DNA alkylator/crosslinker is a molecule that alkylates DNA or can cross link with DNA. DNA alkylator/crosslinker can have mutagenic, pharmaceutical, or other effects. 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. Alkylating agents are widely used in chemistry because the alkyl group is probably the most common group encountered in organic molecules. Selective alkylation, or adding parts to the chain with the desired functional groups, is used, especially if there is no commonly available biological precursor. Alkylation with only one carbon is termed methylation. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Crosslinking of DNA occurs when various exogenous or endogenous agents react with two different positions in the DNA. This can either occur in the same strand (intrastrand crosslink) or in the opposite strands of the DNA (interstrand crosslink). Crosslinks also occur between DNA and protein. DNA replication is blocked by crosslinks, which causes replication arrest and cell death if the crosslink is not repaired. The RAD51 family plays a role in repair.
||Thio-TEPA is a DNA alkylating agent, with antitumor activity.
||Bendamustine (SDX-105) HCl
||Bendamustine Hcl(SDX105; EP-3101) is a DNA-damaging agent with IC50 of 50 μM.
||Melphalan is an effective DNA alkylating agent, with antitumor activity.
||Ifosfamide is a nitrogen mustard alkylating agent used in the treatment of cancer.
||Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.
||Chlorambucil is an alkylating agent with antitumor activity.
||Altretamine (RB-1515, WR-95704)
||Altretamine is an alkylating antineoplastic agent.
||Satraplatin is an alkylating agent, with potent antitumor effect.
||Miriplatin is a chemotherapy agent which belongs to the class of alkylating agents.
||Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA.
||VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.
||SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA; with potent antitumor activity.
||Miriplatin hydrate is a chemotherapy agent which belongs to the class of alkylating agents.
||Altretamine (RB-1515, WR-95704) HCl
||Altretamine hydrochloride is an alkylating antineoplastic agent.
||Treosulfan is an alkylating agent with activity in ovarian cancer and other solid tumor types.
||Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.
||Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities.
||Uramustine is an oral alkylating agent, effective in the treatment of lymphosarcoma, chronic lymphatic leukaemia, and thrombocythemia.
|| Mitomycin C is a DNA-damaging agent and small-molecule inhibitor effectively sensitize cancer cells to tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL).