Toward powerful new anticancer drugs with new ways of targeting tumors
Journal of the American Chemical Society
The search for new anticancer drugs has led scientists in Pittsburgh to synthesize a compound that works in a different way than existing agents and is so potent that minute levels of 10 parts per trillion block the growth of tumor cells in laboratory experiments. Kazunori Koide and colleagues describe the compound as one of the most potent of all anticancer agents in a report scheduled for the March 7 issue of the Journal of the American Chemical Society.
The parent compound, FR901464, inhibited the growth of cancer cells implanted into laboratory mice. Because of structural similarity between FR901464 and their analogue, called meayamycin, the Koide group is cautiously optimistic that meayamycin also will be effective against tumors in mice. The amount that the Koide employed against cancer cells is equivalent to 10 seconds in 32,000 years or one packet of sugar (5 grams) in a coffee cup the size of 400 Olympic-size pools.
In the article, researchers explain that existing chemotherapy medications work by targeting only a handful of vulnerable spots in a tumor, such as the DNA or hormone receptors. That limited range of targets has led scientists to seek new generations of medications that work in different ways.
http://pubs.acs.org/cgi-bin/sample.cgi/jacsat/asap/pdf/ja067870m.pdf
Total Synthesis, Fragmentation Studies, and Antitumor/Antiproliferative Activities of FR901464 and Its Low Picomolar Analogue
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