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It is now widely appreciated that the most exciting discoveries can be made at the common boundaries of chemistry and biology. Understanding of the disease process at molecular level is one manifestation of the nexus between chemistry and biology. This understanding of the molecular targets combined with technological progress has led to the development of a whole range of biological screening methods as essential drug discovery tools. Along with this, biological and pharmacological screenings involving experimental animals, isolated organs, cell and tissue cultures and microorganisms are extensively used. Using these tools of biological evaluation, a large number of lead molecules are routinely discovered. However since such molecules are reported in thousands of publications and it is often difficult to extract information about the more important lead structures. Each issue of the new journal Current Bioactive Compounds will bring the most exciting lead discoveries in important therapeutic areas such as cancer, diabetes, HIV, inflammation, infections of various types, cardiovascular disorders, CNS disorders, etc. Along with this, compounds with antioxidant and anti-obesity activities, enzyme inhibitory and many other activities have also been included. These molecules, from both synthetic and natural sources, have been searched out from a huge body of recent chemical literature and presented in an easy-to-read format with the necessary details about the structures, biological assay methods employed and results obtained. We hope that this compilation of useful data will immensely benefit the researchers associated with drug discovery programs both in pharmaceutical industries and in academic institutions.