Estramustine phosphate sodium (EMP, Emcyt, Estracyt) is an antitumour drug with a unique dual mode of action. Estrone and estradiol, products of the metabolism of estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels. Estramustine(the cytotoxic metabolite produced by dephosphorylation of estramustine phosphate sodium) is an antiprostatic tumor drug with antimicrotubule effects.

Inosine (NSC 20262, INO 495) is a nucleoside that is formed when hypoxanthine is attached to a ribose ring via a β-N9-glycosidic bond.

Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes.

Parbendazole (SKF 29044) is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules.

Fabomotizole hydrochloride (Fabomotizole, CM346, CM346, Afobazol, Afobazole) exhibits anxiolytic and neuroprotective properties. Fabomotizole hydrochloride is a potent sigma1-receptor agonist with IC50 of 7.1 µM and Ki of 5.9 µM.

Biochanin A (4-Methylgenistein), an O-methylated isoflavone from Trifolium pratense, inhibits protein tyrosine kinase (PTK) of epidermal growth factor receptor with IC50 values of 91.5 μM.

Daidzin (Daidzoside, Daidzein 7-O-glucoside, Daidzein 7-glucoside), a natural organic compound in the class of phytochemicals known as isoflavones, is a potent and selective inhibitor of human mitochondrial aldehyde dehydrogenase and inhibits ALDH-I selectively (Ki=20 nM); at least 500 times less effective against ALDH-Ⅱ, the cytosolic isozyme (Ki=10 μM).

Glycyrrhizin (NSC 167409, Glycyrrhizic Acid) is a direct HMGB1(high mobility group box 1) inhibitor that inhibits HMGB1-dependent inflammatory molecule expression and oxidative stress; modulates P38 and P-JNK but not p-ERK signalling; Also inhibits 11 beta-hydroxysteroid dehydrogenase and monoamine oxidase (MAO).

Gossypol Acetate (Gossypol Acetic acid, Pogosin, AT101) is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes.

Roquinimex (FCF 89, Linomide, LS 2616) is a novel immunomodulator augmenting natural killer (NK) cell activity and T-lymphocyte related effector functions. Roquinimex is a potent oral active tumor antiangiogenic agent. Roquinimex inhibits the secretion of TNF-α.