Current Medicinal Chemistry - Volume 20, Issue 22, 2013

Heat shock proteins (HSPs) and chaperones are highly conserved stress-induced factors. They regulate not only protein folding and stability but are also actively involved in protein transport and transcriptional regulation. HSPs have cytoprotective roles and are essential for cancer cell survival. Noteworthy, HSPs are often upregulated in cancer. Therefore, HSPs emerged as drug targets for cancer therapy. Especially for prostate Read More

Centrally acting opioids, such as morphine, are the most frequently used analgesic agents for the treatment of severe pain. However, their usefulness is limited by the production of a range of adverse effects such as constipation, respiratory depression, tolerance and physical dependence. In addition, opioids generally exhibit poor efficacy against neuropathic pain. Endomorphin-1 and -2, two endogenous opioid Read More

Many pharmaceuticals on the market suffer from two significant limitations to their activity: lack of specificity toward the pathological site and poor aqueous solubility. Both factors therefore require the application of a large total dose of a drug to achieve high local concentration, causing numerous off-target toxic effects. Consequently, the grand aim of targeted drug delivery - the often-referred “magic bullet” - promises t Read More

Arterial thrombosis is the acute complication that develops on the chronic lesions of atherosclerosis and reasons heart attack and stroke, today the most common causes of mortality in developed countries. According to the WHO, 17.1 million people died world wide of cardiovascular diseases (CVD), per year, accounting for one-third of all deaths globally. On the basis of current estimates from the American Heart Association, Read More

Agelasines, asmarines and related compounds are natural products with a hybrid terpene-purine structure isolated from numerous genera of sponges (Agela sp, Raspailia sp). Nuttingins and malonganenones are tetraprenylated purine alkaloids from gordonian (Eplexura sp, Leptogorgia sp). Some of these alkaloids displayed broad spectrum activity including cytotoxic activity against several cancer cells. The review summ Read More

Herbal therapies gained much popularity among the general public, but compared to therapies approved by official authorities, toxicological studies are frequently not available for them. Hence, there may be inherent risks and the kidneys may be especially vulnerable to toxic effects. Herbs may induce nephrotoxicity by induction of apoptosis. High oxalate contents in Star fruit (Averrhoa carambola L.) may induce acute nephropat Read More

In the search for new estrogen receptor alpha (ERα) modulators, a trial molecular screening was conducted and 5,6-dihydroxybenzofuran was identified as a possible drug target for ERα. The target molecular modelling molecule 1 and a series of 5,6-dihydroxybenzofurans have been synthesized and evaluated for their anti-proliferation activities against MCF-7 and MDA-MB-231 cells. From the SAR studies, potential fun Read More