Mini Reviews in Medicinal Chemistry - Volume 17, Issue 8, 2017

Background: Quantum dots are an emerging nanomaterial with broad use in technical disciplines; however, their application in the field of biomedicine becomes also relevant and significant possibilities have appeared since the discovery in 1980s. Objective: The current review is focused on the therapeutic applications of quantum dots which become an emerging use of the particles. They are introduced as potent Read More

Background: Glucocorticoids (GCs) are largely used in different inflammatory, autoimmune and proliferative diseases. To date their mechanism of action is not completely clear and more studies are necessary, in particular to explain the great interindividual variability in clinical response. In this panorama the glucocorticoid receptor (GR) has an important role: in fact it regulates the pharmacological response thanks to the capabi Read More

Background: Caffeic acid (CA) and related phenylpropanoic acids are ubiquitous natural products of the shikimic acid pathway origin. Due to the presence of diorthohydroxyl aromatic (catecholic) moiety, CA is not only one of the most potent antioxidant phenyl propanoids but also displays numerous other pharmacological effects ranging from antiinflammatory to anticancer effects. Objective: Recent studies also demonstra Read More

Background: Tip60, the founding member of MYST histone acetyltransferase family, was originally identified as a cellular acetyltransferase protein that interacts with HIV-1 Tat. Tip60 plays roles in many processes such as cellular signaling transmission, DNA damage repair, cell cycle and checkpoint control and apoptosis by acetylating its histone or non-histone substrates. Results: Dysfunction of Tip60 could promote or sup Read More

Background: The widespread application of fluorine in drug design benefits from distinctive properties. Incorporation of fluorine can positively modulate certain pharmacokinetics properties, including lipophilicity, eletrophilicity, metabolic stability, chemical stability, et al., which were of interest to medicinal chemists. Herein, fluorinated compounds, which have been designed and evaluated for anticancer, antimicrobial, a Read More

Background: The genus Piper L. has the shikimic acid pathway predominantly expressed, biosynthesizing many cinnamic acid derivatives (CAD). Objective: Neolignans comprise an important class of CAD that exhibit a wide range of pharmacological properties such as antibacterial, antitumor, insecticidal, anti-inflammatory, antioxidant, smooth muscle relaxant, neuroprotective, antiprotozoal and against platelet aggregation fac Read More

Background: Thiazolidinediones (TZDs) and sulfonamides are important and highly consumption class of antidiabetic drugs having insulin sensitizing and stimulating properties in patients with type 2 diabetes, respectively. Objective: In this paper, some novel benzothiazole derivatives of TZD-sulfonamides were synthesized (I-IV) and evaluated for anti-hyperglycemic and anti-hyperlipidemic activities in the STZ-induced diabetic Read More