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Scripps research team achieves critical step to opening elusive class of compounds to drug discovery
Date:11/6/2011

LA JOLLA -- Taxanes are a family of compounds that includes one of the most important cancer drugs ever discovered, Taxol, among other cancer treatments. But the difficulty producing these complex molecules in the lab has hampered or blocked exploration of the family for further drug leads. Now, a group of Scripps Research Institute scientists has successfully achieved a major step toward the goal of synthetically producing Taxol and other complex taxanes on a quest to harness chemical reactions that could enable research on previously unavailable potential drugs.

The project, led by Scripps Research chemist Phil Baran, is described November 6, 2011 in an advance, online issue of the journal Nature Chemistry.

Taxol, the trade name for a chemical called paclitaxel first discovered in 1967 in the bark of a yew tree, is a highly successful drug used to treat ovarian, breast, lung, liver, and other cancer types. No less than seven different research groups have designed several ways to produce Taxol synthetically, beginning in the 1990s with a team led by K.C. Nicolaou, chair of the Scripps Research Department of Chemistry.

While each synthesis was a significant accomplishment, each has also been exceedingly complex and inefficient. Using all these methods collectively, researchers have produced less than 30 milligrams of synthetic Taxol. Producing other chemicals from the same promising taxanes chemical group is nearly as challenging, vastly limiting access to them for research.

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Finding an efficient way to produce Taxol in sizable quantity in the laboratory remains one of the most sought-after and elusive goals in organic chemistry. If accomplished, it would open the door to producing countless other taxanes that are not accessible from nature. Past methods were devised using conventional schemes where researchers plot a linear path of increasingly complex molecules leading to a targ
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Contact: Mika Ono
mikaono@scripps.edu
858-784-2052
Scripps Research Institute
Source:Eurekalert  

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