Carbendazim is a broad-spectrum benzimidazole antifungal with potential antimitotic and antineoplastic activities widely used as a fungicide in agriculture and home gardening, and as an antihelminthic in veterinary medicine. As a fungicide, carbendazim used for controls Ascomycetes, Fungi Imperfecti, and Basidiomycetes on a wide variety of crops, including bananas, cereals, cotton, fruits, grapes, mushrooms, ornamentals, peanuts, sugarbeet, soybeans, tobacco, and vegetables. Carbendazim is a chemically stable and relatively persistent fungicide which only metabolizes to a limited extent in plants and in soil. The only detected metabolite is 2-aminobenzimidazole, which constitutes less than 5% of the total residues in leaves. Carbendazim may be anticipated to metabolize in the animal into hydroxylated analogues which may appear in meat and milk products. Carbendazim acts as a mitotic poison by altering tubulin binding and microtubule formation. This has been proposed as a possible mechanism of action for the developmental abnormalities seen in animal studies with high concentrations.

Navuridine (AzddU) is a nucleoside analogue which demonstrated significant anti-HIV activity and low toxicity in preclinical studies. The drug was originally developed by University of Georgia. Navuridine is a dideoxyuridine inhibitor of HIV reverse transcriptase that is related to zidovudine. Navuridine exhibits a relatively short half-life and incomplete oral bioavailability and has not been developed into a clinical drug.

Mafosfamide is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. The effects of mafosfamide on various types of cancer cells were determined during preclinical investigations and clinical trials. Its development has been discontinued.

Mofarotene is an analog of retinoic acid patented by a Swiss multinational healthcare company Hoffmann-La Roche as neoplasm inhibitors and agent for treating dermatoses. Like other retinoic acid agents, mofarotene binds to and activates retinoic acid receptors (RARs), thereby altering the expression of certain genes leading to cell differentiation and decreased cell proliferation in susceptible cells. Mofarotene has demonstrated considerable antitumor activity in a number of cancer cell lines. Mofarotene in combination with cisplatin and etoposide was studied in phase I clinical trials but further development was discontinued.

Ortataxel (previously known as IDN 5109 or BAY59-8862), a second-generation taxane derivative that was developed as an antitumor agent. Ortataxel binds to and stabilizes tubulin molecules, thereby interfering with the dynamics of microtubule assembly/disassembly. This results in the inhibition of cell division and cellular proliferation. In addition, ortataxel modulates multi-drug resistance mechanisms and may be useful for treating multi-drug resistant tumors that express Pgp, MRP-1, and BCRP. This drug participated in phase II clinical trials in patients with advanced renal cell carcinoma and in patients with Non-Hodgkin's lymphoma. However, these studies were discontinued. Ortataxel was also involved in phase II clinical trials for patients with glioblastoma; however, in a limited number of patients, the drug produced a benefit that lasted for a long time. Besides, ortataxel successfully completed phase II trials in taxane-resistant metastatic breast cancer patients and in taxane-resistant non-small cell lung cancer patients.

Cytochlor is a radio-sensitizing pyrimidine nucleoside with potential antineoplastic activity. Cytochlor is metabolized first to a phosphate derivative, CldCMP, by the enzyme deoxycytidine kinase and then to the active uracyl derivative, CldUMP, by the enzyme dCMP deaminase. CldUMP, the active metabolite, incorporates into DNA and, upon exposure to radiation, induces the formation of uracil radicals and double-strand DNA breaks. Cytochlor has been used in trials studying the treatment of Head and Neck Cancer and Brain and Central Nervous System Tumors.

Epothilone D (KOS-862 or BMS-241027) is an intermediary obtained in the synthesis of members of the epothilone family and is a small-molecule microtubule stabilizer. It was investigated in Phase II trials in colorectal, metastatic breast and non-small-cell lung cancers. However, development was discontinued in 2007 in favor of a second-generation analog with a better safety profile. This drug also was studied for the treatment of Alzheimer's disease. The study ended in October 2013, and evaluation of epothilone D for Alzheimer's disease was subsequently discontinued. The mechanism by which epothilones induce microtubule polymerization appears to be similar to that of paclitaxel, in that epothilones compete with paclitaxel for binding to microtubules and suppress microtubule dynamics in a manner similar to that of paclitaxel.

Datelliptium is a DNA-intercalating agent, an analog of a natural alkaloid ellipticine. The compound was active in vivo against a variety of murine solid tumors. In a phase I clinical trial no objective complete or partial responses were observed in patients with solid tumors or lymphoma treated with datelliptium.

Ecomustine, or CY233 (NSC-609224), is a water-soluble nitrosoureido derivative of deoxysugar exerting antineoplastic activity. It acts as an alkylating agent. It demonstrated effectivity in the treatment of tumors in animal models.

Rodorubicin (Cytorhodin S, HLB 817) is a synthetic tetraglycosidic anthracycline antibiotic with antineoplastic activity. Rodorubicin is thought to intercalate DNA and cause cell death. Compared to standard anthracyclines, this compound has an atypical spectrum of activity and toxicity. Rodorubucin was the first drug that was being developed clinically despite its inactivity in animal transplantation tumor systems (it was detected in a human tumor-based screening system). Delayed nephrotoxicity is the dose-limiting factor for this drug, namely proteinuria and clearance reduction. Because of the severe side effects, rodobubicin was never marketed.