Archive for the ‘News’ Category

Issue 1 2012 just published!

Happy New Year to all our readers and welcome to our first issue of 2012!

On the cover of this issue is work by John Spencer et al. on the synthesis of a small library of ferrocene-based HDAC inhibitors via click chemistry – click JAHAs.  This article is from our forthcoming web collection on Epigenetics, take a look at some of the other interesting articles published in this series.

Click JAHAs: conformationally restricted ferrocene-based histone deacetylase inhibitors
John Spencer, Jahangir Amin, Ramesh Boddiboyena, Graham Packham, Breeze E. Cavell, Sharifah S. Syed Alwi, Ronald M. Paranal, Tom D. Heightman, Minghua Wang, Brian Marsden, Peter Coxhead, Matthew Guille, Graham J. Tizzard, Simon J. Coles and James E. Bradner.
DOI: 10.1039/C1MD00203A

Also in this issue are reviews on polyamine-based epigenetic modulators, Stat5 signalling inhibitors, protein structure-based pharmacophore modeling and hot papers on the inhibition of E. coli DXP synthase and a glucuronide prodrug of doxorubicin.

View the rest of the issue here

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Nominations for the 2012 RSC Prizes and Awards now open

Nominations for the 2012 RSC Prizes and Awards close on the 15 January 2012

Our Prizes and Awards represent the dedication and outstanding achievements and are a platform to showcase inspiring science to gain the recognition deserved. Don’t forget to nominate colleagues who have made a significant contribution to advancing the chemical sciences.

View our full list of Prizes and Awards and use the online system to nominate a colleague.

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Drug-target residence times and covalent binders themed issue – call for papers

On behalf of Professor Dr Koen Augustyns (University of Antwerp), Guest Editor, we would like to invite authors to contribute to this themed issue which aims collect together in one place some of the latest exciting research from across the breadth of drug residence and covalent drug research.

Analysis of drug-target residence time has begun to play a larger role in drug discovery as suggested by recent literature. For compounds with a slow off rate, long action at the target may render a perfect pharmacokinetic profile unnecessary, and selectivity vs. other targets inhibited only briefly may be more readily achieved. Reversible and irreversible covalent binding drugs may be considered as the logical extreme for this approach. For other targets or therapeutic areas, other kinetic profiles may be desirable. Finally, there is a real need to build a better understanding in the medicinal chemistry community of the preferred profiles, screening methods, at which stage of a project lifetime to characterize the kinetics, and ideally a structural bases for design to achieve a desired kinetic profile.

-Koen Augustyns, Guest Editor

Authors will benefit from increased exposure of their research alongside similar high level and cutting edge work. In addition, as this is a web-based theme issue, printing of articles will not be held for a specific issue thereby allowing rapid dissemination of the science presented online and in print without delay. Both reviews and primary research are suitable for this issue.

The submission deadline for the web theme issue will be Monday 6th February 2012.

If you would like to contribute to this exciting themed issue, please contact the Editorial Office.

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Make the most of the last month of free access from MedChemComm

Free online access to MedChemComm will finish at the end of 2011, but there is still time to take a look at all the articles we’ve published so far free of charge.

Don’t know where to start?  Why not take a look at some of the top accessed articles over the last year:

Molecular obesity is weighing down drug discovery
Michael M. Hann, DOI: 10.1039/C1MD00017A

Michael Hann from GSK suggests that the search for potency can lead to drug molecules that are too large and liphophilic to make it to market, coining the term ‘molecular obesity‘ to describe the risk that this presents to the fitness of lead compounds.

Drugs that go beyond the rule of five – or do they?
Alexander Alex et al., DOI: 10.1039/C1MD00093D

David S. Millan and colleagues at Pfizer R&D explore the influence of intramolecular hydrogen bonding on the membrane permeability and bioavailability drugs which operate outside of the traditional rule of five – are they actually much closer to rule of five space than previously thought?


New antibiotics to repair faulty genes
Jeyakumar Kandasamy et al,. DOI: 10.1039/C0MD00195C

Timor Baasov and co-workers developed new aminoglycoside derivatives to suppress nonsense mutations, which result in a variety of genetic diseases, that show enhanced targeting and reduced cell toxicity compared to a leading antibiotic.

Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structure–activity relationship
Shoujun Chen et al., DOI: 10.1039/C0MD00215A

2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization
Ahmed Kamal et al., DOI: 10.1039/C0MD00177E

Impact of ion class and time on oral drug molecular properties
Paul D. Leeson, Stephen A. St-Gallay and Mark C. Wenlock, DOI: 10.1039/C0MD00157K

Structure–activity relationships of methyl-lysine reader antagonists
J. Martin Herold and Stephen V. Frye et al., DOI: 10.1039/C1MD00195G

New insight into the mode of action of vancomycin dimers in bacterial cell wall synthesis
Osamu Yoshida et al., DOI: 10.1039/C0MD00230E

If you would like to continue to receive access to MedChemComm in 2012 please contact sales@rsc.org and ask for a quote.

Additionally, why not consider submitting your next manuscript to the journal? We now also offer optional Accepted Manuscript publication, so that your manuscript is available faster in a citable form.

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Themed issue on Drug-Target Residence Times – deadline extended

We are pleased to inform our authors that we will be extending the submission deadline for our forthcoming drug-target residence times web theme issue to Monday 6th February 2012.

The issue will be guest edited by Professor Dr Koen Augustyns (University of Antwerp) and aims collect together in one place some of the latest exciting research from across the breadth of drug residence research.

Authors will benefit from increased exposure of their research alongside similar high level and cutting edge work. In addition, as this is a web-based theme issue, printing of articles will not be held for a specific issue thereby allowing rapid dissemination of the science presented online and in print without delay. Both reviews and primary research are suitable for this issue.

If you would like to contribute to this exciting themed issue, please contact the Editorial Office.

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Tracking immune cell migration on the cover of Issue 11

On the cover of Issue 11 is a hot article from Mark Bradley and coworkers on a method to track innate immune cell migration in vivo using dye-labelled peptoids.

Far red and NIR dye-peptoid conjugates for efficient immune cell labelling and tracking in preclinical models
Kevin Dhaliwal, Géraldine Escher, Asier Unciti-Broceta, Neil McDonald, A. John Simpson, Chris Haslett and Mark Bradley
Med. Chem. Commun., 2011, 2, 1050-1053
DOI: 10.1039/C1MD00171J

Also in this issue is Ying-Wei Yang’s review on biocompatible nanovalves for drug delivery and release:

Towards biocompatible nanovalves based on mesoporous silica nanoparticles
Ying-Wei Yang
Med. Chem. Commun., 2011, 2, 1033-1049
DOI: 10.1039/C1MD00158B

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MedChemComm in the news

Matthew Piggott’s MedChemComm article on modifying MDMA to treat cancer cells has been picked up by an American news website, First Coast News.  The article also appeared in our August Top 10 list, so congratulations to the authors!

Read the news story here or go straight to the original research article, Redesigning the designer drug ecstasy: non-psychoactive MDMA analogues exhibiting Burkitt’s lymphoma cytotoxicity

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First MedChemComm Accepted Manuscript published

The first MedChemComm “Accepted Manuscript” is now published. Jacqueline Marchand-Brynaert (Université catholique de Louvain, Belgium) and colleagues’ article is now available to download.

All MedChemComm authors now have the opportunity to have the unedited version of their article published shortly after acceptance, meaning that results are now published, in citable form, even earlier than before. More details…..

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RSC e-membership launched

This week, the RSC launched a new product, RSC e-membership, allowing anyone to access an electronic version of Chemistry World through a MyRSC account and to enjoy the benefits of electronic networking via this professional online community for £20/year.

Subscribers to this do not benefit from the professional recognition or any of the other many services and discounts available to RSC Members, but it allows chemists from around the world, many already members of another chemical society in their own country, to benefit from the highly-esteemed content in Chemistry World and the networking opportunities offered from MyRSC, which now stands at over 11,000 members. The RSC e-membership also allows subscribers to join a virtual specialist interest group on MyRSC. If you are interested in joining, please visit www.rsc.org/emembership.

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MedChemmComm article on PAM in the press

MedChemComm has been making the headlines again!

The recently published article by Chris Easton and colleagues at the Australian National University entitled “Potent and selective inhibitors of human peptidylglycine α-amidating monooxygenase”  was picked-up by several news outlets, including Medical News Today:

Love Hormone Oxytocin Inspires New Small-cell Lung Cancer Treatment Research
One in Every 28 Australians Are Diagnosed With Lung Cancer, Says Study
Lung cancer breakthrough yields new love hormone insights
Sex gives clues to new lung cancer treatment
Enzyme PAM Linked to Small Cell Lung Cancer: Study

Congratulations to Professor Easton and team!

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