RSC Medicinal Chemistry Blog

Recent HOT MedChemComm articles

25 Sep 2014

The following are HOT articles, as recommened by the reviewers of the articles. These have all been made free to access until 24th October:

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
Apirat Chaikuad, Andrew M. Petros, Oleg Fedorov, Jing Xu and Stefan Knapp
Med. Chem. Commun., DOI: 10.1039/C4MD00237G, Concise Article
From themed collection Epigenetics

Gold compounds as aquaporin inhibitors: new opportunities for therapy and imaging
Andreia de Almeida, Graça Soveral and Angela Casini
Med. Chem. Commun., DOI: 10.1039/C4MD00265B, Review Article

A novel surface-coated nanocarrier for efficient encapsulation and delivery of camptothecin to cells
Rie Wakabayashi, Ryutaro Ishiyama, Noriho Kamiya and Masahiro Goto
Med. Chem. Commun., DOI: 10.1039/C4MD00179F, Concise Article
From themed collection In celebration of Seiji Shinkai’s 70^th Birthday

Peptide HIV fusion inhibitors: modifications and conjugations
Wei Liu, Jianjun Tan, Mohammadreza Mohammadzad Mehryar, Zhiping Teng and Yi Zeng
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00214H, Review Article

3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors
Craig J. Kutz, Steven L. Holshouser, Ethan A. Marrow and Patrick M. Woster
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00283K, Concise Article
From themed collection Epigenetics

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Christian Heinis receives MedChemComm Lectureship at EFMC-ISMC

18 Sep 2014

By Richard Kelly.

Christian Heinis with MedChemComm Managing Editor Richard Kelly. Photograph: Fabien Venturi

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Medicinal Chemistry Residential School comes to Asia

15 Aug 2014

By James Anson.

Registration now open for Medicinal Chemistry Residential School 2014

With a 40 year history in the UK, the Royal Society of Chemistry Medicinal Chemistry Residential School has trained some of the world’s leading medicinal chemists working in the pharmaceutical industry. Now, for the first time, this highly successful course will be coming to Asia – from 20-23 November, Shangai, China.

Do you want to develop your medicinal chemistry skills?

This 3-day course strengthens excellence in medicinal chemistry by highlighting best practice and facilitating understanding of the factors governing modern drug discovery.

What you will learn

The course covers all aspects of drug discovery. A full list of themes is on our website. These topics will be explored through a varied programme of lectures, case histories, and hands-on tutorial sessions.

Who you will learn from

This is a truly unique opportunity for discussions and networking with peers and internationally recognised leaders in the field. See our list of prestigious speakers.

Registration is now open. There are limited spaces available on the course so make sure you register as soon as possible.

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Recent HOT MedChemComm articles

24 Jul 2014

By Judy Allen, Publishing Assistant.

Check out the following HOT articles, these have been made free to access for a limited time:

Recognition of diazirine-modified O-GlcNAc by human O-GlcNAcase
Andrea C. Rodriguez and Jennifer J. Kohler
Med. Chem. Commun., 2014,5, 1227-1234
DOI: 10.1039/C4MD00164H

Recognition of diazirine-modified O-GlcNAc by human O-GlcNAcase

Free to access until 21st August 2014

Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition
Phillip P. Sharp, Jean-Marc Garnier, David C. S. Huang and Christopher J. Burns
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00182F

Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition

Free to access until 21st August 2014

Beyond substrate analogues: new inhibitor chemotypes for glycosyltransferases
Lauren Tedaldi and Gerd K. Wagner
Med. Chem. Commun., 2014,5, 1106-1125
DOI: 10.1039/C4MD00086B

Beyond substrate analogues: new inhibitor chemotypes for glycosyltransferases

Free to access until 21st August 2014

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RSC Organic Division Poster Symposium 2014

04 Jul 2014

By James Anson.

RSC Organic Division Poster Symposium 2014, headline sponsored by F. Hoffmann-La Roche, Ltd.

The poster symposium, for final year organic chemistry PhD students, will take place at The Royal Society of Chemistry, Burlington House, London on Monday 01 December 2014.

The symposium offers final year PhD students a chance to showcase their research to their peers, leading academics and industrial chemists, and is open to all branches of organic chemistry. The symposium has a tradition of being the most competitive and highly regarded organic chemistry symposium for PhD students in the UK and ROI and we would like to thank F. Hoffmann-La Roche, Ltd. for their generous support of the event.

There will be a first prize of £500, two runner-up prizes of £250, and a “selected by Industry Prize”. Industrial delegates will make this selection by considering the research’s potential for application in an industrial context; the winner will also receive a prize of £500.

Closing date for submissions is Wednesday 01 October 2014.
For more information and to submit your abstract go to http://rsc.li/organic-poster

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European Federation for Medicinal Chemistry (EFMC) Awards

20 Jun 2014

By Judy Allen, Publishing Assistant.

Every two years the European Federation for Medicinal Chemistry (EFMC), a partner society of MedChemComm, honour three awards at the International Symposium on Medicinal Chemistry (EFMC-ISMC). Congratulations to the following winners of the EFMC EFMC Awards 2014!

Nauta Award for Pharmacochemistry
Professor Paul Leeson
GlaxoSmithKline, UK

UCB-Ehrlich Award for Excellence in Medicinal Chemistry
Professor Craig Crews
Yale University, Department of Chemistry, New Haven, USA

Prous Institute-Overton and Meyer Award for New Technologies in Drug Discovery
Professor György Ferenczy and Professor György Keseru
Research Centre for Natural Sciences, Hungarian Academy of Sciences, Budapest, Hungary

These awards acknowledge outstanding achievements in the field of Medicinal Chemistry.

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Make your journal work for you

10 Jun 2014

By James Anson.

Find out how to get the most from MedChemComm

Want to know about the latest research we publish in MedChemComm? Want to be told about upcoming themed issues, or the most read articles, or other journal news?

Here are a few ways you can stay in touch with us and all that is happening:

Most recent articles

Be informed about the latest articles published on our website by adding us to your RSS Feed.

Issue alerts

Get the table of contents of the latest issue of MedChemComm sent direct to you when we publish the issue.

News alerts

By joining our news alerts we can let you know about:

Up-coming themed collections (print & electronic)
Top Ten most accessed articles
Changes to our Editorial Board
Important news for the journal

Twitter

We can also be found on Twitter @MedChemComm, add us and say hello.

And of course you can always come back to this blog to find out about our journal news.

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Kinase 2014

05 Jun 2014

By James Anson.

A very successful Kinase 2014 was held on 19-20 May 2014 with some great talks and interesting perspectives being presented on the future of kinase inhibitor research.

Kinase 2014 Chinese Pharmaceutical Association delegation

Kinase 2014 CPA delegation

Eight VIP Chinese Pharmaceutical Association (CPA) delegates attended the Kinase 2014 held at the Babraham Research Institute in Cambridge. Three of the CPA delegates presented their research at the meeting which also included a lecture from Nathanael S Gray (Harvard), recent guest editor for Med Chem Comm themed issue “Chemical Biology for Target Identification and Validation”.

Along with the talks a series of posters were also presented. Two of these recieved Poster Prizes sponsored by the Chemistry Biology Interface Division (CBID) and MedChemComm.

Jeff Kropf (Gilead Sciences) won the MedChemComm prize for his research on the discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase (Syk).

Charlotte Griffiths-Jones (Astex Pharmaceuticals) won the CBID prize for her poster on fragment based drug discovery of selective inhibitors of fibroblast growth facter receptor (FGFR).

Jeff Kropf being presented with his poster prize

Charlotte Griffiths-Jones being presented with her CBID prize

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MedChemComm Lectureship – nominations now open!

30 May 2014

By Richard Kelly.

Nominations for the MedChemComm Emerging Investigator Lectureship are now open. This annual Lectureship recognises an emerging scientist who has made a significant contribution to medicinal chemistry or a related field in the early part of their independent career.

To make a nomination, please contact the MedChemComm Editorial Office with the name and affiliation of the person you are nominating. Nominees must have completed their PhD on or after the 31st December 2004.

Closing date for Nominations is the 30^th June 2014

The decision to award the Lectureship will be made by a panel of MedChemComm Editorial Board members. The recipient will receive a contribution towards speaking at a conference. Previous Lectureship winners are Professor Patrick Gunning (University of Toronto, Canada) and Professor Christian Heinis (École Polytechnique Fédérale de Lausanne, Switzerland).

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Targeting mitochondria with hydrogen sulfide donors

27 May 2014

By Stephen Moore.

Decreased biosynthesis of hydrogen sulfide is found in a range of disease states. In cell based assays, hydrogen sulfide can prevent oxidant-induced cell damage. Together, these findings suggest that strategies to increase hydrogen sulfide bioavailability may have potential in the treatment of disease states such as hypertension and diabetes.

A recent article published in MedChemComm reports the synthesis of a hydrogen sulfide donor molecule coupled to a triphenylphosphonium cation (AP39).

The effects of this molecule on oxidative stress were compared against a compound with known vasodilatory activity in a cellular model. Lipophilic cation, such as the triphenylphosphonium cation, can accumulate within mitochondria (the main source of detrimental oxidant production within cells). The cytoprotective potency of the synthesised compound was greater than that of the comparator, suggesting that compounds capable of delivering hydrogen sulfide to mitochondria may have therapeutic potential.

AP39 [(10-oxo-10-(4-(3-thioxo-3H-1,2-dithiol-5-yl)- phenoxy)decyl)triphenylphosphonium bromide] a mitochondria-targeted hydrogen sulfide donor

The synthesis and functional evaluation of a mitochondria-targeted hydrogen sulfide donor, (10-oxo-10-(4-(3-thioxo-3H-1,2-dithiol-5-yl)phenoxy)decyl)triphenylphosphonium bromide (AP39)
Sophie Le Trionnaire, Alexis Perry, Bartosz Szczesny, Csaba Szabo, Paul G. Winyard, Jacqueline L. Whatmore, Mark E. Wood and Matthew Whiteman
Med. Chem. Commun., 2014, DOI: 10.1039/C3MD00323J, Concise Article

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RSC Medicinal Chemistry Blog

Recent HOT MedChemComm articles

Christian Heinis receives MedChemComm Lectureship at EFMC-ISMC

Medicinal Chemistry Residential School comes to Asia

Recent HOT MedChemComm articles

RSC Organic Division Poster Symposium 2014

European Federation for Medicinal Chemistry (EFMC) Awards

Make your journal work for you

Kinase 2014

MedChemComm Lectureship – nominations now open!

Targeting mitochondria with hydrogen sulfide donors

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