Mini Reviews in Medicinal Chemistry - Volume 6, Issue 4, 2006

Coumarins, an old class of compounds, are naturally occurring benzopyrene derivatives. A lot of coumarins have been identified from natural sources, especially green plants. These natural compounds have served as valuable leads for further design and synthesis of more active analogs. The pharmacological and biochemical properties and therapeutic applications of simple coumarins depend upon the pattern of substituti Read More

A major recent focus of quinolone antibacterials has been the development of agents with enhanced activity against Gram-positive bacteria. The extensive research efforts have enabled a better definition of the structural features of quinolones that offer the best combination of clinical efficacy and reduced resistance selection in Gram-positive bacteria. This review considers the structural features of new quinolones and Read More

Novel anti-cancer treatments use knowledge about the underlying biology of the tumor to find suitable molecular targets. The recent years have seen great advances in understanding the biology of melanoma. In the current review we discuss the most promising molecular targets for melanoma and suggest possible strategies for overcoming resistance.

Ifosfamide (IFO), an oxazaphosphorine-type anticancer alkylating agent, was found to be particularly useful in the treatment of a wide variety of neoplasm in adults and children. IFO is a positional isomer of cyclophosphamide (CPA) and was introduced into clinical practice in the '80s and has recently attracted much attention. Therapeutic application of high-dose IFO is limited by several side-effects; among them neurotoxicity Read More

Genistein, one of the predominant soy isoflavones, has been shown to compete with 17 β-estradiol for estrogen receptor binding because of its structural similarity, resulting in agonistic or antagonistic activity. It causes inhibition of cell growth in breast and prostate cancers in vivo and in vitro. From gene expression profiles, genistein has been found to regulate the genes that are critical for the control of cell proliferation, Read More

Reactive oxygen species can induce several biological processes by stimulating signal transduction components such as cytosolic free calcium concentration. The physiological significance of the role of biological oxidants in the regulation of calcium signalling pathway as well as the mechanisms of the oxidantstimulation of signal transduction are discussed in this review.

The pharmacokinetics of corticosteroids provides a large set of mathematical models which led to analyse many kinetic profiles corresponding to many clinical and/or physiological situations. In this paper, we present a review on the usefulness, advantages and limits of such models which could find a large application in medicinal chemistry.

Neuraminidase (NA) is the major surface glycoprotein of the influenza virus. It has been considered a suitable target for designing agents against influenza viruses. Rational drug design of NA inhibitors is now in the clinic and is effective for the treatment of influenza. Recently, research of structure-based NA inhibitors is becoming an interesting field, leading to a breakthrough in the control of influenza. Here we review a se Read More

Computational methods for predicting compounds of specific pharmacodynamic, pharmacokinetic, or toxicological property are useful for facilitating drug discovery and drug safety evaluation. The quantitative structure-activity relationship (QSAR) and quantitative structure-property relationship (QSPR) methods are the most successfully used statistical learning methods for predicting compounds of specific property. Read More

The unique biological properties of Geminin, particularly as an inhibitor of DNA replication initiation, have been recognized, and this has prompted a number of investigations into this molecule to explore its potential therapeutic as well as diagnostic usefulness. This review summarizes the possibility of Geminin serving as a new molecular target in the development of new anticancer drugs.

CC chemokine receptor (CCR) 8, which is expressed on Th2 cells and eosinophils, has been implicated in allergic diseases. This review represents an overview of the functional roles of CCR8 in the pathogenesis of eosinophilic inflammation and debates the potential of recently developed CCR8 antagonists to treat allergic disorders.

Cardiovascular diseases are still the main cause of morbidity and mortality in the world. Anti-platelet drugs have found clinical application in the secondary prevention of vascular events including acute myocardial infarction, stroke and cardiovascular death. In the present review, we have developed sixteen quantitative structure-activity relationships (QSAR) for different sets of compounds that are X-phenols (I), Xcatechols ( Read More

Human serum albumin (HSA), the most prominent protein in plasma, is best known for its extraordinary ligand binding capacity. The three homologous domains of HSA (labeled I, II, and III), each in turn composed of two subdomains (named A and B), give rise to the three-dimensional structure of HSA. This flexible structural organization allows the protein structure to adapt to a variety of ligands. As conformational ada Read More