Current Medicinal Chemistry - Volume 19, Issue 4, 2012

MicroRNAs (miRNAs) are small (typically 22 nucleotides) non-coding, endogenous, single-stranded RNAs. MiRNA genes are evolutionarily conserved and are located within the introns or exons of protein-coding genes, as well as in intergenic areas. Before the discovery of miRNAs, it had been known that a large part of the genome is not translated into proteins. This so called “junk” DNA was thought to be evolution debris with Read More

The heterogeneous nature of cancer requires a comprehensive approach for attacking the multiple mechanisms underlying the initiation and progression of cancers. Histone deacetylase inhibitors (HDACi) have emerged as a new class of anticancer agents, targeting the biological processes including cell cycle, apoptosis and differentiation. Studies have revealed that HDACi are synergistic with diverse classes of anti Read More

Tuberculosis (TB) caused by Mycobacterium tuberculosis claims millions of lives each year globally. Although it can be controlled by currently available drug regimen (DOTS), yet the emergence of multidrug resistance (MDR) and extensively drug resistance (XDR) TB is a growing concern. The increasing rate of MDR-TB, co-infection with HIV and XDR-TB necessitates the development of new anti-TB agents that have a practi Read More

Cellular interactions among platelets, leukocytes and endothelial cells are considered as a major cause of inflammation and atherosclerosis in many diseases. Via exposed surface receptors and released soluble substances, activated platelets play a crucial role in the initiation of inflammatory processes, resulting in endothelial injury and leading to formation of atherosclerotic plaque with possible thrombotic complications. Clas Read More

Neuroprotectins, resolvins, and maresins are subfamilies of endogenous oxygenated metabolites derived from n-3 or ω-3 fatty acids (eicosapentaenoic and docosahexaenoic acids). These metabolites are associated with signal transduction processes involved in downregulation of oxidative stress, neuroinflammation and apoptosis. Eicosapentaenoic acid-derived E-series resolvins (RvE1 and RvE2) and docosahexaen Read More

The G protein-coupled receptors (GPCRs) are membrane proteins that transmit signals via G-protein coupling. They have long been the target of small molecule therapeutics accounting for 30% of the launched drug targets. They are subdivided into several classes, with rhodopsins corresponding to the largest class. Furthermore, a high number of new rhodopsin-like GPCR proteins are included in the druggable geno Read More

Z-DNA, an active element in genome, has drawn intense interest in chemical and biological field. Its dynamic and transient state makes it challenging to target and regulate. Thus, stabilizing and inducing Z-DNA both in vitro and in vivo is essential, so far, much many efforts have been made in these aspects. However, Z-DNA's induction and stabilization are always performed in high salt condition and sequence-depende Read More

There has been considerable interest in the development of novel compounds with anticonvulsant, antioxidant, hormone antagonist, analgesic, anti-inflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and anti-trypanosomal activities. Hydrazones possessing an azometine -NHN=CH- proton constitute an important class of compounds for new drug development. Therefo Read More

The inbuilt 2-N-hydroxy-1-oxo-3-carboxylic acid of isoquinolone was designed as pyrophosphate mimic for hepatitis C NS5B polymerase. Various 2-hydroxy-1-oxo-1,2-dihydroisoquinoline-3-carboxylic acid derivatives 11a-p were synthesized and evaluated as HCV NS5B polymerase inhibitors. Compound 11c exhibited moderate inhibitory potency based on the inorganic pyrophosphate generation (IC50 = 9.5 μM) and based on Read More