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 carriers of drugs and as a material well suited for the diagnosis of disparate pathologies like visualization of cancer cells or pathogenic microorganisms. Conclusion: Quantum dots toxicity and modifications for the toxicity reduction are discussed here as well. Survey of actual papers and patents in the field of quantum dots use in the biomedicine is provided.

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 capability to interact with different molecules (DNA, RNA, ncRNA and proteins) that are known to influence its activity. Results: In this review our aim is to highlight the knowledge about the role of protein-protein, RNAprotein interactions and epigenetic modifications on the GR and the consequent response to GCs. The characteristics of these interactions with the GR and their effects on the pharmacological activity of GCs will be examined. Conclusion: This information could contribute to the prediction of individual sensitivity to steroids through the identification of new markers of GC resistance. In addition this knowledge may be used in developing new strategies for targeted therapy.

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 demonstrated that CA both in its free form or conjugated with other groups such as quinic acid and sugars displays profound effects in the brain including protection from toxicity induced by a variety of agents and/or experimental models of Alzheimer's disease (AD). In this communication, the anti-AD therapeutic potential of CA and its two most common conjugated natural bioactive derivatives, chlorogenic acid (CGA) and caffeic acid phenethyl ester (CAPE), is scrutinised by reviewing literature in the past ten years. Besides the common global antioxidant effects, specific antiinflammatory mechanisms in the brain along with the various processes of β-amyloid formation, aggregation and neurotoxicity targets are discussed. Conclusion: The mini-review also provides an insight into enhancing the therapeutic potential of existing anti-AD drugs by incorporating a CA structural moiety.

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 suppress diseases including different kinds of cancers. Conclusion: Here, main functions and its known inhibitors were summarized. >

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, anti-inflammatory and antivirus activity, et al. during the last 6 years (2010-2015) are summarized. Conclusion: The emphasis is to highlight the importance of fluorinated compounds and the changes in the properties of compounds when introducing fluorine atom.

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 factor. These substances have been extracted and isolated from Piper species using different technics. Results: The present review aims to summarize extraction and isolation methods and biological activities of the different types of neolignans covering the period from 1968 to January 2016.

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 rat model. Results: Results indicated that all new conjugated compounds showed significant hypoglycemic activities compared to control animals that were better for I and IV than others. Moreover, these new compounds displayed high efficiency for lowering lipid profiles as compared to control and standard (Pioglitazone) groups that was significant and higher for I than others. Conclusion: It is concluded that these new conjugated TZD-sulfonamide-benzothiazoles (I-IV) can indicate useful results for hypoglycemic and hypolipidemic activities compared to control and standard groups, respectively with different mechanism that is closer to TZDs' analogs.