J. Beisler
1982
Citations
0
Influential Citations
10
Citations
Journal
Progress in Medicinal Chemistry
Abstract
Publisher Summary This chapter presents a comprehensive review of chartreusin, its chemistry, biosynthesis, biological action and drug potential. Spurred on by its activity in mouse leukemias as well as in solid tumour test systems, the present interest in chartreusin is centered on its potential as a cancer chemotherapy drug. Chartreusin is a biologically active parent structure on which to base an analogue synthesis effort. The structure of the antibiotic is not complex and should be amenable to an analogue synthesis programme. The chemical explorations that lead to total syntheses of the aglycone should prove to be useful in the generation of analogues. Because chartreusin is rapidly and efficiently excreted in the bile, the antibiotic could be used to study the process of biliary excretion. Phenolphthalein has been used in such studies, but conjugation with glucuronic acid is a complicating factor.