Current Medicinal Chemistry - Volume 10, Issue 21, 2003

Natural products are the valuable source of structurally diverse compounds which possess therapeutic potential for treatment of human diseases. Many of the clinically used therapeutic agents are of natural products origin, used either in the naturally occurring forms or as the derivatives or analogs after structural optimization. The influence of natural products upon drug discovery has been well recognized and documented. Read More

This article reviews the discovery and the further studies on qinghaosu and its derivatives or analogs over the last decades in the fields of medicinal chemistry and some pharmacology research, with an emphasis on the progress achieved in China.

HupA is a potent, reversible AChEI, which crosses the blood-brain barrier smoothly, and shows high specificity for AChE with a prolonged biological half-life. It has been approved as the drug for the treatment of AD in China, and marketed in USA as a dietary supplement. HupA has been the subject of investigations by an ever-increasing number of researchers since 1980's. In the last four years, HupA has been further studied Read More

The characteristic components of Spiraea japonica complex, which consists of seven varieties, are the hetisine- and atisine-type diterpene alkaloids, and the atisanetype diterpenes. From this complex, 20 hetisines, 37 atisines and 7 diterpenes were isolated during 1964-2001, including the observations of the isomerization of spiraea diterpene alkaloids having the oxazolidine ring and the interconversion of the oxazolidin Read More

Cyclodeca-1,5-diyn-3-ene, the parent core of naturally occurring 10- membered ring enediyne antitumor antibiotics, decomposes at 37°C with a t1 / 2 value of 18 h. A prodrug approach was envisaged by in situ formation of the core structure via rearrangement of an allylic double bond. Three synthetic methods including intramolecular lithium acetylide addition to aldehyde, intramolecular Nozaki-Hiyama- Kishi reaction, and intr Read More

Combinatorial chemistry can be used to synthesize diversified molecules on a large scale. As with all large-scale experiments, this process requires a major investment in equipment, consumables and time. Therefore, careful design is critical. As the complexity of the libraries to be generated increases, additional considerations become important. What are the issues that should be considered when planning combinatorial che Read More

This review gives a brief account on the current status of enediyne biosynthesis and the prospective of applying combinatorial biosynthesis methods to the enediyne system for novel analog production. Methods for cloning enediyne biosynthetic gene clusters are first reviewed. A unified paradigm for enediyne biosynthesis, characterized with (a) the enediyne PKS, (b) the enediyne PKS accessory enzymes, and (c) tailoring Read More

Natural products, containing inherently large-scale structural diversity than synthetic compounds, have been the major resources of bioactive agents and will continually play as protagonists for discovering new drugs. However, how to access this diverse chemical space efficiently and effectively is an exciting challenge for medicinal chemists and pharmacologists. While virtual screening, which has shown a great promis Read More