RSC Medicinal Chemistry Blog

Highly selective agonist for the metabotropic glutamate receptor mGluR2

05 Oct 2011

Work from this international collaboration spanning Denmark, Italy, Sweden and the USA brings insights into the synthesis and characterization of a selective agonist for the metabotropic glutamate receptor mGluR2, a potential therapeutic target for neurologic and psychiatric diseases.

The team’s approach to the agonist design was to induce selectivity for mGluR2 over other family members via imposing conformational rigidity into the carbon skeleton of the Glu analogues. This resulted in an increase of selectivity of at least two orders of magnitude compared to homologous mGluR3 as well as mGluR1, 4, 5, 7.

A highly selective agonist for the metabotropic glutamate receptor mGluR2
Simon D. Nielsen, Marica Fulco, Michaela Serpi, Birgitte Nielsen, Maria B. Hansen, Kasper L. Hansen, Christian Thomsen, Robb Brodbeck, Hans Bräuner-Osborne, Roberto Pellicciari, Per-Ola Norrby, Jeremy R. Greenwood and Rasmus P. Clausen

Interested? Why not read this MedChemComm article now! All our content is currently FREE to access .

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Pyridazine-containing drugs and single-step labelling of a matrix metalloprotease inhibitor on the cover of MedChemComm Issue 10

05 Oct 2011

By Francesca Burgoyne.

Two hot articles feature on the cover of MedChemComm this month:

The outside front cover features the review from Camille Wermuth, Prestwick Chemical Inc., France, on the applications of pyridazine scaffolds for medicinal chemistry. This article has featured in our Top 10 lists for the last 3 months, so why not take a look at what everyone else has been reading?

Are pyridazines privileged structures?
Camille G. Wermuth
Med. Chem. Commun., 2011, 2, 935-941

The inside front cover is from Chris Overall and David Perrin, demonstrating a technique for easy production of ¹⁸F labelled marimastat, a clinically trialled breast cancer drug, with general applications for PET imaging.

Towards kit-like 18F-labeling of marimastat, a noncovalent inhibitor drug for in vivo PET imaging cancer associated matrix metalloproteases
Ying Li, Richard Ting, Curtis W. Harwig, Ulrich auf dem Keller, Caroline L. Bellac, Philipp F. Lange, James A. H. Inkster, Paul Schaffer, Michael J. Adam, Thomas J. Ruth, Christopher M. Overall and David M. Perrin
Med. Chem. Commun., 2011, 2, 942-949

Read the rest of the issue here

Towards kit-like ¹⁸F-labeling of marimastat, a noncovalent inhibitor drug for in vivo PET imaging cancer associated matrix metalloproteases

Ying Li, Richard Ting, Curtis W. Harwig, Ulrich auf dem Keller, Caroline L. Bellac, Philipp F. Lange, James A. H. Inkster, Paul Schaffer, Michael J. Adam, Thomas J. Ruth, Christopher M. Overall and David M. Perrin

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MedChemComm in the news

05 Oct 2011

By Francesca Burgoyne.

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

28 Sep 2011

By Richard Kelly.

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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Top ten most accessed articles in August

20 Sep 2011

By Nathalie Horner.

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

Molecular obesity, potency and other addictions in drug discovery
Michael M. Hann
Med. Chem. Commun., 2011, 2, 349-355
DOI: 10.1039/C1MD00017A

Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors
Frédéric Pin, Frédéric Buron, Fabienne Saab, Lionel Colliandre, Stéphane Bourg, Françoise Schoentgen, Remy Le Guevel, Christiane Guillouzo and Sylvain Routier
Med. Chem. Commun., 2011, 2, 899-903
DOI: 10.1039/C1MD00141H

Design, synthesis, and structure–activity relationships of 1,3,4-oxadiazol-2(3H)-ones as novel FAAH inhibitors
László E. Kiss, Humberto S. Ferreira, Alexandre Beliaev, Leonel Torrão, Maria João Bonifácio and David A. Learmonth
Med. Chem. Commun., 2011, 2, 889-894
DOI: 10.1039/C1MD00136A

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00134E

Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space
Alexander Alex, David S. Millan, Manuel Perez, Florian Wakenhut and Gavin A. Whitlock
Med. Chem. Commun., 2011, 2, 669-674
DOI: 10.1039/C1MD00093D

Are pyridazines privileged structures?
Camille G. Wermuth
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00074H

Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes
Jeffrey A. Pfefferkorn, Angel Guzman-Perez, Peter J. Oates, John Litchfield, Gary Aspnes, Arindrajit Basak, John Benbow, Martin A. Berliner, Jianwei Bian, Chulho Choi, Kevin Freeman-Cook, Jeffrey W. Corbett, Mary Didiuk, Joshua R. Dunetz, Kevin J. Filipski, William M. Hungerford, Christopher S. Jones, Kapil Karki, Anthony Ling, Jian-Cheng Li, Leena Patel, Christian Perreault, Hud Risley, James Saenz, Wei Song, Meihua Tu, Robert Aiello, Karen Atkinson, Nicole Barucci, David Beebe, Patricia Bourassa, Francis Bourbounais, Anne M. Brodeur, Rena Burbey, Jing Chen, Theresa D’Aquila, David R. Derksen, Nahor Haddish-Berhane, Cong Huang, James Landro, Amanda Lee Lapworth, Margit MacDougall, David Perregaux, John Pettersen, Alan Robertson, Beijing Tan, Judith L. Treadway, Shenping Liu, Xiayang Qiu, John Knafels, Mark Ammirati, Xi Song, Paul DaSilva-Jardine, Spiros Liras, Laurel Sweet and Timothy P. Rolph
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/c1md00116g

Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors
Brad E. Sleebs, Danny Ganame, Alla Levit, Ian P. Street, Alison Gregg, Hendrik Falk and Jonathan B. Baell
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00138H

Redesigning the designer drug ecstasy: non-psychoactive MDMA analogues exhibiting Burkitt’s lymphoma cytotoxicity
Michael N. Gandy, Matthew McIldowie, Katie Lewis, Agata M. Wasik, Danielle Salomonczyk, Keith Wagg, Zak A. Millar, David Tindiglia, Philippe Huot, Tom Johnston, Sherri Thiele, Blake Nguyen, Nicholas M. Barnes, Jonathan M. Brotchie, Mathew T. Martin-Iverson, Joanne Nash, John Gordon and Matthew J. Piggott
Med. Chem. Commun., 2010, 1, 287-293
DOI: 10.1039/C0MD00108B

Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors
Brad E. Sleebs, Alla Levit, Ian P. Street, Hendrik Falk, Tim Hammonds, Ai Ching Wong, Mark D. Charles, Michael F. Olson and Jonathan B. Baell
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00137J

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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Biocompatible nanovalves as smart therapeutics for cancer therapy – A Review

09 Sep 2011

By Marie Cote, Deputy Editor.

Biocompatible nanovalves can effectively store and protect drugs inside nano-reservoirs, then deliver and release them to kill targeted cancer cells under external stimuli. As such they are a promising example of smart materials that are devised to both address the controlled release of the therapeutics and selectively target diseased cells.

In this recent MedChemComm review article, Ying Wei Yang from Jilin University, Changchun (P.R China) provides a timely and comprehensive update on the recent progress of biocompatible nanovales based on mesoporous silica nanoparticles. The review highlights the cutting-edge progress in this field, with details of the nanovalves construction, therapeutic release mechanisms, while specifically focusing on the water-based systems for therapeutic applications.

Whether you are in the Medical, Materials or Chemistry field, this MedChemComm review is for you!

Free to access for the next 4 weeks.

Towards biocompatible nanovalves based on mesoporous silica nanoparticles Ying-Wei Yang
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00158B, Review

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Review: Practical use of Minisci reactions

09 Sep 2011

By Sarah Dixon.

In this MedChemComm review Matthew Duncton, Renovis Inc., highlights the attractive potential of Minisci reactions – addition of radicals to heteroaromatic bases – for medicinal and biological chemists.

These reactions can be used to introduce a broad-range of selective CH-functionalization groups, such as alkyls, cycloalkyls, sugars, esters and more. In many cases, these processes are highly chemo- and regio-selective, making them ideal for industrial applications, because complicating factors such as protecting group strategies can be avoided.

Graphical abstract: Minisci reactions: Versatile CH-functionalizations for medicinal chemists

Read this review now for specific examples and future developments of these useful reactions. It’s free to download for the next 4 weeks!

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton, Med. Chem. Commun., 2011, DOI: 10.1039/C1MD00134E

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RSC e-membership launched

02 Sep 2011

By Francesca Burgoyne.

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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Tubulin polymerization inhibitors on the cover of Issue 9

01 Sep 2011

By Marie Cote, Deputy Editor.

Welcome to MedChemComm Issue 9.

Ahmed Kamal and colleagues from the Indian Institute of Chemical Technology in Hyderabad (India) have devised a series of novel 2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives through simple synthetic schemes that exhibit potent anticancer efficacy via the inhibition of tubulin polymerisation, thus blocking mitotic division.

Interested? Why not read the article now! As with all our Cover articles, it will be FREE to access for the next 6 weeks.

2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization Ahmed Kamal, Y. V. V. Srikanth, Thokhir B. Shaik, M. Naseer A. Khan, Md. Ashraf, M. Kashi Reddy, K. Anil Kumar and Shasi V. Kalivendi
Med. Chem. Commun., 2011, 2, 819-823 DOI: 10.1039/C0MD00177E

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RSC Medicinal Chemistry Blog

Highly selective agonist for the metabotropic glutamate receptor mGluR2

Pyridazine-containing drugs and single-step labelling of a matrix metalloprotease inhibitor on the cover of MedChemComm Issue 10

MedChemComm in the news

First MedChemComm Accepted Manuscript published

Top ten most accessed articles in August

Biocompatible nanovalves as smart therapeutics for cancer therapy – A Review

Review: Practical use of Minisci reactions

RSC e-membership launched

Tubulin polymerization inhibitors on the cover of Issue 9

Top ten most accessed articles in July

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