MedChemComm Symposium a great success!

The MedChemComm UK-China Symposium took place last month. The Symposium, organised by MedChemComm and the RSC International Programme, took place on the 22nd November at the Chemistry Centre in London.

Professor Zhenjun Yang presenting at the symposium

A great line-up of speakers gave presentations on topics from across the broad spectrum of medicinal chemistry. Dr Jason Wong (Roche R&D Centre, China) started off the day with his work on the development of a novel epigenetic modulator for hepatocellular carcinoma. Jason was followed by MedChemComm Editorial Board member Dr Mark Bunnage (Pfizer, UK), who talked about small molecule modulators of stem cells, and then Professor Zhenjun Yang (Peking University, China) reporting chemically modified siRNAs and their biological properties.

Dr Rich Soll (WuXi AppTec, China) opened up after lunch describing collaborative medicinal chemistry at WuXi AppTec, followed by Professor Paul Wyatt (University of Dundee, UK) describing some of his recent work developing antiparasitic leads. Rounding off the day were Professor Fa-Jun Nan (Shanghai Institute of Materia Medica, CAS, China), speaking about a hepatitis B inhibitor derived from a marine natural product, and Professor Chris Abell (University of Cambridge, UK), who spoke about anti-tuberculosis natural products.

Dr Richard Pike, CEO of the Royal Society of Chemistry and Professor Jingkang Shen, representing the Chinese Pharmaceutical Association, exchange gifts

Many thanks to the organising committee, the symposium sponsors – Pfizer and AstraZeneca – and everyone who attended.

Why not contribute to the success of MedChemComm by submitting your article today?

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Top ten most accessed articles in October

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

Silver nanoparticles – the real “silver bullet” in clinical medicine? 
Kenneth K. Y. Wong and Xuelai Liu 
Med. Chem. Commun., 2010, 1, 125-131, DOI: 10.1039/C0MD00069H, Review  

Targeting epigenetic modifiers: Inhibitors of histone methyltransferases 
Elisabeth-Maria Bissinger, Ralf Heinke, Wolfgang Sippl and Manfred Jung 
Med. Chem. Commun., 2010, 1, 114-124, DOI: 10.1039/C0MD00062K, Review  

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, Review  

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, 16-29, DOI: 10.1039/C0MD00055H, Review  

Boronic acids in medicinal chemistry: anticancer, antibacterial and antiviral applications 
Paul C. Trippier and Christopher McGuigan 
Med. Chem. Commun., 2010, 1, 183-198, DOI: 10.1039/C0MD00119H, Review  

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, DOI: 10.1039/C0MD00072H, Concise Article 

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, 1, 331-338, DOI: 10.1039/C0MD00148A, Concise Article  

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, Concise Article  

Aromatic chloride to nitrile transformation: medicinal and synthetic chemistry 
Lyn H. Jones, Nicholas W. Summerhill, Nigel A. Swain and James E. Mills 
Med. Chem. Commun., 2010, 1, 309-318, DOI: 10.1039/C0MD00135J, Review  

Selective inhibition of EGFR and VEGFR2 tyrosine kinases controlled by a boronic acid substituent on 4-anilinoquinazolines 
Hiroyuki Nakamura, Ryoji Horikoshi, Taikou Usui and Hyun Seung Ban 
Med. Chem. Commun., 2010, 1, 282-286, DOI: 10.1039/C0MD00115E, Concise Article 

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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HOT: Estrogen dependent breast cancer lead compound

Adam McCluskey and colleagues at The University of Newcastle have developed a library of compounds that can act as anti-cancer agents.

In this paper, they report the discovery of a family of 2-phenylacrylonitriles with excellent growth inhibition of a panel of ten human cancer cell lines.

Read this MedChemComm full paper free to access.

Library synthesis and cytotoxicity of a family of 2-phenylacrylonitriles and discovery of an estrogen dependent breast cancer lead compound
Mark Tarleton, Jayne Gilbert, Mark J. Robertson, Adam McCluskey and Jennette A. Sakoff
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C0MD00147C , Concise Article

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Meet the MedChemComm team

The MedChemComm team will be attending a number of conferences in 2011 and we would be delighted to meet you.

Here’s where you can meet us in the coming months:

Please let us know if you are planning on attending any of these meetings as it would be lovely to meet you there.

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Promising anabolic agent for bone disease

Chan Soo Shin, Seung Bum Park and colleagues at Seul National University in Korea have discovered a novel small-molecule bone anabolic agent with osteogenic effects.

The efficacy of this new benzopyranyl compound has been confirmed and evaluated both in vivo and in vitro.

Find out more about this promising anabolic agent for bone disease on our free to access MedChemComm article.


Discovery of a novel benzopyranyl compound as a potent in vitro and in vivo osteogenic agent

Sangmi Oh, Sun Wook Cho, Jae-Yeon Yang, Hyun Jin Sun, Young Sun Chung, Chan Soo Shin and Seung Bum Park
Med. Chem. Commun., 2010, Advance Article
DOI: 10.1039/C0MD00149J, Concise Article
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Top ten most accessed articles in September

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

Boronic acids in medicinal chemistry: anticancer, antibacterial and antiviral applications 
Paul C. Trippier and Christopher McGuigan 
Med. Chem. Commun., 2010, 1, 183-198, DOI: 10.1039/C0MD00119H , Review 

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, 16-29, DOI: 10.1039/C0MD00055H , Review 

Antivascular and anticancer activity of dihalogenated A-ring analogues of combretastatin A-4 
Thomas M. Beale, Rebecca M. Myers, James W. Shearman, D. Stephen Charnock-Jones, James D. Brenton, Fanni V. Gergely and Steven V. Ley 
Med. Chem. Commun., 2010, 1, 202-208, DOI: 10.1039/C0MD00095G , Concise Article 

Targeting epigenetic modifiers: Inhibitors of histone methyltransferases 
Elisabeth-Maria Bissinger, Ralf Heinke, Wolfgang Sippl and Manfred Jung 
Med. Chem. Commun., 2010, 1, 114-124, DOI: 10.1039/C0MD00062K , Review 

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 , Concise Article 

Design, synthesis, and structure–activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists 
Glenn Walker et al 
Med. Chem. Commun., 2010, 1, 54-60, DOI: 10.1039/C0MD00022A , Concise Article 

Redesigning the designer drug ecstasy: non-psychoactive MDMA analogues exhibiting Burkitt’s lymphoma cytotoxicity 
Matthew J. Piggott et al 
Med. Chem. Commun., 2010, 1, 287-293, DOI: 10.1039/C0MD00108B , Concise Article 

Selective inhibition of EGFR and VEGFR2 tyrosinekinases controlled by a boronic acid substituent on 4-anilinoquinazolines 
Hiroyuki Nakamura, Ryoji Horikoshi, Taikou Usui and Hyun Seung Ban 
Med. Chem. Commun., 2010, 1, 282-286, DOI: 10.1039/C0MD00115E , Concise Article 

Silver nanoparticles—the real “silver bullet” in clinical medicine? 
Kenneth K. Y. Wong and Xuelai Liu 
Med. Chem. Commun., 2010, 1, 125-131, DOI: 10.1039/C0MD00069H , Review 

Synthesis and biological evaluation of substituted α- and β-2,3-dihydrofuran naphthoquinones as potent anticandidal agents 
Cristina Pessoa Veloso Freire, Sabrina Baptista Ferreira, Nivea Suely Melo de Oliveira, Ani Beatriz Jackisch Matsuura, Ivson Lelis Gama, Fernando de C. da Silva, Maria Cecília B. V. de Souza, Emerson Silva Lima and Vitor Francisco Ferreira 
Med. Chem. Commun., 2010, 1, 229-232, DOI: 10.1039/C0MD00074D , Concise Article 

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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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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Extending the life of peptides

Christian Heinis and Lisa Pollaro talk about different strategies to prolong the in vivo plasma residence time of peptides.

Several strategies that extend the elimination half-life of peptides from minutes to several hours or even days are described in this interesting review.

You can read it for free here

Strategies to prolong the plasma residence time of peptide drugs
Lisa Pollaro and Christian Heinis
Med. Chem. Commun., 2010, Advance Article
DOI: 10.1039/C0MD00111B, Review

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