Current Medicinal Chemistry - Volume 10, Issue 5, 2003

The development of an increasing number of antiretroviral agents has dramatically reduced HIV-associated morbidity and mortality. However, most of these drugs have been approved through clinical trials where only surrogate markers for clinical endpoints have been used. Ideally, a surrogate marker should be biologically plausible, predictive of disease progression and measurable by standardized assays. Historically, a number Read More

The development of small molecule kinase inhibitors as potential cancer therapeutics is an area of intense interest, and a subset of these agents target cyclindependent kinase (CDK) activity. Ten distinct CDKs (1-9, 11), when paired with their cyclin activators, are integral to such diverse processes as cell cycle control, neuronal development, and transcriptional regulation. Mutation and / or aberrant expression of certain C Read More

The importance of lipophilicity for pharmacological and toxicological potency of xenobiotics has been recognized for a century. The reference lipophilicity scale is defined by the logarithm of partition coefficient, log P, determined in the loctanol- water partition system. The tediousness of determinations and limited interlaboratory reproducibility of log P, on one hand, and the observations of linear relationship between log Read More

Anthracycline antibiotics are of particular value in the therapy of malignant diseases and exert profound effects not only on tumor cells but also on cells in the cardiovascular system. These quinone drugs affect vascular tone by a multitude of mechanisms, including acute modulation of Ca2+ homeostasis, altered expression of membrane proteins and enzymes that are involved in the control of smooth muscle contraction, and Read More