Current Medicinal Chemistry - Volume 10, Issue 1, 2003

Natural xanthonolignoids are formed by the coupling of cinnamyl alcohol with an appropriate ortho-dihydroxyxanthone. More than twenty xanthonolignoids have been isolated and synthesized and some interesting pharmacological activities of these compounds have been described.The purpose of this review is to describe the natural occurrence, isolation, structure elucidation and synthesis - both biomimet Read More

The notion that medicines derived from plants depend for their action on active principles present has to be modified in view of the findings that there are, in many cases, adjuvant substances in the plant which enhance the activity of the components actually responsible for the effect. This synergy may involve protection of an active substance from degradation by enzymes, it may facilitate transport across barriers such as Read More

In this present review we report different synthetic methodologies for the preparation of fluoroquinolones and their biological properties. The appearance of the fluoroquinolones, a new class of antibacterial agents (based on nalidixic acid, 4-quinolone-3-carboxylates), in early 1980's, gave a new impulse for the international competition to synthesize more effective drugs. Fluoroquinolones have a broad spectrum of activity Read More

Irinotecan, a camptothecin analogue, is a prodrug which requires bioactivation to form the active metabolite SN-38. SN-38 acts as a DNA topoisomerase I poison. Irinotecan has been widely used in the treatment of metastatic colorectal cancer, small cell lung cancer and several other solid tumors. However, large inter-patient variability in irinotecan and SN-38 disposition, as well as severe but unpredictable diarrhea lim Read More

With the recent emergence of combinatorial chemistry and high-speed parallel synthesis for drug discovery applications, the multi-component reaction (MCR) has seen a resurgence of interest. Easily automated one-pot reactions, such as the Ugi and Passerini reactions, are powerful tools for producing diverse arrays of compounds, often in one step and high yield. Despite this synthetic potential, the Ugi reaction is limited b Read More