RSC Medicinal Chemistry Blog

Promising anabolic agent for bone disease

19 Nov 2010

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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MedChemComm in ISI

03 Nov 2010

By Richard Kelly.

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

25 Oct 2010

By Lorena Tomas Laudo.

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

25 Oct 2010

By Lorena Tomas Laudo.

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

25 Oct 2010

By Lorena Tomas Laudo.

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

21 Oct 2010

By Lorena Tomas Laudo.

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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Reviews in MedChemComm in 2010

18 Oct 2010

By Richard Kelly.

MedChemComm publishes Review articles on key topics across the breadth of medicinal chemistry. Take a look below at those published so far in 2010, or contact the Editor, Richard Kelly, if you have an idea for a Review of your own!

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

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

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

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

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

Recent advances in the chemistry and biology of stable synthetic Lipoxin analogues
Colm D. Duffy and Patrick J. Guiry
Med. Chem. Commun., 2010, 1, 249-265

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, Advance Article

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MedChemComm article by William Troger picked up in media outlets

05 Oct 2010

By Lorena Tomas Laudo.

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:

HealthImaging.com : http://www.healthimaging.com/index.php?option=com_articles&view=article&id=24183&division=hiit&division=hiit
Yahoo News: http://in.news.yahoo.com/139/20100920/981/tsc-gas-filled-silica-sphere-markers-can_1.html
Kenya Star: http://story.kenyastar.com/index.php/ct/9/cid/a1e025da3c02ca7c/id/687279/cs/1/
Division of Physical Sciences: flyproxy0.appspot.com/http/physicalsciences.ucsd.edu/
Newspolitan: http://www.newspolitan.com/india/sci-tech/2010/09/20/oneindia-Gas-filled-silica-sphere-markers-can-detect-breast-cancer-early
Highlights in Chemical Biology http://www.rsc.org/Publishing/Journals/cb/Volume/2010/11/Tumour_detection.asp
Chemistry World http://www.rsc.org/chemistryworld/index.asp

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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Top ten most accessed articles in August

27 Sep 2010

By Jackie Cockrill, Publishing Assistant.

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

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

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 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 article

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 article

Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates
Shanshan Yan, Marvin J. Miller, Timothy A. Wencewicz and Ute Mollmann
Med. Chem. Commun., 2010, 1, 145 – 148, DOI: 10.1039/c0md00015a, Concise article

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 article

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, DOI: 10.1039/c0md00063a, Concise article

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, DOI: 10.1039/c0md00032a, Concise article

Synthesis and biological evaluation of substituted alpha- and beta-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

Synthesis, modeling, and crystallographic study of 3,4-disubstituted-1,2,5-oxadiazoles and evaluation of their ability to decrease STAT3 activity
Dae-Seop Shin, Daniela Masciocchi, Arianna Gelain, Stefania Villa, Daniela Barlocco, Fiorella Meneghetti, Alessandro Pedretti, Young-Min Han, Dong Cho Han, Byoung-Mog Kwon, Laura Legnani and Lucio Toma
Med. Chem. Commun., 2010, 1, 156 – 164, DOI: 10.1039/c0md00057d, 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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RSC Medicinal Chemistry Blog

Promising anabolic agent for bone disease

Top ten most accessed articles in September

MedChemComm in ISI

Analysis of public datasets of antimalarial “hits” and drugs

Novel approach to high-throughput screening of molecules

Extending the life of peptides

Tumour detection takes an ultrasonic leap

Reviews in MedChemComm in 2010

MedChemComm article by William Troger picked up in media outlets

Top ten most accessed articles in August

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