Glyhexamide (SQ 15,860) is a sulfonylurea with antihyperglycemic activity. Its hypoglycemic effect was first observed in rats, dogs and rabbits when orally administered, in 1965. This hypogelycemic activity was however not accompanied by increases in serum (immunoreactive) insulin concentrations.

Cyanamide is an organic compound with the formula CN2H2. It is used in agriculture as a plant growth regulator to break bud dormancy and stimulate more uniform and earlier bud break. Cyanamide is an inhibitor of alcohol dehydrogenase. Administration of citrated calcium cyanamide sensitizes individuals to the action of alcohol and is used for the treatment of chronic alcoholism.

Quingestrone is a progestin, or a synthetic progestogen, patented by Laboratoires francais de chimiotherapie as an anti-inflammatory agent. Quingestrone acts as an agonist of the progesterone receptor weak glucocorticoid activity. Quingestrone was formerly used in combination with ethinylestradiol or mestranol in combined birth control pills in Italy. The medication was studied in the clinical prevention of miscarriage during pregnancy, but insufficient efficacy was observed at the dosage assessed

Zearalenone (ZEN) is a toxic non-steroidal mycoestrogen produced by fungi that widely contaminate agricultural products, eliciting estrogenic responses by mimicking sex steroid hormones. Zearalenone is biosynthesised through a polyketide pathway by a variety of Fusarium fungi including Fusarium graminearum (Gibberella zeae), Fusarium culmorum, Fusarium equiseti, Fusarium crookwellense, Fusarium cerealis and Fusarium semitectum. Zearalenone and its derivatives share similar molecular mechanisms and activity with estrogens. They interact with the estrogen receptors (ERa and ERb) leading to functional and morphological changes in the reproductive system in both animals and humans. Zearalenone exposure is associated with the estrogenic syndrome and infertility in animals and premature thelarche and precocious puberty in girls. In animal models, it was found that prepubertal exposure to a low dose of Zearalenone, decreased breast cancer risk. When prepubertal rats were treated with 20 lg (1 mg ⁄ kg body weight) of Zearalenone, a significant reduction of both the incidence and multiplicity of DMBA-induced mammary tumours was noted. Zearalenone has been used to treat postmenopausal symptoms in women.

PGD2 (Prostaglandin D2) is a major cellular regulator, has been shown to bind different receptors: D prostanoid receptor (DP) and chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). PGD2 reportedly inhibits platelet aggregation, the proliferation of cells, and activation of neutrophils. This compound is also a potent vasodilator that also relaxes smooth muscle but causes contraction of the bronchial airways. PGD2 promotes T cell migration via CRTH2 and aggravates asthma. In contrast, there have been some studies suggesting that PGD2 exerts anti-inflammatory effects via DP, such as inhibiting the migration and activation of neutrophils, basophils, dendritic cells and T cells. Elevated levels of prostaglandin D2 (PGD2) have been shown to be present in the bald scalp of androgenic alopecia (AGA) patients and was suggested the PGD(2)-GPR44 pathway as a potential target for treatment. Also was revealed, that PGD2 might be a new target for asthma therapy, PGD2 in serum and BALF were lower in the treated group than in the untreated group.

Cocculine is an alkaloid found in the leaves of Cocculus laurifolius, the laurel-leaved snail tree. Cocculine has hypotensive and ganglion blocking properties.

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.