Archive for the ‘News’ Category

Poster Session at the 2013 Medicinal Chemistry Residential School

Sunday night saw the inaugural poster session at the 2013 RSC Medicinal Chemistry Summer School. In total 16 delegates presentPoster Session at the 2013 Medicinal Chemistry Residential Schooled their work on the evening. A broad spectrum of chemistry was discussed over a glass of wine and posters provided a great way to see the research interests of delegates. There were 2 poster prizes up for grabs – a 1 year subscription to MedChemComm  and a book from the RSC Books Drug Discovery Series.
On Monday morning, Andy Davis announced the winners; there was a tie for the MedChemComm sponsored Prize which was shared between:

  • Louis Allot ( University of Hull) for his work on PET imaging of nuclear receptor expression.
  • Kate Nicholson (University of Hull) for her work on synthesis and evaluation of novel coordination complexes as CXCR4 antagonists.

 Poster Session at 2013 Medicinal Chemistry Residential School

Delegates also had an opportunity to vote for their favourite poster, the winner of the “participants prize” went to Madura Jayatunga (University of Oxford) for his work on non-covalent and covalent inhibitors of the HIF1a-p300 interaction. Madura received the RSC Book PrizeNew Therapeutic Strategies for Type 2 Diabetes.

Thanks to our 2 judges Andy Davis and Roger Griffin; and of course everyone that took part!

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Chemistry skills for drug discovery

Chemistry expertise is critical to technical success across the spectrum of innovative medicines R&D. This position paper describes the changes that have taken place in the drug discovery sector and the challenges this presents in terms of ensuring chemistry, as the key enabling science, continues to deliver the essential translation of biological opportunity into clinical application.

It includes:

  • Impact of recent developments on training capacity and mobility
  • Key skills and capabilities for drug discovery chemists 

RSC-science-Drug discovery position paper

Read the full position paper by David Fox at RSC Science

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Take 1.. minute for chemistry in health

Take 1.. minute for chemistry in health

Do you know how chemical scientists can tackle global challenges in Human Health? If so, the RSC is running a one minute video competition this summer for young researchers such as PhD and Post-doc students; get involved and innovate the way scientists share their research. Your video should communicate your own personal research or an area of research that interests you, highlighting its significance and impact to Human Health.

Five videos will be shortlisted by our judging panel and the winner will be selected during the ‘How does chemistry keep us healthy?’ themed National Chemistry Week taking place 16-23 November.

A £500 prize and a fantastic opportunity to shadow the award winning video Journalist, Brady Harran, is up for grabs for the winner.

The judging panel will include the makers of The Periodic Tale of Videos, Martyn Poliakoff and Brady Harran, and RSC Division representatives.

Check out our webpage for further details of the competition and an example video.

The competition opened on 02 April 2013 and the closing date for entries is 01 July 2013. Please submit yours to rsc.li/take-1-video-competition.

The winner will be chosen and announced during National Chemistry week, 11-16 November 2013

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Chemical biology and medicinal: Ionic liquids could aid in the delivery of active pharmaceutical compounds in the body

US scientists have provided a strategy to improve the properties of active pharmaceutical ingredients (APIs) by combining ionic liquids (used to improve the properties of solid APIs) with prodrugs (used to improve solubility, permeability and bioavailability of APIs). The prodrug ionic liquids present additional advantages such as controlled release of the APIs in simulated body fluids. This work could offer an important strategy to improve the properties of APIs and drug delivery.

Prodrug ionic liquids: functionalizing neutral active pharmaceutical ingredients to take advantage of the ionic liquid form

Prodrug ionic liquids: functionalizing neutral active pharmaceutical ingredients to take advantage of the ionic liquid form
O. Andreea Cojocaru, Katharina Bica, Gabriela Gurau, Asako Narita, Parker D. McCrary, Julia L. Shamshina, Patrick S. Barber and Robin D. Rogers
MedChemComm, 2013
DOI: 10.1039/C3MD20359J

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Chemical biology and medicinal: Modulation of ghrelin signalling for the treatment of obesity

Scientists in the UK and Sweden have identified compounds that work against a ligand (ghrelin) that’s part of a growth hormone that’s thought to increase the amount of food we eat. The compounds could be used to prevent obesity and diabetes.

Ghrelin, a 28 amino acid acylated peptide hormone, is the endogenous ligand of growth hormone secretagogue receptor type 1a (GHS-R1a), and is thought to control food intake. Acylated ghrelin is released from mucosal cells in response to hunger cues, resulting in a peak of plasma ghrelin levels before meals. It has also been shown that ghrelin infusion in both rodents and humans increases appetite and food intake. Therefore, peripheral and central nervous system (CNS) penetrant ghrelin receptor antagonists could be a potential cure for obesity and diabetes.

In this work, the team identified a tool compound within a pyrazolo-pyrimidinone based series of GHS-R1a antagonists that had good overall properties and sufficient oral plasma and CNS exposure to demonstrate reduced food intake in mice through a mechanism involving GHS-R1a.

Graphical Abstract

Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity
William McCoull, Peter Barton, Anders Broo, Alastair Brown, David Clarke, Gareth Coope, Rob D M Davies, Alastair Dossetter, Elizabeth Kelly, Laurent Knerr, Philip Macfaul, Jane Holmes, Nathaniel Martin, Jane E Moore, David Morgan, Claire Newton,  Krister Osterlund, Graeme Robb, Eleanor Rosevere, Nidhal Selmi, Stephen Stokes, Tor Svensson, Victoria Ullah and Emma Williams
Med. Chem. Commun.
DOI: 10.1039/C2MD20340E

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MedChemComm Emerging Investigator Lectureship award – nominations now open!

Voting for the MedChemComm Emerging Investigator Lectureship is now open. This annual Lectureship recognises an emerging scientist who has made a significant contribution to medicinal chemistry or a related field in the early part of their independent career.

To make a nomination, please contact the MedChemComm Editorial Office with both the name and affiliation of the person you are nominating along with a brief description of why they should be considered. All members of the community are eligible to vote; however, nominated individuals must have published their work in MedChemComm in order to be eligible for entry. Nominees must also have completed their PhD on or after the 31st December 2002.

Closing date for Nominations is the 31st December 2012

The decision to award the Lectureship will be made by a panel of MedChemComm Editorial Board members. The receipient will receive a contribution towards speaking at a conference of their choice.

This year’s winner Dr Patrick Gunning, (University of Toronto, Canada) was presented with the Lectureship due to his prominent work into the investigation and manipulation of protein function. He will be presenting a lecture at an international conference in 2013.

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Chemical biology and medicinal: Optimising compounds for diabetes treatment

Scientists have optimised a series of compounds that have the potential to treat diabetes and obesity.
The drug candidates work by inhibiting the enzyme diacylglycerol acetyl transferase 1, which is responsible for catalysing the production of triglycerides. Excessive levels of triglycerides contribute to metabolic syndrome, which increases risk of diabetes, heart disease and stroke. Previous drug inhibitors have been unsuccessful in clinical trials due to low solubility. The optimised compounds are highly soluble and exhibit excellent potency for their target.

Graphical Abstract

Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 – the discovery of AZD2353
Michael J. Waring, Alan M. Birch, Susan Birtles, Linda K. Buckett, Roger J. Butlin, Leonie Campbell, Pablo Morentin Gutierrez, Paul D. Kemmitt, Andrew G. Leach, Philip A. MacFaul, Charles O’Donnell and Andrew V. Turnbull
Med. Chem. Commun., DOI: 10.1039/C2MD20190A

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Top 5 most downloaded articles

Take a look at the top 5 most downloaded MedChemComm articles in 2012 and blog your thoughts and comments below.

The developability of heteroaromatic and heteroaliphatic rings – do some have a better pedigree as potential drug molecules than others?
Timothy J. Ritchie, Simon J. F. Macdonald, Simon Peace, Stephen D. Pickett and Christopher N. Luscombe
Med. Chem. Commun., 2012,3, 1062-1069, DOI: 10.1039/C2MD20111A

Gd(III) chelates for MRI contrast agents: from high relaxivity to “smart”, from blood pool to blood–brain barrier permeable
Chang-Tong Yang and Kai-Hsiang Chuang
Med. Chem. Commun., 2012,3, 552-565, DOI: 10.1039/C2MD00279E

The use of phosphate bioisosteres in medicinal chemistry and chemical biology
Thomas S. Elliott, Aine Slowey, Yulin Ye and Stuart J. Conway
Med. Chem. Commun., 2012,3, 735-751, DOI: 10.1039/C2MD20079A

Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy
Silviya D. Furdas, Luca Carlino, Wolfgang Sippl and Manfred Jung
Med. Chem. Commun., 2012,3, 123-134, DOI: 10.1039/C1MD00201E

Development of second generation epigenetic agents
Philip Jones
Med. Chem. Commun., 2012,3, 135-161, DOI: 10.1039/C1MD00199J

Fancy submitting an article to MedChemComm? Then why not submit to us today or alternatively email us your suggestions.

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TamiGold and tubulin polymerization inhibitors on MedChemComm’s covers this month

Wecome to MedChemComm Issue 11, 2012

Featuring on the front cover of this issue of MedChemComm is the work of Hansjörg Streicher and colleagues who report the strong and selective binding of 2 types of gold nanoparticles, decorated with the oseltamivir (aka TamifluTM) pharmacophore, to wild-type and resistant influenza virus strains. Streicher et al. describe how the particles interact with the virus neuraminidase rather than the hemagglutinin and could serve as a vantage point for novel influenza virus sensors.

‘TamiGold’: phospha-oseltamivir-stabilised gold nanoparticles as the basis for influenza therapeutics and diagnostics targeting the neuraminidase (instead of the hemagglutinin)
Mathew Stanley, Nicholas Cattle, John McCauley, Stephen R. Martin, Abdul Rashid, Robert A. Field, Benoit Carbain and Hansjörg Streicher
DOI: 10.1039/C2MD20034A

The inside front cover illustrates work by Ahmed Kamal et al. (CSIR-Indian Institute of Chemical Technology, Hyderabad), who have synthesized a new series of tetrazole based isoxazolines that show promising activity as tubulin polymerization inhibitors that could be developed for the treatment of cancer.

Synthesis of tetrazole–isoxazoline hybrids as a new class of tubulin polymerization inhibitors
Ahmed Kamal, A. Viswanath, M. Janaki Ramaiah, J. N. S. R. C. Murty, Farheen Sultana, G. Ramakrishna, Jaki R. Tamboli, S. N. C. V. L. Pushpavalli, Dhananjaya pal, Chandan Kishor, Anthony Addlagatta and Manika pal Bhadra
DOI: 10.1039/C2MD20085F

Enjoy FREE access to both articles for the next 6 weeks

Also in this issue, why not read  the following 2 review articles:

Small molecules targeting phosphoinositide 3-kinases
Peng Wu and Yongzhou Hu
Med. Chem. Commun., 2012, 3, 1337-1355
DOI: 10.1039/C2MD20044A

Diaryl ether derivatives as anticancer agents – a review
Florence Bedos-Belval, Anne Rouch, Corinne Vanucci-Bacqué and Michel Baltas
Med. Chem. Commun., 2012, 3, 1356-1372
DOI: 10.1039/C2MD20199B

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Top ten most accessed articles in July 2012

This month sees the following articles in MedChemComm that are in the top ten most accessed:

The developability of heteroaromatic and heteroaliphatic rings – do some have a better pedigree as potential drug molecules than others?
Timothy J. Ritchie, Simon J. F. Macdonald, Simon Peace, Stephen D. Pickett and Christopher N. Luscombe
Med. Chem. Commun., 2012, 3, 1062-1069
DOI: 10.1039/C2MD20111A

The use of phosphate bioisosteres in medicinal chemistry and chemical biology
Thomas S. Elliott, Aine Slowey, Yulin Ye and Stuart J. Conway
Med. Chem. Commun., 2012, 3, 735-751
DOI: 10.1039/C2MD20079A

Gd(III) chelates for MRI contrast agents: from high relaxivity to “smart”, from blood pool to blood–brain barrier permeable
Chang-Tong Yang and Kai-Hsiang Chuang
Med. Chem. Commun., 2012, 3, 552-565
DOI: 10.1039/C2MD00279E

Property based optimisation of glucokinase activators – discovery of the phase IIb clinical candidate AZD1656
Michael J. Waring, David S. Clarke, Mark D. Fenwick, Linda Godfrey, Sam D. Groombridge, Craig Johnstone, Darren McKerrecher, Kurt G. Pike, John W. Rayner, Graeme R. Robb and Ingrid Wilson
Med. Chem. Commun., 2012, 3, 1077-1081
DOI: 10.1039/C2MD20077E

A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for heterocyclic replacements of di-substituted benzene containing compounds – identification of those isosteres more likely to have beneficial effects
Alexander G. Dossetter, Adam Douglas and Charles O’Donnell
Med. Chem. Commun., 2012, 3, 1164-1169
DOI: 10.1039/C2MD20155K

Small molecules targeting phosphoinositide 3-kinases
Peng Wu and Yongzhou Hu
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C2MD20044A

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011, 2, 1135-1161
DOI: 10.1039/C1MD00134E

On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin
Vincent Mascitti, Benjamin A. Thuma, Aaron C. Smith, Ralph P. Robinson, Thomas Brandt, Amit S. Kalgutkar, Tristan S. Maurer, Brian Samas and Raman Sharma
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C2MD20163A

Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists
James S. Scott, Alan M. Birch, Katy J. Brocklehurst, Hayley S. Brown, Kristin Goldberg, Sam D. Groombridge, Julian A. Hudson, Andrew G. Leach, Philip A. MacFaul, Darren McKerrecher, Ruth Poultney, Paul Schofield and Per H. Svensson
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C2MD20130E

Editorial: natural products themed issue
Sylvie Garneau-Tsodikova and Christopher T. Walsh
Med. Chem. Commun., 2012, 3, 852-853
DOI: 10.1039/C2MD90031A

Why not take a look at the articles today and blog your thoughts and comments below.

Fancy submitting an article to MedChemComm? Then why not submit to us today or alternatively email us your suggestions.

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