Among various antitumor chemicals, alkylating agents are one of the earliest, most extensive and largest families of antitumor drugs. Since the application of nitrogen mustard in the treatment of malignant lymphoma in 1942, alkylating agents have become the most important class of drugs in cancer chemotherapy. The main common feature of these drugs is the cytotoxic component of the molecular structure, that is, the molecule contains an alkyl group, usually containing one or two alkyl groups, and is therefore referred to as a monofunctional or bifunctional alkylating agent, respectively. These alkyl groups can usually be converted into electron-deficient intermediates, which are related to the electronic groups (such as amino groups, sulfhydryl groups, hydroxyl groups, carboxylic acid groups, phosphate groups, etc.) contained in the biological macromolecules (DNA, RNA and protein) of the cells. Covalently combined, an alkylation reaction occurs, which causes these cellular components to lose their function in cell metabolism, thereby mutating the composition of the cells, affecting cell division, and causing cell death. Compared with other anti-tumor drugs, this class of drugs rarely produces drug resistance, including less cross-resistance between alkylating agents or between alkylating agents and non-alkylating agents, and to a lesser extent. Myelosuppression and gastrointestinal reactions are common side effects of this class of drugs. At present, the commonly used alkylating agent antitumor drugs can be divided into: nitrogen mustard and its derivatives (dichloroethylamine), ethyleneimine, methanesulfonate, nitrosourea, epoxide and others.
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Amino compound
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Oxy-containing amino compound
Cycloalkylamines, aromatic monoamines, aromatic polyamines and derivatives and salts thereof
Acyclic monoamines, polyamines and their derivatives and salts
Amide compound
Sulfonic acid amino compound
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Alcohols, phenols, phenolic compounds and derivatives
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2-cycloalcohol
Halogenated, sulfonated, nitrated or nitrosated derivatives of alcohols
Extremely halogenated, sulfonated, nitrated or nitrosated derivatives of phenols
Phenol and its halogenated, sulfonated, nitrated or nitrosated derivatives
Acyclic alcohol
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Nitrogen-containing compound
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Nitrile compound
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Organic derivative of hydrazine or hydrazine
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Terpenoid
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Ether compounds and their derivatives
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Ether, ether alcohol
Halogenation, sulfonation, nitration or nitrosation of ethers, ether alcohols, ether phenols
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Aldehyde
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Carboxylic compounds and derivatives
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Cyclic carboxylic acid
Halogenation, sulfonation, nitration or nitrosation of carboxylic acids
Halogenation, sulfonation, nitration or nitration of carboxylic anhydrides
Carboxylic acid halide
Carboxylic esters and their derivatives
Salt of carboxylic acid ester and its derivatives
Acyclic carboxylic acid
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Hydrocarbon compounds and their derivatives
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Aromatic hydrocarbon
Cyclic hydrocarbon
Hydrocarbon sulfonate
Hydrocarbon halide
Hydrocarbon nitrite
Acyclic hydrocarbon
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Ketone compound
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Alkyl ureas and their derivatives and salts
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Inorganic acid ester
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Heterocyclic compound
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Diazo, azo or azo compound
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Organosilicon compound
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Organometallic compound
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Organic palladium
Organic germanium, cobalt, strontium, barium, gallium, germanium, germanium, germanium, germanium, etc.
Organic calcium
Zirconium
Organic potassium
Organic
Organic lithium
Organic
Organic aluminum
Organotin
Organic manganese
Organic sodium
Organic nickel
Organic titanium
Organic iron
Organic copper
Organotin
Organic zinc
Organic
Organic
Organic germanium, mercury, silver, platinum, etc.
Organic germanium, antimony, bismuth, tungsten, antimony, bismuth, lead, vanadium, molybdenum, chromium, antimony, etc.
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Organic sulfur compound
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Organic phosphine compound
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Organometallic salt
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Organic fluorine compound
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Fluorobenzoic acid series
Fluorobenzonitrile series
Fluorobenzaldehyde series
Fluorobenzyl alcohol series
Fluoroanisole series
Fluoroaniline series
Fluorophenylacetic acid series
Fluorophenol series
Fluorobenzoic acid series
Fluoronitrobenzene series
Fluoropyridine series
Potassium fluoroborate series
Fluorobenzyl alcohol series
Fluorotoluene series
Fluorine red series
Fluoroethane series
Fluoropropane series