Mini Reviews in Medicinal Chemistry - Volume 17, Issue 7, 2017

Background: The design, medicinal chemistry, pharmacokinetics and development of the highly selective α2-adrenoceptor antagonist fluparoxan are reviewed. Method: The drug's activity and selectivity in vitro, its efficacy in animals and its excellent oral pharmacokinetics and central α2-adrenoceptor antagonist activity in man, are evaluated as well as its ability to increase extracellular levels of noradrenaline, dopamine a Read More

Background: Breast cancer is the second leading cause of cancer-related deaths among women in the Western World. Method: Upon diagnosis and treatment in the preinvasive state, the five years survival rate levitate up to 93%, making early detection crucial for dedicative diagnosis and treatment. Currently, mammography is the most efficacious diagnostic modality. However, this technique does not match the ultimate s Read More

Background: Proliferation of the smooth muscle and epithelial cells within the prostatic transition zone in older men leads to benign prostatic hyperplasia (BPH), which is hallmarked by the troublesome lower urinary tract symptoms. The affair responsible for the initiation and promotion of disease is still unresolved, though alpha-blockers and 5α-reductase inhibitors are used as management options for relief from the dyna Read More

Background: Acremonium fungi have been isolated from various sources, such as soil, plants, and marine organisms. Method: The species in Acremonium have been proved to be rich sources of novel and bioactive secondary metabolites. Up to now, 356 metabolites belonging to steroids (6 compounds), terpenoids (86), meroterpenoids (66), polyketides (89), alkaloids (28), peptides (75), and miscellaneous types (6) have b Read More

Background: The water insolubility of fullerene C60 nanostructure greatly hampers its biological applications as an effective HIV-1 protease inhibitor, which suggests to synthesis new C60 derivatives with different functional polar groups. Method: The new carbon nanostructures of fulleropyrrolidines with one and two polar acetoxyhydroxyl (AcH) groups (C60-A and C60-B, respectively) were constructed to evaluate t Read More