Nifurmerone, a 5-nitrofuran derivative, is an antifungal agent.

BI-2536, an inhibitor of Polo-like kinase 1 (Plk-1) was being investigated by Boehringer Ingelheim as a possible treatment for cancer. BI-2536 inhibits Plk1 enzyme activity at low nanomolar concentrations. The compound potently causes a mitotic arrest and induces apoptosis in human cancer cell lines of diverse tissue origin and oncogenome signature. BI-2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens. In treated tumors, cells arrest in prometaphase, accumulate phosphohistone H3, and contain aberrant mitotic spindles. This mitotic arrest is followed by a surge in apoptosis, detectable by immunohistochemistry and noninvasive optical and magnetic resonance imaging. For addressing the therapeutic potential of Plk1 inhibition, BI-2536 has progressed into clinical studies in patients with locally advanced or metastatic cancers. It underwent phase II clinical studies for the treatment of breast cancer; non-small cell lung cancer; pancreatic cancer; prostate cancer; small cell lung cancer, but these studies were discontinued later.

Lifibrate is the antihyperlipidemic agent. It is a potent hepatic peroxisome proliferator. Administration of lifibrate at a dietary concentration of 0.15% for 3 weeks, increased the activity of catalase in both liver and kidney of male wild type (Cs-a strain) mice. The hypolipidemic activity of lifibrate is eight to nine times greater than that of chlorphenoxy isobutyric acid ethyl ester in the male Wistar rat.

Nisobamate is a tranquilizer, sedative and hypnotic.

Harmine (aka telepathine) is a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds. It is a naturally occurring metabolite in a number of plants, notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi. Harmine is a reversible inhibitor of monoamine oxidase A (MAO-A), but not MAO-B. Harmine has been found to have potential anti-cancer and neuroprotective properties, and also promotes differentiation of osteoblasts and chondrocytes while inhibiting osteoclastogenesis. Harmine has also been used as a C-11 labeled probe in positron emission tomography.

Oxotremorine, a metabolite of tremorine, is a non-hydrolyzed muscarinic acetylcholine receptor agonist used as a research tool. This compound is a muscarinic agent equal in potency to acetylcholine, but completely lacking in nicotinic activity.

Gloximonam (SQ-82531) is a beta-lactam antibiotic. This is a class of antibiotics that contains a beta-lactam ring in their molecular structure, such as penicillin derivatives. Gloximonam is orally absorbed and has shown anti-bacterial activity against different bacteria of the Enterobacteriaceae and Haemophilus influenzae families. Gloximonam is not effective against staphylococci and strict anaerobes (like aztreonam) and (unlike aztreonam) against Pseudomonas aeruginosa.

Torbafylline is a xanthine derivative. Torbafylline significantly ameliorated the decreased skeletal muscle blood flow, red cell flux and surface pO2 after acute occlusion of the femoral artery, with more pronounced effects on the microcirculatory parameters, the laser-Doppler flux and pO2. Torbafylline treatment caused an increased lactate dehydrogenase activity in intact fast muscles and decreased it in soleus. Torbafylline decreased the activity of citrate synthase but increased activity of 3-hydroxyacyl-CoA dehydrogenase in soleus. Torbafylline is a powerful inhibitor of muscle wasting that blocks enhanced Ub-proteasome-dependent proteolysis in situations where TNF production rises, including cancer and sepsis. Torbafylline suppresses malaria antigen or LPS-induced secretion of TNF-a and IL-1a secretion, but not of IL-6 from human mononuclear cells in vitro. Torbafylline also blocks TNF-a and IL-1a secretion by malaria parasite preparations indicating that it may be useful in the treatment of malaria. Torbafylline has a protective effect on antigen-induced bronchoconstriction in guinea pigs and may be a useful agent in the therapy of bronchial asthma. Torbafylline had been in phase II clinical trial for the treatment of peripheral arterial occlusive disorders. However, this development was discontinued.