Mini Reviews in Medicinal Chemistry - Volume 9, Issue 11, 2009

Carbon nanotubes are widely used for biomedical applications as intracellular transporters of biomolecules, due to their high propensity to cross cell membranes. In this review we summarize the recent advancement in the functionalization of carbon nanotubes, focusing particular attention on the chemistry involved in the preparation of nanovectors for drug delivery systems, and on the physical and chemical properties that affect cellular up-take and biodistribution phenomena.

Neurodegenerative disorders are a heterogeneous group of diseases and are among the most invaliding syndromes for humans. The aim of this manuscript is to review what has been reported so far in the literature about coumarins as a novel class of pharmacologically active compounds in chemoprevention and/or therapy of these diseases.

High levels of cholesterol are a primary risk factor in the development of cardiovascular diseases. In this review, we have summarized the structural, chemical and computational aspects of hypocholesterolemic drugs, both statins and non-statins, that target enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA) to block cholesterol biosynthesis.

Laminin-332 and α6β4 integrin is major hemidesmosome components in the skin. As many studies have shown that laminin-332 and α6β4 integrin play important roles in tumor progression via activation of phosphatidylinositol-3 kinase signaling, understanding of the molecular mechanisms of them could lead to a new drug for cancer therapy.

Anti-Candida activity of essential oils has been widely studied and as a consequence they are being investigated as possible alternatives or complementary therapeutic agents for candidosis. We reviewed the most studied essential oils concerning chemical composition and in vitro/in vivo studies under the perspective of their possible clinical use.

This mini-review summarizes the development of the derivatives and conjugates of Amphotericin B (AMB) which have not been clinically applied so far but are therapeutically promising. Effects of chemical modifications of AMB upon biological activities of the resulting derivatives are discussed. The examples presented include variation of functional groups in AMB, covalent conjugates with other molecules, poly(ethylene glycols) and polysaccharides. Possibilities of targeted delivery of AMB are discussed.

Complexation of known drugs with carbohydrate-containing plant metabolites is a promising way to synthesize new drugs that does not only save pharmacological properties of initial agent but also acquire a number of advantageous features such as increased water solubility, bioavailability and decreased toxicity. This review reports on the development and pharmacological evaluation of novel complexes of various well-known drugs with vegetable coplexation agents: glycyrrhizic acid, Stevia glycosides, gypsogenin tetraoside, pectin, xyloglucan, arabinogalactan. The aim of this review is to describe advantages of the new approach, suggested by authors, in the development of low toxic and high-performance drugs.

Chloramphenicol (CAP) is a widely used broad-spectrum antibiotic. As the precursor of CAP, chloramphenicol bases are stereochemically pure agents and could be used as resolution agents, chiral catalysts and so on. This review summarizes these applications and discusses the structural modifications of chloramphenicol bases.

Novel amphiphilic protein-loaded hyperbranched poly (amine-ester) copolymers nanoparticles were fabricated by double emulsion (DE) and nanoprecipitation (NP) methods. Encapsulation efficiency (EE) of nanoparticles to Bovine serum albumin (BSA) could reach 97.8% at BSA (0.01g/ml), internal phase volume (0.5ml), copolymer weight (50mg), and PVA concentration (4%, w/v) condition.

Cisplatin has become one of the most commonly used compounds for the treatment of a wide spectrum of human malignancies. Unfortunately, cisplatin has several major drawbacks. Driven by the impressive impact of cisplatin on cancer chemotherapy, great efforts have been made to develop new derivatives with improved pharmacological properties. Among the over 30 platinum agents which have entered clinical trials after the onset of clinical studies with cisplatin in the early 1970s, only carboplatin and oxaliplatin have received worldwide approval so far, nedaplatin, lobaplatin and heptaplatin have gained regionally limited approval. It has become quite evident that mere analogues of cisplatin or carboplatin will not probably offer any substantial clinical advantages over the existing drugs. Consequently, attention turned to the synthesis of non-classical platinum anticancer drugs which were capable of forming a different range of DNA adducts which could display a different spectrum of anticancer activity compared to cisplatin. The status of non-classical biand multi-nuclear platinum anticancer drug development has been reviewed. This review will summarize the structural types and structure-activity of non-classical mononuclear platinum anticancer drugs, and discuss their future potential as anticancer agents.