Archive for the ‘News’ Category

Call for papers – MedChemComm Natural Products themed issue

We are delighted to announce a special themed issue of MedChemComm on Natural Products, due for publication in summer 2012

This themed issue, guest edited by Professor Christopher T. Walsh and Dr Sylvie Garneau-Tsodikova will collect together in one place some of the latest exciting research natural products chemistry, including, but not limited to: biosynthesis, novel natural products as drug or drug leads, novel technologies for natural products discovery, novel chemical transformations in natural product biosynthesis, as well as chemical and chemoenzymatic synthesis of natural products. Authors will benefit from increased exposure of their research alongside similar high level and cutting edge work.

Deadline for Submission: January 31, 2012. Although publication of the issue is scheduled for summer 2012, web publication of the Advance Article versions of each manuscript will proceed as soon as the article is ready, ensuring that research is disseminated without delay.

Manuscripts can be submitted using the online web submissions service at http://mc.manuscriptcentral.com/mcc. Please indicate on submission in the comments to editor section that your manuscript is invited and intended for the Natural Products themed issue.

For more information please contact the Editorial Office.

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

MedChemComm’s Most Cited

Take a look at MedChemComm‘s most cited articles so far. As with all of our articles, you can enjoy free access to these for the remainder of 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
GA

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
GA

Silver nanoparticles—the real “silver bullet” in clinical medicine?
Kenneth K. Y. Wong and Xuelai Liu
Med. Chem. Commun., 2010, 1, 125-131
GA

Cytotoxic sugar analogues of an optimized novobiocin scaffold
Alison C. Donnelly, Huiping Zhao, Bhaskar Reddy Kusuma and Brian S. J. Blagg
Med. Chem. Commun., 2010, 1, 165-170
GA

Photografted poly(methyl methacrylate)-based high performance protein microarray for hepatitis B virus biomarker detection in human serum
Yingshuai Liu, Weihua Hu, Zhisong Lu and Chang Ming Li
Med. Chem. Commun., 2010, 1, 132-135
GA

Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design
Hengmiao Cheng, Shubha Bagrodia, Simon Bailey, Martin Edwards, Jacqui Hoffman, Qiyue Hu, Robert Kania, Daniel R. Knighton, Matthew A. Marx, Sacha Ninkovic, Shaoxian Sun and Eric Zhang
Med. Chem. Commun., 2010, 1, 139-144
GA

Effect of particle shape on phagocytosis of CdTe quantum dot–cystine composites
Zhisong Lu, Yan Qiao, Xin Ting Zheng, Mary B. Chan-Park and Chang Ming Li
Med. Chem. Commun., 2010, 1, 84-86
GA

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

MedChemComm delighted to meet authors!

The Royal Society of Chemistry was present in Anaheim for the ACS Spring 2011 National Meeting and Exposition last March. Very hectic few days full of Journal celebrations, product demos and workshops.

We were very happy to hear that one of our MedChemComm authors, Jose Medina Franco, paid the RSC booth a visit.
Here you can see him with a copy of MedChemComm Issue 1, where his article was published.

Thanks to Jose for dropping by! You can now read his article, which is free to access here.

Structure–activity relationships of benzimidazole derivatives as antiparasitic agents: Dual activity-difference (DAD) maps
Jaime Pérez-Villanueva, Radleigh Santos, Alicia Hernández-Campos, Marc A. Giulianotti, Rafael Castillo and Jose L. Medina-Franco
Med. Chem. Commun., 2011, 2, 44-49
DOI: 10.1039/C0MD00159G

If you want to find out where we are going this year and you want to come and meet us, like Jose did, we would love to hear from you. These are the list of conferences we are planning to go to:

  • Lakeland Heterocyclic meeting, May – Grasmere, UK
  • ACS National Organic Symposium – 5th – 9th June – Princeton, US
  • Frontiers in Medicinal Chemistry Meeting: Emerging Targets, Novel Candidates and Innovative Strategies- 19th-21st July – Stockholm, Sweden 
  • International Symposium on Macrocyclic and Supramolecular Chemistry (ISMSC) – 3rd-7th July, Brighton, UK
  • European Symposium on Organic Chemistry – 10th-15th July, Crete, Greece 
  • 22nd International Symposium: Synthesis in Organic Chemistry – 11th-14th July, Cambridge, UK
  • OMCOS 16 – 24th-28th July – Shanghai, China
  • GRC Medicinal Chemistry – 7th – 12th August – New Hampshire, US
  • 4th International Symposium on Advances in Synthetic and Medicinal Chemistry – 21st-25th August, St Petersburg, Russia 
  • 242nd Meeting of the American Chemical Society- 27th – 31st August, Denver, US
  • 16th RSC-SCI Medicinal Chemistry meeting – 11th-14th September, Cambridge, UK
Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

RSC Residential School in Medicinal Chemistry – book your place now!

Don’t miss out on early bird registration for the RSC’s Residential School in Medicinal Chemistry, being held this year at Burleigh Court Conference Centre at Loughborough University on 4-8 July 2011.

For over 30 years this course has been regarded as the pre-eminent industry training course for medicinal chemists. It brings together cross-industry and cross-discipline practitioners to provide lectures, tutorials, workshops and case-studies illustrating modern drug discovery. This provides an excellent training opportunity for young medicinal chemists. The course also provides a refresher for those who are more experienced but wish to expand their knowledge or offers an introduction to drug design thinking for any scientist working in cross-functional discovery teams. In addition, the opportunity to network with and learn from highly experienced medicinal chemistry professionals is the unique feature of this training school. For the training content and list of course tutors, please see www.rsc.org/medchemtraining

The early bird registration for this event will close on 1st April (although standard registration will remain open until 13th May). Places can be secured quickly and simply via the online booking system. Please note that previous courses have been oversubscribed so please encourage interested parties to register early to be sure of their place!

To find course details, register online and download flyers visit: www.rsc.org/medchemtraining

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

MedChemComm Issue 3 is here

Welcome to MedChemComm Issue 3!

In this new issue, you’ll find a new collection of exciting papers on medicinal chemistry research, which you can download for free!

This month’s menu includes:

The importance of solvation in the design of ligands targeting membrane proteins

Repairing faulty genes by aminoglycosides: Identification of new pharmacophore with enhanced suppression of disease-causing nonsense mutations

Synthesis and anti HSV-1 evaluation of novel indole-3,4-diones

Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship

Scaffold-hopping from aminoglycosides to small synthetic inhibitors of bacterial protein biosynthesis using a pseudoreceptor model

The discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection

Synthesis and biological evaluation of novel ferrocenyl curcuminoid derivatives

Interactions of polysulfanes with components of red blood cells

Structure-based design, synthesis, and profiling of potent and selective neuronal nitric oxide synthase (nNOS) inhibitors with an amidinothiophene hydroxypiperidine scaffold

Carba-LNA modified siRNAs targeting HIV-1 TAR region downregulate HIV-1 replication successfully with enhanced potency

That is a great selection, isn’t it? We hope you enjoy it and you find it enlightening.

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Repairing faulty genes

Israeli scientists have developed compounds that could be better treatments for genetic diseases than current drugs.

Timor Baasov and his colleagues at the Israel Institute of Technology have improved compounds used to suppress faults in genes called nonsense mutations.

Nonsense mutations, which cause more than 1800 human diseases, are alterations in the genetic code that stop protein production prematurely, leading to truncated or nonfunctional proteins. Gene therapy is one treatment, but it’s had limited success. With suppression therapy, small molecules allow cells’ protein producing equipment to skip over nonsense mutations to restore the proteins. Aminoglycosides – antibiotic amine-modified sugars – are the only clinically available drug family known to be effective in suppression therapy, but at effective doses, the compounds have high human toxicity.


Two aminoglycoside derivatives were found to suppress alterations in the genetic code called nonsense mutations

Read the full story in Chemistry World
 
Link to journal article
Repairing faulty genes by aminoglycosides: Identification of new pharmacophore with enhanced suppression of disease-causing nonsense mutations
Jeyakumar Kandasamy, Dana Atia-Glikin, Valery Belakhov and Timor Baasov,
Med. Chem. Commun., 2011, DOI: 10.1039/c0md00195c

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

MedChemComm in The Korea Herald

MedChemComm article by Chung Sung-kee and co-workers has been highlighted in The Korea Herald.

A group of South Korean researchers said Monday that they found a way to use drugs to fight brain tumors that are currently treated with only surgery and chemotherapy.

You can read the whole story here and also download the article which is free to access here.

Preparation of blood-brain barrier-permeable paclitaxel-carrier conjugate and its chemotherapeutic activity in the mouse glioblastoma model
Juyoun Jin, Woo Sirl Lee, Kyeung Min Joo, Kaustabh K. Maiti, Goutam Biswas, Wanil Kim, Kyong-Tai Kim, Se Jeong Lee, Kang-Ho Kim, Do-Hyun Nam and Sung-Kee Chung
Med. Chem. Commun., 2011
DOI: 10.1039/C0MD00235F

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

New hepatitis C drug

Scientists in the UK have developed a compound to combat the hepatitis C virus that could be taken as a pill.

David Pryde and his team from Pfizer Global Research and Development, Sandwich, have made new compounds to activate a protein in the immune system called TLR7 – toll-like receptor 7 – which fights the infection. Toll-like receptors identify foreign DNA, such as a virus, and produce proteins that inhibit the virus’ replication.

300 million people suffer from hepatitis C worldwide. The virus that causes the disease resides in the liver and can lead to cirrhosis, with some sufferers requiring liver transplants. Current treatments only cure half of patients and are administered intravenously. Recent research has focused on increasing the effectiveness of the drugs and on developing oral treatments.

Pryde’s team made heterocyclic analogues based on the structure of purines, known activators of TLR7 and the basis of current oral drugs. ‘The most potent TLR7 agonists are purine-based,’ explains Pryde. ‘But we wanted to design potent non-purine based agonists to maximise the chances of avoiding any unwanted off-target pharmacology.’ 


The compounds activate a protein in the immune system, which fights hepatitis 

Read the full story in Chemistry World

The discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection
David C. Pryde, Thien-Duc Tran, Peter Jones, Gemma C. Parsons, Gerwyn Bish, Fiona M. Adam, Mya C. Smith, Donald S. Middleton, Nick N. Smith, Frederick Calo, Duncan Hay, Michael Paradowski, Katie J. W. Proctor, Tanya Parkinson, Carl Laxton, David N. A. Fox, Nigel J. Horscroft, Giuseppe Ciaramella, Hannah M. Jones, Jonathan Duckworth, Neil Benson, Anthony Harrison and Rob Webster.
Med. Chem. Commun., 2011, DOI: 10.1039/c0md00197j
Link to journal article

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

MedChemComm Issue 2 published on line- Free access!

Our second issue of MedChemComm 2011 is here already!

This new and exciting issue comes with two reviews.
The first one by Paul Leeson and collegues on the impact of ion class and the time on the properties of oral drugs and the second one by Peter Kovacic and Ratnasamy Somanathan on the mechanisms of aromatic primary amines and the influence on the physiological activity.

The issue also contains six vibrant concise articles that bring you the best medicinal chemistry research.
From 2D and 3D activity landscape representations to imaging contrast agents. For those of you who are more synthetic medchems you can find articles on the synthesis and biological activities of AA-Trp-Trp-OBzl and isoquinolones. We close the issue with a study of activation energies and their influence in the stability of drugs and a final article on HIV-integrase inhibitors.

What do you think? We would like to receive your feedback on the new RSC medicinal chemistry journal MedChemComm!

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

New antibiotics repair faulty genes

Many genetic diseases, such as cystic fibrosis and muscular dystrophy, are caused by DNA mutations that terminate protein synthesis in the mutant gene. Aminoglycoside based antibiotics have been shown to stop these mutations but are often toxic and cause unpleasant side-effects in patients.   

Now Timor Baasov and colleagues have designed and synthesised new aminoglycoside derivatives that show enhanced targeting and reduced cell toxicity, compared with the leading antibiotic gentamicin. Baasov’s compounds contain a chiral methyl group at the side-chain of the ribosamine ring, which they claim could be an essential feature responsible for the compound’s biological activity.

These findings could have immediate therapeutic applications for the treatment of many genetic diseases and could also aid treatment of several types of cancer caused by DNA mutations.

Download this paper for free now!

Repairing faulty genes by aminoglycosides: Identification of new pharacophore with enhanced suppression of disease-causing nonsense mutations.  
Jeyakumar Kandasamy, Dana Atia-Gilkin, Valery Belakhov and Timor Baasov 
Med.Chem. Commun, 2011, Advance Article, DOI: 10.1039/C0md00195c

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)