Author Archive

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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Hybrid ligands targeting Aβ fibrillization for Alzheimer

Alzheimer disease is the most common form of dementia. It is a neurodegenerative disorder characterized by a progression from episodic memory problems to a slow global decline of cognitive function and it affects 10% of the people over the age of 65.

Unfortunately, the current treatments are  purely symptom-relieving and an actual treatment or prevention of Alzheimer is still lacking.

Ilona B. Bruinsma and her team at Nijmegen, The Netherlands, have designed bifunctional “β -sheet breakers” that interfere with the portions of the Aβ peptide known to contribute to aggregation and GAG interaction.

Read this interesting paper free to access from MedChemComm

A rational design to create hybrid β-sheet breaker peptides to inhibit aggregation and toxicity of amyloid-β 
Ilona B. Bruinsma, Anna Karawajczyk, Gijs Schaftenaar, Robert M. W. de Waal, Marcel M. Verbeek and Floris L. van Delft
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C0MD00213E

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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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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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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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