Mini Reviews in Medicinal Chemistry - Volume 7, Issue 6, 2007

Allosteric enhancers at the adenosine A1 receptor have received attention as anti-arrhythmic cardiac agents, and, more recently, as anti-lipolytic agents. In addition, allosteric modulators at the adenosine A1 receptor have therapeutic potential as analgesics and neuroprotective agents. In particular, the compounds with improved potency as enhancers and reduced antagonist properties are mentioned.

Present review describes research on novel natural anticancer agents isolated from terrestrial and marine sources. More than 120 cytotoxic anticancer compounds have shown confirmed activity in vitro tumor cell lines bioassay and are of current interest to Natural Cancer Institute for further in vivo evaluation. Intensive searches for new classes of pharmacologically potent agents produced by terrestrial and marine org Read More

The traditional treatment of secondary hyperparathyroidism, which affects many patients with chronic kidney disease and is associated with an increased risk of morbidity and mortality, is not very effective. Recent approaches to its management include the use of vitamin D analogues, non-calcium non-aluminium containing phosphate binders, and calcimimetics.

For more than a century, inhibition of prostaglandin biosynthesis via inhibition of the fatty acid cyclooxygenase (COX) has been achieved by non-steroidal anti-inflammatory drugs (NSAIDs), which targets both COX-1 and COX-2 and as such could be responsible for causing gastrointestinal (GI) toxicity. COX-2 is an inducible enzyme produced by many cell types in response to multiple stimuli. Recently, COX-2 over-expression has Read More

Typically, malignant melanoma has wild-type p53, and yet this cancer proliferates. S100B, which binds p53 and is up-regulated in melanoma, down-regulates wild-type p53 tumor suppressor function. Inhibitors of the S100B-p53 interaction were identified using computer aided drug design (CADD) combined with NMR methodologies and represent potentially new chemotherapeutics for melanoma.

Nuclear hormone receptors (NHRs) are transcription factors that bind to lipophilic signaling molecules (ligands), and subsequently regulate the expression of target genes. Since NHR ligands have potential as therapeutic agents, one of the most active research areas in the NHR field is the synthesis and identification of small molecule ligands for NHRs. Wipf et al. have recently reported the creation of a discovery library usin Read More

Since the discovery of the DNA intercalation process by Lerman in 1961 thousands of organic, inorganic octahedral (particularly ruthenium(II) and rhodium(III)) and square-planar (particularly platinum(II)) compounds have been developed as potential anticancer agents and diagnostic agents. The design and synthesis of new drugs is focused on bisintercalators which have two intercalating groups linked via a variety of ligands, Read More

Malignant melanoma is one of the most highly invasive and metastatic tumors. Melanoma is an increasingly common malignancy as well, and its mortality rates have been rapidly increasing above those of any other cancer in recent years. Surgical resection and systemic chemotherapy are the main therapeutic strategies for the treatment of malignant melanoma. However, these approaches are insufficiently effective and Read More