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Toxicity of the Alkylating Agent Bendamustin [PDF]
, 1985 In acute toxicity studies the maximum tolerated dose (MTD), the LD50 and the LD100 of Bendamustin were determined in rats and mice after i.v. and oral administration. In a subchronic study male rats were given Bendamustin for 28 days at oral dose levels of 5, 10, 20 or 40 mg/kg/day.
Härtl A, Horn U, Güttner J, Hoffmann H
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Aldehydes as Alkylating Agents for Ketones
Chemistry – A European Journal, 2019AbstractCommon and non‐toxic aldehydes are proposed as reagents for alkylation of ketones instead of carcinogenic alkyl halides. The developed reductive alkylation reaction proceeds in the presence of the commercially available ruthenium catalyst [(cymene)RuCl2]2(as low as 250 ppm) and carbon monoxide as the reducing agent.
Sofiya A. Runikhina +7 more
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Hybrid ligand-alkylating agents targeting telomeric G-quadruplex structures.
Organic and biomolecular chemistry, 2012The synthesis, physico-chemical properties and biological effects of a new class of naphthalene diimides (NDIs) capable of reversibly binding telomeric DNA and alkylate it through an electrophilic quinone methide moiety (QM), are reported.
F. Doria +11 more
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Mechanisms of Resistance to Alkylating Agents
1996A major problem in cancer chemotherapy is the frequently encountered rapid loss in responsiveness to therapeutic agents [1]. Drug resistance can be the result of the induction of a variety of protective mechanisms or the result of the selection of resistant clones.
Philip G. Penketh +2 more
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Chemosensitization by monofunctional alkylating agents
International Journal of Radiation Oncology*Biology*Physics, 1986The chemosensitizing ability of model monofunctional alkylating agents with known DNA base alkylating characteristics, that is, methylmethanesulphonate (MMS), ethyl methanesulphonate (EMS) and N-methyl-N-nitrosoguanidine (MNNG) have been investigated. Whereas the alkyl sulphonates chemosensitize V79 cells to cisplatin and melphalan, MNNG does not.
J.M. Walling, Ian J. Stratford
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Mechanisms of resistance to alkylating agents
1998Alkylating agents are the most widely used anticancer drugs whose main target is the DNA, although how exactly the DNA lesions cause cell death is still not clear. The emergence of resistance to this class of drugs as well as to other antitumor agents is one of the major causes of failure of cancer treatment.
Maurizio D'Incalci, Giovanna Damia
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Vestibulotoxic Effect of Alkylating Agents
ORL, 1977The vestibular sensory epithelia from 3 patients treated with cytotoxic drugs were studied with a surface specimen technique, 2 cases had been treated with cyclophosphamide and 1 with melphalan. In all 3 cases there was some slight degeneration affecting the cristae ampullares. The macula utriculi showed no signs of degeneration.
Ulf Rosenhall, Harald Nyman, Jan Stahle
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Photogeneration and reactivity of naphthoquinone methides as purine selective DNA alkylating agents.
Journal of the American Chemical Society, 2010A one-step protecting-group-free synthesis of both 6-hydroxy-naphthalene-2-carbaldehyde and the bifunctional binaphthalenyl derivative afforded 6-hydroxymethylnaphthalen-2-ol, 6-methylaminomethyl-naphthalen-2-ol, [(2-hydroxy-3-naphthyl)methyl]trimethyl ...
D. Verga +7 more
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Alkylating agents: Mechanisms and modulation
1989The term alkylating agents encompasses a wide range of compounds that are capable of covalently modifying a variety of intracellular targets. The mechanism(s) by which alkylating agents kill human tumor cells has not been completely characterized and is therefore not fully understood.
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Mechanisms of resistance to alkylating agents
1994The alkylating agents produce cytotoxicity by chemically reacting with cellular components that contain electron-rich nitrogen, sulfur, or oxygen atoms. A multitude of cellular constituents, including amino acids, nucleotides, proteins, nucleic acids, and cell membranes are alkylated by the therapeutic alkylating agents.
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