Archive for the ‘News’ Category

MedChemComm Issue 1 2011 is now published!

Welcome to MedChemComm Issue 1 of the New Year!

 

2011 is going to be a very exciting year for MedChemComm and you will still be able to read all our content for free until the end of the year. You just need to register for a RSC personal account.
We also encourage you to keep up-to-date with the latest news by following us on Twitter, signing up for our e-alerts and receiving MedChemComments (our newsletter) in your inbox.

Don’t forget to keep an eye on the MedChemComm Blog! You can also sign up for our RSS feed.

Without further delay, here you have the first issue of 2011.

We start the year with a great selection of articles, including ‘Proteochemometric Modeling as a Tool to Design Selective Compounds and Extrapolating to Novel Targets’ by Andreas Bender et al. and ‘Evaluation of FR901464 analogues in vitro and in vivo’ by Kazunori Koide et al.

I hope you find the articles interesting and you consider submitting your research to MedChemComm in the near future.

From the MedChemComm editorial office we wanted to wish a very happy New Year to all our readers, authors and referees and a very successful one in medicinal chemistry.

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MedChemComm is now indexed in ISI

We are really pleased to say that MedChemComm is now being indexed in ISI Web of Science.

Issue 1 is already there and some of the articles have already been cited. Congratulations to Jean-Louis Reymond, Julia M. Adam, Franco Chimenti and Zhisong Lu and their research teams for being the first cited authors of MedChemComm in ISI.

Remember that you can now read all these articles for free!

Happy Holidays and best wishes for 2011!

Chemical space as a source for new drugs
Jean-Louis Reymond, Ruud van Deursen, Lorenz C. Blum and Lars Ruddigkeit
Med. Chem. Commun., 2010, 1, 30-38
DOI: 10.1039/C0MD00020E

Design, synthesis, and structure–activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists
Julia M. Adam, Jim Cairns, Wilson Caulfield, Phillip Cowley, Iain Cumming, Morag Easson, Darren Edwards, Morag Ferguson, Richard Goodwin, Fiona Jeremiah, Takao Kiyoi, Ashvin Mistry, Elizabeth Moir, Richard Morphy, Jason Tierney, Mark York, James Baker, Jean E. Cottney, Andrea K. Houghton, Paul J. Westwood and Glenn Walker
Med. Chem. Commun., 2010, 1, 54-60
DOI: 10.1039/C0MD00022A

Synthesis and selective inhibition of human monoamine oxidasesof a large scaffold of (4,5-substituted-thiazol-2-yl)hydrazones
Franco Chimenti, Daniela Secci, Adriana Bolasco, Paola Chimenti, Arianna Granese, Simone Carradori, Melissa D’Ascenzio, Matilde Yáñez and Francisco Orallo
Med. Chem. Commun., 2010, 1, 61-72
DOI: 10.1039/C0MD00014K

Effect of particle shape on phagocytosisof CdTe quantum dot–cystinecomposites
Zhisong Lu, Yan Qiao, Xin Ting Zheng, Mary B. Chan-Park and Chang Ming Li
Med. Chem. Commun., 2010, 1, 84-86
DOI: 10.1039/C0MD00008F

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MedChemComm in ISI

This week the MedChemComm team received the news that the journal has been accepted into ISI products by Thomson Reuters. In the next month you will be able to see MedChemComm listed in the following product:

* Science Citation Index Expanded
* Chemistry Citation Index
* Biological Abstracts
* BIOSIS Previews

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Analysis of public datasets of antimalarial “hits” and drugs

Sean Ekins and Tony Williams examine molecular properties across datasets of antimalarial screening hit compounds and compare them with compounds screened against Mycobacterim tuberculosis to identify patterns, trends or relationships.

The antimalarial hits were also filtered with computational rules to identify potentially undesirable substructures. They were surprised that approximately 75–85% of these compounds failed one of the sets of filters that they applied during this work.

To find out more about their findings I invite you to read this article. If you have something to say,  you can comment on this blog.

Meta-analysis of molecular property patterns and filtering of public datasets of antimalarial “hits” and drugs
Sean Ekins and Antony J. Williams
Med. Chem. Commun., 2010, Advance Article
DOI: 10.1039/C0MD00129E, Concise Article

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Novel approach to high-throughput screening of molecules

Jason Kettle and colleagues at AstraZeneca in UK outline a simple and direct strategy for extraction of potentially high value reagents from patent and other medicinal literature.

This approach is based on fragmentation and analysis of molecules described in patent and medicinal chemistry literature. They also highlight an example of key secondary amines with potential for broad applicability across medicinal chemistry.

Read it free to access.

Data-mining patent literature for novel chemical reagents for use in medicinal chemistry design
Jason G. Kettle, Richard A. Ward and Ed Griffen
Med. Chem. Commun., 2010, Advance Article
DOI: 10.1039/C0MD00148A, Concise Article

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Tumour detection takes an ultrasonic leap

By Philippa Ross

Hollow silica nanoparticles filled with gas behave as efficient contrast agents for use in ultrasound imaging. This could improve detection of tumours in breast cancer patients, claim US scientists.

Ultrasound imaging is a safe, fast and non-invasive technique used for medical diagnosis. However, one shortcoming is the inferior image contrast compared to more sophisticated magnetic resonance imaging (MRI). To improve this, radiologists use microbubble contrast agents to enhance the reflection of ultrasonic waves and therefore improve the quality of the ultrasound image, or radioactive seeds that are injected into the patient before surgery to visualise the entire tumour.
However, the contrast particles – normally comprised of a soft protein outer shell and a gas core – can be unstable due to their high sensitivity to changes in pressure, while the radioactive seeds have to be painfully injected into the patient and only last a few hours.

Now, a team led by William Trogler at the Univeristy of Califonia, San Diego have developed a stable, hard shell, hollow particle which, when filled with gas, produces a ultrasound signal and can be safely and painlessly injected into breast tissue to locate tumours. The gas-filled microbubbles adhere to human breast tissue for days and have a longer imaging lifetime than their soft counterparts, explains Trogler. So if used in early stage breast cancer patients, they could help surgeons better visualise the tumours and remove it all in one procedure.

Elizabeth Shaughnessy, a specialist in breast diseases at the University of Cincinnati in the US agrees. ‘The injection of these silica hollow spheres with gas-filled contrast provides a less toxic alternative, [to radioactive seeds] that won’t degrade within a short time period.’ She adds that the work is ‘highly innovative and will have great appeal to surgeons, radiologists and patients, as well as operating staff.

It is still early days but next Trogler and his team hope to move to animal models, toxicology studies and eventually clinical trials. Methods are also being developed to make biodegradable gas filled silica micro and nanoshells that would broaden the possible imaging applications.

This story has been published on the  Highlights in Chemical Biology website.

Read the paper free to access

Hard shell gas-filled contrast enhancement particles for colour Doppler ultrasound imaging of tumors
H. Paul Martinez, Yuko Kono, Sarah L. Blair, Sergio Sandoval, Jessica Wang-Rodriguez, Robert F. Mattrey, Andrew C. Kummel and William C. Trogler, Med. Chem. Commun., 2010, 1, 266
DOI: 10.1039/c0md00139b

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MedChemComm article by William Troger picked up in media outlets

The concise article by Robert F. Mattrey, Andrew C. Kummel, William Troger and colleagues at University of California, San Diego, on gas filled hollow porous silica microshells for ultrasound image contrast has had a tremendous impact in media outlets worldwide. This article is now included in MedChemComm Issue 4 and as all the MedChemComm content, it is free to access.

These are some of the web pages in which the article has been highlighted:

Congratulations to the authors! It is a truly interesting piece of research.

You can read it for free here:

Hard shell gas-filled contrast enhancement particles for colour Doppler ultrasound imaging of tumors
H. Paul Martinez, Yuko Kono, Sarah L. Blair, Sergio Sandoval, Jessica Wang-Rodriguez, Robert F. Mattrey, Andrew C. Kummel and William C. Trogler
Med. Chem. Commun., 2010, 1, 266-270
DOI: 10.1039/C0MD00139B , Concise Article

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MedChemComm poster prize winner

Congratulations go to Dr Oliver Schwardt from the University of Basel, Switzerland, who won the MedChemComm poster prize at the recent EFMC-ISMC meeting in Brussels, Belgium. Dr Schwardt wins an RSC book and a year’s subscription to the journal.

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Interview with Mark Bunnage: Medically speaking

Mark Bunnage talks to Leanne Marle about pharmaceuticals, chemologics and economics

Mark Bunnage is executive director of worldwide medicinal chemistry at Pfizer in Sandwich, UK. His areas of responsibility include chemistry leadership for regenerative medicine. He is also a member of the Executive Committee of the European Federation for Medicinal Chemistry (EFMC) and an editorial board member for MedChemComm. 

What led you into a career in medicinal chemistry?
I did a doctorate in organic chemistry at the University of Oxford, UK, followed by a post doc in total synthesis in the US. I guess I wanted to apply my skills as an organic chemist to help come up with new medicines – it seemed a really exciting way to put my training and skills to good use. This attracted me to the pharmaceutical industry and to join Pfizer.

What do you find most exciting about medicinal chemistry?
It feels a great privilege to be able to design and synthesise molecules that have never existed before. It is a genuine invention and very exciting to discover new molecules that can modulate human biology to potentially treat disease. This is a great way to apply chemistry and one of the best things about my job is that every day I’m learning new science. The field of medicinal chemistry is evolving quite significantly – so it’s a constant learning environment which is great fun. But the ultimate success is new medicines which can help people so it’s motivating from both the science and the application.

What projects are you working on at the moment?
One of the things we’re working on at the moment is regenerative medicine and the potential of stem cells as therapies. There’s a great opportunity for chemistry to influence this area of research by identifying small molecules that can modulate how stem cells behave. This could be to help generate viable cell therapy products or to find small molecule oral drugs that can influence stem cells to become new cell types and cause regeneration. It’s a cutting edge area in which chemistry is playing an important role.

One project the regenerative medicine group is working on is the treatment of blindness caused by age related degeneration of the cells in the eye. Basically if you could get a cell therapy to replace the retinal pigmented epithelial cells you could potentially restore sight.

What are the current challenges facing drug discovery?
Everyone recognises that the pharmaceutical industry has significant productivity challenges in terms of the number of new drug approvals each year relative to the R&D investment. One of the big reasons that we’ve not been as successful as we might is that we don’t always select the right target, so you can put a lot of investment in and take a quality molecule all the way to a Phase II clinical study but it doesn’t work. As an industry we’ve got to get much better at selecting molecular targets that can really influence disease. We really need to embrace chemical biology because the tools of chemical biology can help make the link between target and disease, and there are some cracking breakthroughs in this area of science that can now be applied in that sense.

This is why we’ve established a dedicated chemical biology group at Pfizer in Sandwich to really apply chemical biology with that aim. Selecting the target to work on is probably the most important decision we make and chemical biology can help with that. In addition, we are also applying the synthetic approaches of chemical biology to generate novel ‘chemologic’ therapeutics that are at the interface between small molecules and large.

What achievement are you most proud of?
One project that I’ve been involved in and that I’m excited about is a new treatment for respiratory disease that is in Phase II trials and is looking promising. There is still a major medical need to treat diseases such as asthma and chronic obstructive pulmonary disease and we’ve hopefully got quite an interesting inhaled product that will make a good addition to treatment options for patients.

You’re on the Editorial Board for the new RSC Journal MedChemComm, how did you get involved?
I’m also involved with the EFMC and the RSC approached us when they were thinking about a medicinal chemistry journal, so we partnered with the RSC to bring forward MedChemComm. We recognised it as a real opportunity for a quality new journal in the field of medicinal chemistry, and particularly one that perhaps helps to drive the scientific agenda within our discipline by covering traditional medicinal chemistry but also going beyond this to illustrate some of the ways that medicinal chemistry is evolving. I was very excited about the opportunity and that’s why I agreed to join the Editorial Board.

As a child, what did you want to be when you grew up?
Well sadly, what I wanted to be when I was a teenager was an economist, which I now look back in horror at the thought of this! But thankfully I saw the light when I studied A-Level Chemistry and saw that there was much more fun to be had in chemistry than in economics. Especially with recent events I’m really glad I didn’t end up in economics!

Download his first (but not last) MedChemComm paper

Small molecule modulation of stem cells in regenerative medicine: recent applications and future direction
Timothy E. Allsopp, Mark E. Bunnage and Paul V. Fish, Med. Chem. Commun., 2010, 1, 16
DOI: 10.1039/c0md00055h

See here the original interview

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MedChemComm at the 21st EFMC-ISMC Symposium

MedChemComm was at the 21st International Symposium on Medicinal Chemistry in Brussels last week. The meeting, organised by the journal’s official partner the European Federation for Medicinal Chemistry, was a great success, especially the MedChemComm reception on the Tuesday afternoon. We’d like to thank everyone who attended the reception and hope that you had a great time.

The MedChemComm reception at the 21st EFMC-ISMC meeting

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