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Cortifen
Cortifen, also known as cortiphen or kortifen, as well as fencoron, is a synthetic glucocorticoid corticosteroid and cytostatic antineoplastic agent which was developed in Russia for potential treatment of tumors. It is a hydrophobic chlor phenacyl nitrogen mustard ester of 11-deoxycortisol (cortodoxone). See also * List of hormonal cytostatic antineoplastic agents * List of corticosteroid esters This is a list of corticosteroid esters, including esters of steroidal glucocorticoids and mineralocorticoids. Esters of natural corticosteroids Desoxycortone esters * Desoxycortone acetate (deoxycortone acetate; desoxycorticosterone aceta ... References Acetate esters Tertiary alcohols Amines Corticosteroid esters Glucocorticoids Ketones Mineralocorticoids Nitrogen mustards Organochlorides Prodrugs Russian drugs Chloroethyl compounds {{Antineoplastic-drug-stub ...
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List Of Corticosteroid Esters
This is a list of corticosteroid esters, including esters of steroidal glucocorticoids and mineralocorticoids. Esters of natural corticosteroids Desoxycortone esters * Desoxycortone acetate (deoxycortone acetate; desoxycorticosterone acetate) * Desoxycortone cypionate (deoxycortone cypionate; desoxycorticosterone cypionate) * Desoxycortone enanthate (deoxycortone enanthate; deoxycorticosterone enanthate) * Desoxycortone glucoside (deoxycortone glucoside; deoxycorticosterone glucoside) * Desoxycortone pivalate (deoxycortone pivalate; deoxycorticosterone pivalate) Hydrocortisone esters * Benzodrocortisone (hydrocortisone 17-benzoate) * Hydrocortamate (hydrocortisone 21-(diethylamino)acetate) * Hydrocortisone aceponate (hydrocortisone 21-acetate 17α-propionate) * Hydrocortisone acetate * Hydrocortisone bendazac * Hydrocortisone buteprate (hydrocortisone 17α-butyrate 21-propionate) * Hydrocortisone butyrate (hydrocortisone 17α-butyrate) * Hydrocortisone 21-butyrat ...
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Corticosteroid Esters
This is a list of corticosteroid esters, including esters of steroidal glucocorticoids and mineralocorticoids. Esters of natural corticosteroids Desoxycortone esters * Desoxycortone acetate (deoxycortone acetate; desoxycorticosterone acetate) * Desoxycortone cypionate (deoxycortone cypionate; desoxycorticosterone cypionate) * Desoxycortone enanthate (deoxycortone enanthate; deoxycorticosterone enanthate) * Desoxycortone glucoside (deoxycortone glucoside; deoxycorticosterone glucoside) * Desoxycortone pivalate (deoxycortone pivalate; deoxycorticosterone pivalate) Hydrocortisone esters * Benzodrocortisone (hydrocortisone 17-benzoate) * Hydrocortamate (hydrocortisone 21-(diethylamino)acetate) * Hydrocortisone aceponate (hydrocortisone 21-acetate 17α-propionate) * Hydrocortisone acetate * Hydrocortisone bendazac * Hydrocortisone buteprate (hydrocortisone 17α-butyrate 21-propionate) * Hydrocortisone butyrate (hydrocortisone 17α-butyrate) * Hydrocortisone 21-butyrat ...
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List Of Hormonal Cytostatic Antineoplastic Agents
This is a list of dual hormonal antineoplastic agent, hormonal and cytostatic antineoplastic agents. Marketed Estrogen-based * Estramustine phosphate (Emcyt, Estracyt; Leo 299, NSC-89199, Ro 21-8837/001; estradiol 3-[bis(2-chloroethyl)carbamate] dihydrogen phosphate) Corticosteroid-based * Prednimustine (Mostarina, Sterecyst; chlorambucil prednisolone ester; prednisolone 21-(4-(4-(bis(2-chloroethyl)amino)phenyl)butanoate)) Never marketed Estrogen-based * Alestramustine (estradiol 3-(bis(2-chloroethyl)carbamate) 17β-(L-alaninate)) * Atrimustine (bestrabucil, busramustine; KM-2210; estradiol 3-benzoate 17β-((4-(4-(bis(2-chloroethyl)amino)phenyl)-1-oxobutoxy)acetate) * Cytestrol acetate (1α-hydroxyethinylestradiol 3-(bis(2-chloroethyl)carbamate) 11α,17β-diacetate) * Estradiol mustard (NSC-112259; chlorphenacyl estradiol diester; estradiol 3,17β-bis(4-(bis(2-chloroethyl)amino)phenyl)acetate) * Estramustine (Leo 275, Ro 21–8837; estradiol 3-(bis(2-chloroethyl)carbamate) est ...
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Cytostatic Antineoplastic Agent
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, whic ...
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11-deoxycortisol
11-Deoxycortisol, also known as cortodoxone (INN), cortexolone as well as 17α,21-dihydroxyprogesterone or 17α,21-dihydroxypregn-4-ene-3,20-dione, is an endogenous glucocorticoid steroid hormone, and a metabolic intermediate towards cortisol. It was first described by Tadeusz Reichstein in 1938 as Substance S, thus has also been referred to as Reichstein's Substance S or Compound S. Function 11-Deoxycortisol acts as a glucocorticoid, though is less potent than cortisol. 11-Deoxycortisol is synthesized from 17α-hydroxyprogesterone by 21-hydroxylase and is converted to cortisol by 11β-hydroxylase. 11-Deoxycortisol in mammals has limited biological activity and mainly acts as metabolic intermediate within the glucocorticoid pathway, leading to cortisol. In sea lamprey, a member of the agnathans that evolved more than 500 million years ago, 11-deoxycortisol is the major and final glucocorticoid, with mineralocorticoid activity. 11-deoxycortisol also takes part, by binding t ...
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Prodrugs
A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects. History Many herbal extracts historically used in medicine contain glycosides (sugar derivatives) of the active agent, which are hydrolyzed in the intestines to release the active and more bioavailable aglycone. For example, salicin is a β-D-glucopyranosid ...
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Organochlorides
An organochloride, organochlorine compound, chlorocarbon, or chlorinated hydrocarbon is an organic compound containing at least one covalently bonded atom of chlorine. The chloroalkane class (alkanes with one or more hydrogens substituted by chlorine) provides common examples. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious. Physical and chemical properties Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage. Natural occurrence Many organochlorine compounds have been isolate ...
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Nitrogen Mustards
Nitrogen mustards are cytotoxic organic compounds with the chloroethylamine (Cl(CH2)2NR2) functional group. Although originally produced as chemical warfare agents, they were the first chemotherapeutic agents for treatment of cancer. Nitrogen mustards are nonspecific DNA alkylating agents. Chemical warfare During World War II nitrogen mustards were studied at the Yale School of Medicine by Alfred Gilman and Louis Goodman, and classified human clinical trials of nitrogen mustards for the treatment of lymphoma started in December 1942. Also during World War II, an incident during the air raid on Bari, Italy, led to the release of mustard gas that affected several hundred soldiers and civilians. Medical examination of the survivors showed a decreased number of lymphocytes. After World War II was over, the Bari incident and the Yale group's studies eventually converged prompting a search for other similar compounds. Due to its use in previous studies, the nitrogen mustard known ...
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Mineralocorticoids
Mineralocorticoids are a class of corticosteroids, which in turn are a class of steroid hormones. Mineralocorticoids are produced in the adrenal cortex and influence salt and water balances (electrolyte balance and fluid balance). The primary mineralocorticoid is aldosterone. Physiology The name mineralocorticoid derives from early observations that these hormones were involved in the retention of sodium, a mineral. The primary endogenous mineralocorticoid is aldosterone, although a number of other endogenous hormones (including progesterone and deoxycorticosterone) have mineralocorticoid function. Aldosterone acts on the kidneys to provide active reabsorption of sodium and an associated passive reabsorption of water, as well as the active secretion of potassium in the principal cells of the cortical collecting tubule and active secretion of protons via proton ATPases in the lumenal membrane of the intercalated cells of the collecting tubule. This in turn results in an increase ...
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Ketones
In organic chemistry, a ketone is a functional group with the structure R–C(=O)–R', where R and R' can be a variety of carbon-containing substituents. Ketones contain a carbonyl group –C(=O)– (which contains a carbon-oxygen double bond C=O). The simplest ketone is acetone (where R and R' is methyl), with the formula . Many ketones are of great importance in biology and in industry. Examples include many sugars (ketoses), many steroids (e.g., testosterone), and the solvent acetone. Nomenclature and etymology The word ''ketone'' is derived from ''Aketon'', an old German word for ''acetone''. According to the rules of IUPAC nomenclature, ketone names are derived by changing the suffix ''-ane'' of the parent alkane to ''-anone''. Typically, the position of the carbonyl group is denoted by a number, but traditional nonsystematic names are still generally used for the most important ketones, for example acetone and benzophenone. These nonsystematic names are considered ret ...
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Glucocorticoids
Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The name "glucocorticoid" is a portmanteau (glucose + cortex + steroid) and is composed from its role in regulation of glucose metabolism, synthesis in the adrenal cortex, and its steroidal structure (see structure below). Glucocorticoids are part of the feedback mechanism in the immune system, which reduces certain aspects of immune function, such as inflammation. They are therefore used in medicine to treat diseases caused by an overactive immune system, such as allergies, asthma, autoimmune diseases, and sepsis. Glucocorticoids have many diverse (pleiotropic) effects, including potentially harmful side effects. They also interfere with some of the abnormal mechanisms in cancer cells, so they are used in high doses to tr ...
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Amines
In chemistry, amines (, ) are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines). Important amines include amino acids, biogenic amines, trimethylamine, and aniline; Inorganic derivatives of ammonia are also called amines, such as monochloramine (). The substituent is called an amino group. Compounds with a nitrogen atom attached to a carbonyl group, thus having the structure , are called amides and have different chemical properties from amines. Classification of amines Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic ...
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