New process opens drug development for new steroid class

The new technique significantly reduces the expense and time required to develop drugs.
By Amy Wallace  |  Sept. 25, 2017 at 3:59 PM
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Sept. 25 (UPI) -- Dartmouth College researchers have developed a new technique to produce synthetic steroids that reduces the time and expense needed to develop new drugs.

The technique is based on a series of new chemical reactions and could pave the way for rapid new drug development.

"This is a fundamentally new molecular strategy for steroid construction," Glenn Micalizio, the New Hampshire Professor of Chemistry at Dartmouth, said in a press release. "This technology allows the preparation of either mirror-image isomer with equal ease, but with unprecedented efficiency."

The core molecular structure of steroids is a basis for most drug development, with more than 100 different steroid molecules approved by the U.S. Food and Drug Administration as therapeutics for a variety of symptoms and diseases from pain and inflammation to cancer and bacterial infections.

All drugs in the steroidal drug class share a common structure consisting of only one of two possible mirror image skeletons known as enantiomers.

The new technique developed at Dartmouth is based on a chemical reaction discovered by Micalizio in 2014 that creates half of the steroid structure. The new class of synthetics can be produced in only five chemical steps.

The study, published today in Nature Chemistry, demonstrated how the new technique produces steroidal structures of either enantiomer with an "unprecedented efficiency," and uses inexpensive and abundant materials.

"With this advancement, we now have the opportunity to investigate fertile regions of chemical space for the identification of untold numbers of unique, medicinally relevant agents," Micalizio said. "This is by far the most concise and flexible route to make a wide variety of novel steroids."

Synthetic mirror image isomers are not readily found in natural sources, so the creation of this class of drugs depends on the ability of organic chemists to prepare them.

"The science of synthetic organic chemistry is an essential component of drug discovery, and advances in this field are directly responsible for our recent discovery," Micalizio said.

"Without the ability to create new collections of molecules, it is difficult to pursue many potentially exciting new directions in drug discovery. As such, advances in chemical synthesis, like this one, can have profound and rippling effects on biomedical science."

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