Tiodazosin is a newly developed antihypertensive agent, structurally related to prazosin. Prazosin and tiodazosin administrated intravenously to anesthetized rats, are equally effective hypotensive agents, but that the hypotensive potency of prazosin is greater than that of tiodazosin. However, chronic administration of equivalent doses of the two compounds for 25 and 52 days via the drinking water indicated approximately equivalent, sustained reductions in blood pressure. Furthermore, at the end of the 52-day chronic dosing period tiodazosin caused appreciably less alpha-adrenergic receptor antagonist activity than prazosin as assessed by the norepinephrine dose-pressor response profiles.

Atiprosin (AY-28,228), an octahydro-pyrazino-pyrido-indole drug, possesses the alpha-adrenoceptor antagonist activity and exerts antihypertensive effects. Atiprosin has never been marketed

IZONSTERIDE, a benzoquinolinone, is a selective inhibitor of the 5-alpha reductase, with antagonistic effect on both the type I (liver, skin, hair follicles) and type II (prostate) isoforms of the enzyme. It is a competitive inhibitor of type I 5-alpha reductase and a non-competitive inhibitor of type II 5-alpha reductase. It was under development for the treatment of prostatic cancer.

Androsterone, a neurosteroid, acts as a positive allosteric modulator of GABA(A) receptors, that can cross into the brain and could have effects on brain function. It was discovered, that the association of beta subunits with alpha subunits GABA(A) receptor affects the sensitivity of glycine receptors to androsterone. In spite of that, androsteron is considered as an inactive metabolite of testosterone. In addition, was studied that androsterone possessed anticonvulsant properties. Although of low potency, the androsterone was present in high abundance and was able to represent endogenous modulator of seizure susceptibility.

BAY-87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. BAY 87-2243 inhibits HIF-1 reporter gene activity and CA9 protein expression with IC50 of 0.7 nM and 2 nM, respectively. In hypoxic lung cancer H460 cells, BAY-87-2243 suppresses HIF target gene expression, and inhibits HIF-1α protein accumulation. BAY-87-2243 showed dose-dependent in vivo antitumor efficacy in the H460 lung tumor xenograft model accompanied by a suppression of HIF-1a protein and HIF-1 target genes without any signs of toxicity or body weight loss. Further mode-of-action analyses revealed that BAY-87-2243 exerts its effect on the HIF pathway by blocking mitochondrial complex I activity and thereby reducing HIF protein levels under hypoxia. BAY-87-2243 had been in phase I clinical trials by Bayer for the treatment of malignancies. However, this study has been terminated for the drug-related adverse events.

Alpha-carotene is a provitamin A carotenoid present in fruits and vegetables. Higher serum concentrations of α-carotene have been associated with lower risk of cancer and all-cause mortality. It was suggested that genetic variants influence serum concentrations of provitamin A. Recently was found, that α-carotene effectively inhibits Lewis lung carcinoma (LLC) metastasis and suppresses lung metastasis in combination with taxol in LLC-bearing mice, suggesting that Alpha-carotene could be used as an anti-metastatic agent or as an adjuvant for anti-cancer drugs.