SG3199 is a PBD dimer which binds in the minor groove of DNA, and forms covalent DNA interstrand cross-links in naked linear plasmid DNA. SG3199 is potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines.
Yoshi-864 alkylates and cross-linksDNA, thereby inhibiting DNA replication. It is an alkyl sulfonate DNAcross-linking agent with potential anti-cancer activity.
PR-104 is a highly specific hypoxia-activated agent that cross-linksDNA, enabling its application in various tumor xenograft models. Functioning as a pre-prodrug of nitrogen mustard, PR-104 undergoes efficient conversion to the dinitrobenzamide mustards alcohol form, known as PR-104A[1].
Anticancer agent 11 an effective broad-spectrum anticancer agent, exerts its therapeutic potential by suppressing angiogenesis and facilitating the formation of DNAcross-links.
Bisantrene (CL-216942; NSC 337766) is a topoisomerase II poison and DNA intercalator. It can be used as a Rac1 inhibitor or model compound to study P-glycoprotein-mediated multi-drug resistance (MDR1). Bisantrene inserts and disrupts the configuration of
Mafosfamide is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide alkylates DNA, forming DNAcross-links and inhibiting DNA synthesis. Although closely related to cyclophosphamide, mafosfamide, unlike cyclophosphamide, does not require hepatic activation to generate its active metabolite 4-hydroxy-cyclophosphamide; accordingly, mafosfamide is potentially useful in the intrathecal treatment of neoplastic meningitis.
Mafosfamide sodium is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide sodium alkylates DNA, forming DNAcross-links and inhibiting DNA synthesis. Although closely related to cyclophosphamide, Mafosfamide sodium, unlike cyclophosphamide, does not require hepatic activation to generate its active metabolite 4-hydroxy-cyclophosphamide; accordingly, Mafosfamide sodium is potentially useful in the intrathecal treatment of neoplastic meningitis.
Porfiromycin is a n N-methyl derivative of the antineoplastic antibiotic mitomycin C isolated from the bacterium Streptomyces ardus and other Streptomyces bacterial species. Bioreduced porfiromycin generates oxygen radicals and alkylates DNA, producing interstrand cross-links and single-strand breaks, thereby inhibiting DNA synthesis. Porfiromycin is preferentially toxic to hypoxic cells.
Caricotamide is a synthetic co-substrate that activates the human endogenous enzyme NRH:quinone oxidoreductase 2 (NQO2) with potential chemoadjuvant activity. When caricotamide is administered simultaneously with the prodrug tretazicar, NQO2 converts tretazicar to the bifunctional alkylating agent dinitrobenzamide, which is capable of forming a high degree of DNA interstrand cross-links, resulting in the inhibition of DNA replication and the induction of apoptosis. NQO2 has been found to be over-expressed in cancers such as hepatocellular carcinoma (HCC), colorectal and ovarian cancers.
Teroxirone, also known as Triglycidyl Isocyanurate and Tris(2,3-epoxypropyl) Isocyanurate, is a triazene triepoxide with antineoplastic activity. Teroxine alkylates and cross-linksDNA, thereby inhibiting DNA replication.
TriN2755 is a synthetic triazene derivative with antineoplastic activity. Upon metabolic activation via N-demethylation, TriN2755 is converted into highly reactive carbocations that can alkylate DNA and other macromolecules, thereby resulting in DNAcrosslinks, inhibiting DNA replication and repair, and subsequently inducing apoptosis. This agent has high hydrophilicity and photostability and shows a favorable toxicity profile over the other triazenes.