Scripps Research Institute Chemists Invent Powerful Toolkit, Accelerating Creation of Potential New Drugs Method provides reactions so robust they can work in a paper cup containing Oolong tea
LA JOLLA, CA November 28, 2012 Scientists at The Scripps Research Institute (TSRI) have invented a set of chemical tools that is radically simplifying the creation of potential new drug compounds.
Pharmaceutical chemists frequently seek to generate dozens or even hundreds of variations of a given compound to see which works best. The new toolkit described in the November 28, 2012 issue of the journal Nature makes this process easier and cheaper, enabling previously time- and cost-prohibitive chemical modifications. This fundamental innovation is already being adopted by drug companies and is expected to speed the development of new compounds in other industries as well.
Feedback from companies that have started to use this toolkit indicates that it solves a real problem for them by boosting their chemists' productivity and by expanding the realm of compounds that they can feasibly generate, said Phil S. Baran, PhD, a professor in the Department of Chemistry and a member of the Skaggs Institute for Chemical Biology at TSRI who led the work.
Robert Lees, PhD, of the National Institutes of Health's National Institute of General Medical Sciences, which partially funded the work, added, Methods to predictably, selectively and efficiently functionalize a given C-H site are difficult to invent but highly significant for developing new therapeutic and diagnostic agents, and studying biomolecules. Practical chemistry for introducing fluorine atoms into organic compounds is also an important current need in medicinal chemistry. The new reagents developed by Professor Baran address both goals, and they will likely be widely utilized in both academic and industrial laboratories.
A Common and Useful Structure
The toolkit is a set of newly invented chemicals and methods for attaching functional groups of molecules to a series of common chemical structures known as nitrogen-containing heterocycles flat molecules with rings made of carbon atoms and at least one nitrogen atom. Though their name might seem esoteric, these structures are common in both natural and synthetic chemicals, and they are found in most drugs that are taken in pill form.
Ironically, the properties that make nitrogen-containing structures so useful in medicines are what also make them so hard to modify, said Baran. The resistance of nitrogen heterocycles to modification by traditional techniques has slowed drug discovery and has put many potential modifications out of reach.
But Baran envisioned a different scenario. The ideal for discovery chemists would be a method that works in water, in an open flask, with procedures that are simple enough to be automated, he said.
A few years ago Baran began to glimpse the possibility of achieving such a method. His lab had just succeeded in synthesizing a complex natural nitrogen heterocycle, palau'amine, a toxin made by sea sponges in the Western Pacific that has shown anticancer, antibacterial and antifungal pharmaceutical promise. As we developed an understanding of how that compound reacts, we recognized that it might help us solve this larger problem that discovery chemists face, he said.
The nitrogen atoms in heterocycles are what make them so tricky to handle. Traditional methods of modification typically aim to block their influence before the addition of any modifying molecules, but this approach can be cumbersome and expensive. The experience with palau'amine, which features an extremely challenging nine nitrogen atoms per molecule, led Baran and his team to try to find chemical reagents tools, in effect that would modify heterocycles directly.
A More Direct Route
Direct methods already had existed, but they often require extreme temperatures as well as expensive and hazardous reagents. During 2010 and 2011, Baran's lab experimented with several comparatively safe chemical reagents that can work in mild conditions to make commonly desired heterocycle modifications, such as the addition of a difluoromethyl group. One of these new reagents, a zinc dialkylsulfinate salt (DFMS) designed to transfer the difluoromethyl group, turned out to work particularly well. We quickly realized that we might be able to make related zinc sulfinate salts that would attach other functional groups to heterocycles, Baran said.
In the new report in Nature, Baran and his colleagues describe an initial toolkit consisting of ten of these zinc-based salts, each of which attaches a different functional group to a heterocycle framework. We selected these groups because they are commonly used by medicinal chemists, said Fionn O'Hara, PhD, a postdoctoral researcher in the Baran laboratory who was a first author of the new report with postdoctoral researcher Yuta Fujiwara, PhD, and technician Janice A. Dixon.
In many cases, chemists will be able to use these reagents sequentially to make more than one modification to a starting compound, noted Fujiwara. The groups that can be attached with the new reagents include trifluoromethyl, difluoromethyl, trifluoroethyl, monofluoromethyl, isopropyl and triethylene glycol monomethyl ether.
To demonstrate the ability of the reagents to work in biological media, Baran's team used them to difluoromethylate or trifluoromethylate heterocycles in a solution of cell lysate the contents of cells as well as to serve as a buffer medium, Tris, commonly used in lab-dish tests. To underscore the general robustness of the reagents, the team even carried out such modifications in a paper cup containing Oolong tea.
Baran's laboratory collaborated in the research with scientists from the pharmaceutical company Pfizer Inc. They provided
Most recent headlines
05/01/2027
Worlds first 802.15.4ab-UWB chip verified by Calterah and Rohde & Schwarz to be ...
07/10/2026
Dalet, a leading technology and service provider for media-rich organizations, today announced the latest Long-Term Supported (LTS) release of Dalet Flex. Build...
06/09/2026
June 9 2026, 23:00 (PDT) Dolby and MagentaTV Bring Fans Closer to the FIFA Worl...
19/08/2026
As the cost of IP nears price parity with traditional SDI, Reynolds argues that ...
19/08/2026
A private 5G bubble was chosen instead of traditional broadcast RF for the race ...
19/08/2026
(L-R) Rafael Manuel and Isabel Sicat attend the Filipi ana premiere during the 2026 Sundance Film Festival at The Ray Theatre on January 23, 2026, in Park Cit...
19/08/2026
Studio owners invited to have their say on rates cuts
The Music Producers Guild (MPG) are inviting UK-based studios to take part in an in-depth survey that ...
19/08/2026
Vintage-inspired desktop interface revealed
Harrison's latest hardware offering sees them head into the world of audio interfaces, delivering a 10-in/12...
19/08/2026
Granular effect remains locked to scale and tempo
Described as your dream granular effect , Minimal Audio's latest creation is capable of turning any s...
19/08/2026
First polyphonic SWAM instrument incoming
Audio Modeling's latest physical-modelling orchestral instrument is just around the corner, and is now availab...
19/08/2026
World Cup Games Generate 84 Billion Minutes Across FOX, Fox Sports 1 and NBCU...
19/08/2026
July brought typical peak-holiday drops in viewership, driven primarily by viewers stepping away from screens and a visible decline in reach across both traditi...
19/08/2026
Share
Copy link
Facebook
X
Linkedin
Bluesky
Email...
19/08/2026
Henry joins BCE as the company accelerates its commercial strategy and expands its international presence across the media, broadcast and technology markets. He...
19/08/2026
iWedia, a leading provider of software solutions for connected TV devices, today announced a major milestone in Android platform optimization with the successfu...
19/08/2026
NTP Technology announces that ST 2110-30 audio-over-IP connectivity with AES67 and RAVENNA capabilities is now available for the brand's world-class audio i...
19/08/2026
Net Insight has been selected to provide its Nimbra platform by the service provider Big Blue Marble, formerly ORS Group, as the core media transport solution f...
19/08/2026
LiveU has supported Coventry City FC and several other top-flight UK football clubs through one of their most demanding live production challenges of the year, ...
19/08/2026
Nature Seekers Documentary Shot with Blackmagic URSA Cine 12K LF
Brie Clayton August 18, 2026
0 Comments
Filming endangered turtles required camera...
19/08/2026
Neyrinck Brings D-Control Consoles Back to Life on Apple Silicon with D-Control ...
19/08/2026
Share
Copy link
Facebook
X
Linkedin
Bluesky
Email...
19/08/2026
Share
Copy link
Facebook
X
Linkedin
Bluesky
Email...
19/08/2026
Share
Copy link
Facebook
X
Linkedin
Bluesky
Email...
19/08/2026
Share
Copy link
Facebook
X
Linkedin
Bluesky
Email...
19/08/2026
Share
Copy link
Facebook
X
Linkedin
Bluesky
Email...
19/08/2026
Riedel Communications today announced that Edith Cowan University (ECU) in Perth, Australia, implemented a comprehensive communications infrastructure that brin...
19/08/2026
QuickLink, a leading provider of award-winning video production and remote guest contribution solutions, will spotlight a major leap forward in remote guest con...
19/08/2026
Integrated platform melds media asset management, playout automation and newsroom workflows
EMAM, PlayBox Neo and SNEWS have officially launched Nuvex, a conne...
19/08/2026
Screen Australia releases the Private Investment Toolkit to strengthen screen in...
19/08/2026
Do Aussies truly value local content? Unpacking Screen Currency 2026 with Deirdr...
19/08/2026
There's an early Christmas gift for Bookish fans, as UKTV confirms the re-commission of the hit U&alibi drama, created by and starring Mark Gatiss. Viewers ...
19/08/2026
Wednesday 19 August 2026
Sky gives sports fans the chance to watch multiple liv...
19/08/2026
On Saturday September 5 Katie Taylor will step into the ring for the fight of her life against Flora Pili in front of 80,000 fans in Croke Park. A legendary fig...
18/08/2026
SportStream 2026, a free three-day virtual event, will take place September 15-17. One registration provides access to all three days of live programming and on...
18/08/2026
BeckTV will introduce BeckFlow to the European market at IBC2026, demonstrated on the Providius stand (10.F53).
BeckFlow is a web-based schematic documentation...
18/08/2026
Boland Communications will introduce a SMPTE ST 2110 input option for its 4K monitors at IBC2026, along with a new 55-inch super-narrow bezel display for video ...
18/08/2026
Dolby Laboratories and the Seattle Seahawks have announced a partnership integrating Dolby OptiView into the Seahawks' live streaming coverage, making the S...
18/08/2026
For BMG Executive Producer of Sports Production, Graham Taylor, producing live s...
18/08/2026
TMRW Sports has appointed Rufus Hack as President of Golf, a newly created role in which he will lead the company's golf businesses including TGL presented ...
18/08/2026
SMT will provide race technology for FOX Sports' coverage of the Freedom 250 Grand Prix of Washington, D.C. on August 23, when the NTT INDYCAR SERIES races ...
18/08/2026
The live, YouTube-native roundtables combine fan voices, credentialed reporters,...
18/08/2026
Behind The Mic provides a roundup of recent news regarding on-air talent, includ...
18/08/2026
The industry legend sounds off on replacing the Heat's iconic Medusa score...
18/08/2026
William F. Rasmussen, the sports fan-turned broadcaster and entrepreneur whose out-of-the-box idea of a 24-hour cable sports network, ESPN, changed forever the ...
18/08/2026
DAZN Group has completed its acquisition of ViewLift, a provider of streaming and digital solutions for sports content owners. The acquisition was first announc...
18/08/2026
The American Association of Professional Baseball (AAPB) has added SI TV, Sports Illustrated's 24/7 streaming channel, as a broadcast partner for the remain...
18/08/2026
The Esports Foundation has announced that the inaugural Esports Nations Cup (ENC), originally scheduled for November 2026 in Riyadh, will be postponed to Novemb...
18/08/2026
Diversified has announced a new Global Managed Services Practice, consolidating the company's managed services capabilities into one organization. Rob Mello...
18/08/2026
Appear has completed a proof of concept with Thoroughbred Racing Productions (TRP), demonstrating multi-camera remote live production over bonded 5G cellular an...
Scripps Research Institute Chemists Invent Powerful Toolkit, Accelerating Creation of Potential New Drugs Method provides reactions so robust they can work in a paper cup containing Oolong tea
