Chromomycin A3 is an anticancer antibiotic, inhibits DNA synthesis by inhibiting DNA gyrase. The antibiotic has potential reactive centers that could interact with GSH, the most abundant non-protein thiol in eukaryotic cells and a putative cofactor involved in the activation of many antibiotics in vivo. It was found, that chromomycin A3 may be potential drug leads for tumor necrosis factor (TNF)-related apoptosis-inducing ligand, TRAIL-resistant and Wnt signal-related diseases and will be useful chemical tools for use in investigating TRAIL and the Wnt signaling pathway.

Acronine is an acridone alkaloid isolated from the bark of Acronychia bauri Schott, scrub ash indigenous to Australia. It possesses broad-spectrum activity against experimental neoplasms. Acronine has been studied in the treatment of multiple myeloma. Acronine analogues also possess cytotoxic and antitumor activity.

Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects. Although its mechanism of action is incompletely defined, amsacrine inhibits DNA synthesis by binding to and intercalating with DNA. Amsacrine also inhibits topoisomerase II activity and may exert an effect on cell membranes. This agent also possesses immunosuppressive and antiviral properties. While amsacrine is not cell cycle phase-specific, cytotoxicity is maximal during the G2 and S phases.

Aclarubicin (INN) or aclacinomycin A is an anthracycline drug is primarily indicated in conditions like Acute non-lymphoblastic leukemia, Breast cancer, Gastric cancer, Lymphoma, Ovarian coma, Small cell lung cancer, Thyroid cancer. Soil bacteria Streptomyces galilaeus can produce aclarubicin. Aclarubicin (HCl) is used in combination with different anticancerous drugs to obtain best therapeutic results and to reduce toxicity or side effects. Aclarubicin (HCl) is administered intravenously. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin.

Bleomycin sulfate is an antineoplastic antibiotic isolated from Streptomyces verticillus. It is a mixture of glycopeptide antibiotics containing primarily Bleomycin A2 (~70%) and B2 (~30%). Bleomycin binds to DNA, inhibits DNA synthesis, and causes single strand scission of DNA in vivo and in vitro at specific base sequences.

Olivomycin is an antitumor glycoside antibiotic that binds to DNA. This drug is used to treat testicular neoplasms, tonsillar tumors and reticulosarcoma with peripheral nodes. In addition, olivomycin was studied for the diagnosis of ureaplasma infection of the sperm.

Actinomycin C is an antibiotic complex composed of actinomycin C1, C2 and C3 and produced by Streptomyces chrysomallus. Actinomycin C reversibly binds to DNA, interfering with the synthesis of RNA, prevention of RNA polymerase elongation and, consequently, with protein synthesis. Actinomycin C exert an inhibitory effect on gram-positive and gram-negative bacteria and on some fungi. However, the toxic properties of the Actinomycin C in relation to antibacterial activity is such as to preclude its use as antibiotics in the treatment of infectious diseases. Because Actinomycin C is cytotoxic, it has an antineoplastic effect which has been demonstrated in experimental animals with various types of tumor implant. This cytotoxic action is the basis for its use in the treatment of certain types of cancer.

Epirubicin is an anthracycline cytotoxic agent, is a 4'-epi-isomer of doxorubicin. The compound is marketed by Pfizer under the trade name Ellence in the US. It is indicated as a component of adjuvant therapy in patients with evidence of axillary node tumor involvement following resection of primary breast cancer. Although it is known that anthracyclines can interfere with a number of biochemical and biological functions within eukaryotic cells, the precise mechanisms of epirubicin’s cytotoxic and/or antiproliferative properties have not been completely elucidated. It is known, that epirubicin forms a complex with DNA by intercalation of its planar rings between nucleotide base pairs, with consequent inhibition of nucleic acid (DNA and RNA) and protein synthesis. Such intercalation triggers DNA cleavage by topoisomerase II, resulting in cytocidal activity. Epirubicin also inhibits DNA helicase activity, preventing the enzymatic separation of double-stranded DNA and interfering with replication and transcription. Epirubicin is also involved in oxidation/reduction reactions by generating cytotoxic free radicals.

Idarubicin is an antineoplastic in the anthracycline class.Idarubicin hydrochloride is a DNA-intercalating analog of daunorubicin which has an inhibitory effect on nucleic acid synthesis and interacts with the enzyme topoisomerase II. The absence of a methoxy group at position 4 of the anthracycline structure gives the compound a high lipophilicity which results in an increased rate of cellular uptake compared with other anthracyclines.Idarubicin possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. Idarubicin in combination with other approved antileukemic drugs is indicated for the treatment of acute myeloid leukemia (AML) in adults.