DNA alkylator

DNA alkylators are a class of compounds that can add alkyl groups (e.g., methyl or ethyl groups) to the DNA molecule, leading to DNA damage. This modification can result in mispairing or prevention of DNA replication, which can lead to cell death. Given their ability to damage DNA, alkylating agents are used as chemotherapy drugs to treat various cancers. However, their use can also be associated with significant side effects, as they can damage normal cells in addition to cancer cells. Popular examples of alkylating agents include cyclophosphamide, melphalan, and busulfan.


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  1. Altretamine is classified as an alkylating antineoplastic agent.This unique structure is believed to damage tumor cells through the production of the weakly alkylating species formaldehyde, a product of CYP450-mediated N-demethylation.
  2. Bendamustine Hydrochloride is a small molecule bifunctional DNA alkylating agent, combining a nitrogen mustard functionality with a purine-analog structure. The dense DNA-damaging functionality of Bendamustine differentiates it from other compounds used as antiproliferative agents, and these functionalities are thought to promote cell death through a variety of different pathways including apoptosis and mitotic catastrophe.

  3. Thiotepa is a polyfunctional, organophosphorus alkylating agent and a stable derivative of N,N',N''-triethylenephosphoramide (TEPA), with antineoplastic activity.
  4. Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.
  5. Cyclophosphamide monohydrate is an alkylating, cytotoxic agent experimentally shown to crosslink DNA, causing strand breakage and inducing mutations.
  6. Uramustine is a chemotherapy drug which belongs to the class of alkylating agents.
  7. DNA alkylating agent

    Melphalan is a cytotoxic drug used to treat multiple myeloma. Phenylamine derivative of mechorethamine.
  8. DNA/RNA Alkylator

    Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA.
  9. Nimustine hydrochloride is an antineoplastic agent especially effective against malignant brain tumors. The resistance which brain tumor cells acquire to the initial effectiveness of this drug can be partially overcome by the simultaneous use of membrane-modifying agents such as reserpine, calcium antagonists such as nicardipine or verapamil, or the calmodulin inhibitor, trifluoperazine.
  10. Treosulfan (NSC 39069;Treosulphan) is an alkylating agent with activity in ovarian cancer and other solid tumor types.
  11. Methylnitronitrosoguanidine (MNNG) is an alkylating agent with toxic and mutagenic effects.
  12. DNA alkylator

    Semustine is a DNA alkylator, binds to DNA, and acts as a cancer chemotherapeutic agent.

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