Betulinic acid (BA) is a plant-derived pentacyclic triterpenoid that exerts potent anti-cancer effects in vitro and in vivo. It`s anticancer property is linked to its ability to induce apoptotic cell death in cancer cells by triggering the mitochondrial pathway of apoptosis. In contrast to the cytotoxicity of betulinic acid against a variety of cancer types, normal cells and tissue are relatively resistant to betulinic acid, pointing to a therapeutic window. Compounds that exert a direct action on mitochondria present promising experimental cancer therapeutics, since they may trigger cell death under circumstances in which standard chemotherapeutics fail. Thus, mitochondrion-targeted agents such as betulinic acid hold great promise as a novel therapeutic strategy in the treatment of human cancers. Betulinic acid has antiretroviral, antimalarial, and anti-inflammatory properties. Betulinic acid exerts its inhibitory effect by preventing topoisomerase I-DNA interaction as a result of which the 'cleavable complex' is not formed. In consequence, it also acts as an antagonist to camptothecin-mediated cleavage. The antitumor pharmacological effects of BA consist of triggering apoptosis via the mitochondrial pathway, regulating the cell cycle and the angiogenic pathway via factors, including specificity protein transcription factors, cyclin D1 and epidermal growth factor receptor, inhibiting the signal transducer and activator of transcription 3 and nuclear factor‑κB signaling pathways, preventing the invasion and metastasis of tumor cells, and affecting the expression of topoisomerase I, p53 and lamin B1. Betulinic Acid has also been used in trials studying the treatment of Dysplastic Nevus Syndrome. Betulinic acid acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 uM. Betulinic acid is an inhibitor of HIV-1 with EC50 of 1.4 uM.

Dicresulene is the antiseptic agent. It was used as a hemostatic drug for the control of persistent bleeding.

Diclonixin is the analgesic and anti-inflammatory agent.

Cinfenoac is a chalcone derivative patented by a pharmaceutical company Biorex Laboratories from the UK. The compound is claimed for the treatment of inflammatory and allergic conditions, as well as for the treatment of the ulcerous condition of the gastrointestinal tract.

Properidine is an isopropyl analog of pethidine that acts as opioid analgesic.

Brallobarbital possessed the sedative and hypnotic properties and was a component of Vesparax that was used to treat sleep disorders. However, was revealed that brallobarbital was responsible for the problems in Vesparax intoxication.

CPI-613 is a lipoate derivative synthesized to be catalytically inert but to potentially mimic lipoate catalytic intermediates. The drug is in phase II of clinical trials for the treatment of Myelodysplastic syndromes; Pancreatic cancer; Small cell lung cancer; Solid tumors; Bile duct cancer; Acute Myeloid leukemia. The mechanism of CPI-613 action can be explained by (I) inhibition of tumor cell pyruvate dehydrogenase complex (PDC) through activation of pyruvate dehydrogenase kinases leading to inactivating phosphorylation of the E1alpha-subunit of PDC; and (II) inhibition of alpha-ketoglutarate dehydrogenase.

Guaisteine, a thiazolidine derivative that was used as an antitussive agent. This compound has never been marketed.

BLI 489 was developed by Wyeth as a 6-methylidene-penem β-lactamase inhibitor for the treatment of bacterial infections and urinary tract infections. BLI-489 has shown the promising clinical data, however, development of this drug, was discontinued.

Mepramidil (PF-26) is a coronary vasodilator.