system. Insulin is a hormone required for the cells to use blood sugar ... with multiple low doses. Usage Streptozotocin is approved by the U.S. Food and Drug Administration (FDA) for treating metastatic cancer of the Islets of Langerhans, pancreatic islet cells. Since it carries a substantial risk of toxicity and rarely cures the cancer, its use is generally limited to patients w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nimustine
Nimustine () is a nitrosourea alkylating agent Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion, or a carbene (or their equivalents). Alkylating agents are reagents for effectin .... It is used to treat malignant brain tumors and has proven to be rather effective. References Alkylating antineoplastic agents Nitrosamines Nitrosoureas[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ranimustine
Ranimustine (INN, marketed under the tradename Cymerin; also known as MCNU) is a nitrosourea alkylating agent approved in Japan for the treatment of chronic myelogenous leukemia and polycythemia vera. It has never been filed for FDA evaluation in the United States The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territori ..., where it is not marketed. References *Cymerin サイメリン(PDF) Mitsubishi Tanabe Pharma. October 2007. Alkylating antineoplastic agents Nitrosamines Nitrosoureas Ureas Chloroethyl compounds {{antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chlorozotocin
Chlorozotocin is a nitrosourea. It is used for cancer therapy. The International Agency for Research on Cancer concluded it was "probably carcinogenic" in 1990 It is an analogue of streptozotocin Streptozotocin or streptozocin ( INN, USP) (STZ) is a naturally occurring alkylating antineoplastic agent that is particularly toxic to the insulin-producing beta cells of the pancreas in mammals. It is used in medicine for treating certain can .... References Alkylating antineoplastic agents IARC Group 2A carcinogens Monosaccharide derivatives Nitrosoureas Chloroethyl compounds {{antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fotemustine
Fotemustine is a nitrosourea alkylating agent used in the treatment of metastatic melanoma. It is available in Europe but has not been approved by the United States FDA. A study has shown that fotemustine produces improved response rates and but does not increase survival (over dacarbazine Dacarbazine (DTIC), also known as imidazole carboxamide, is a chemotherapy medication used in the treatment of melanoma and Hodgkin's lymphoma. For Hodgkin's it is often used together with vinblastine, bleomycin, and doxorubicin. It is given ... in the treatment of disseminated cutaneous melanoma. Median survival was 7.3 months with fotemustine versus 5.6 months with DTIC (P=.067). There was also toxicity prevalence in fotemustine arm. The main toxicity was grade 3 to 4 neutropenia (51% with fotemustine v 5% with DTIC) and thrombocytopenia (43% v 6%, respectively). External links Alkylating antineoplastic agents Nitrosamines Nitrosoureas Organochlorides Phosphonate esters Urea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemotherapy
Chemotherapy (often abbreviated to chemo and sometimes CTX or CTx) is a type of cancer treatment that uses one or more anti-cancer drugs (chemotherapeutic agents or alkylating agents) as part of a standardized chemotherapy regimen. Chemotherapy may be given with a curative intent (which almost always involves combinations of drugs) or it may aim to prolong life or to reduce symptoms ( palliative chemotherapy). Chemotherapy is one of the major categories of the medical discipline specifically devoted to pharmacotherapy for cancer, which is called ''medical oncology''. The term ''chemotherapy'' has come to connote non-specific usage of intracellular poisons to inhibit mitosis (cell division) or induce DNA damage, which is why inhibition of DNA repair can augment chemotherapy. The connotation of the word chemotherapy excludes more selective agents that block extracellular signals (signal transduction). The development of therapies with specific molecular or genetic targets, wh ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
