RSC Medicinal Chemistry Blog

Recent HOT MedChemComm articles

24 Jul 2014

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

Comments Off on Recent HOT MedChemComm articles

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

Comments Off on RSC Organic Division Poster Symposium 2014

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.

Comments Off on European Federation for Medicinal Chemistry (EFMC) Awards

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.

Comments Off on Make your journal work for you

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

Comments Off on Kinase 2014

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).

Comments Off on MedChemComm Lectureship – nominations now open!

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

Comments Off on Targeting mitochondria with hydrogen sulfide donors

Q1 Top Ten most accessed MedChemComm articles

20 May 2014

By Judy Allen, Publishing Assistant.

Please take a look at the following articles which were the Top Ten most accessed during January, February and March!

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011,2, 1135-1161
DOI: 10.1039/c1md00134e

Amidines bearing benzofuroxan or benzimidazole 1,3-dioxide core scaffolds as Trypanosoma cruzi-inhibitors: structural basis for their interactions with cruzipain
Alicia Merlino, Diego Benitez, Nuria E. Campillo, Juan A. Páez, Luzineide W. Tinoco, Mercedes González and Hugo Cerecetto
Med. Chem. Commun., 2012,3, 90-101
DOI: 10.1039/c1md00223f

Discovery of BET bromodomain inhibitors and their role in target validation
S. Müller and S. Knapp
Med. Chem. Commun., 2014,5, 288-296
DOI: 10.1039/c3md00291h

Metabolism-guided drug design
Antonia F. Stepan, Vincent Mascitti, Kevin Beaumont and Amit S. Kalgutkar
Med. Chem. Commun., 2013,4, 631-652
DOI: 10.1039/c2md20317k

3-Hydroxylation of the polycyclic tetramate macrolactam in the biosynthesis of antifungal HSAF from Lysobacter enzymogenes C3
Yaoyao Li, Justin Huffman, Yu Li, Liangcheng Du and Yuemao Shen
Med. Chem. Commun., 2012,3, 982-986
DOI: 10.1039/c2md20026k

Affinity-based target identification for bioactive small molecules
Makoto Kawatani and Hiroyuki Osada
Med. Chem. Commun., 2014,5, 277-287
DOI: 10.1039/c3md00276d

Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments
Charlotte E. Allen, Amanda J. Welford, Thomas P. Matthews, John J. Caldwell and Ian Collins
Med. Chem. Commun., 2014,5, 180-185
DOI: 10.1039/c3md00308f

Ambient mass spectrometry technologies for the detection of falsified drugs
María J. Culzoni, Prabha Dwivedi, Michael D. Green, Paul N. Newton and Facundo M. Fernández
Med. Chem. Commun., 2014,5, 9-19
DOI: 10.1039/c3md00235g

Microwave-assisted synthesis of N-heterocycles in medicinal chemistry
Davide Garella, Emily Borretto, Antonella Di Stilo, Katia Martina, Giancarlo Cravotto and Pedro Cintas
Med. Chem. Commun., 2013,4, 1323-1343
DOI: 10.1039/c3md00152k

Target validation using in-cell small molecule clickable imaging probes
Brahma Ghosh and Lyn H. Jones
Med. Chem. Commun., 2014,5, 247-254
DOI: 10.1039/c3md00277b

If you have any thoughts or comments on any of these articles, please leave these in the comment box below!

Fancy submitting an article to MedChemComm? Submit to us here today!

Comments Off on Q1 Top Ten most accessed MedChemComm articles

Medicinal Chemistry Winners of RSC Awards

06 May 2014

By James Anson.

Congratulations to all of the recently announced Royal Society of Chemistry Prize and Award winners for 2014.

Below are the winners related to medicinal chemistry, taken from the full list of winners

Bioorganic Chemistry Award 2014 Winner

Professor Wilfred van der Donk, University of Illinois at Urbana-Champaign

For his creative work on the chemistry, biosynthesis and mechanistic enzymology of the cyclic peptide and phosphonate classes of antibiotics.

Corday-Morgan Prize 2014 Winner

Professor David Spring, University of Cambridge

For his contributions to chemistry-driven drug discovery through his work in diversity-oriented synthesis and chemical biology.

Rita and John Cornforth Award 2014 Winner

Professor Chas Bountra, Structural Genomics Consortium, University of Oxford

For world leading collaborative research across the disciplines of structural biology, medicinal chemistry, chemical biology and enzymology towards understanding and exploiting the potential of epigenetics as a target family for future drug discovery.

Harrison-Meldola Memorial Prize 2014 Winner

Dr Matthew Fuchter, Imperial College London

For his contribution to the study of epigenetic processes in disease and his insights into chiral aromatic compounds, particularly those with helical chirality.

Norman Heatley Award 2014 Winner

Dr Edward Tate, Imperial College London

For his contributions to the area of antimalarial drug discovery and for pioneering the application of chemical proteomics and its implementation in the identification of novel therapeutic targets

Jeremy Knowles Award 2014 Winner

Professor Gurdyal Besra, University of Birmingham

For his contributions to our understanding of the basic chemistry and biochemistry of the cell wall of Mycobacterium tuberculosis, and his ground-breaking work in the area of tuberculosis T-cell antigens and the CD1 antigen presentation pathway.

George and Christine Sosnovsky Award in Cancer Therapy 2014 Winner

Professor Roger Griffin, Newcastle University

For his major contributions to the discovery of inhibitors of proteins involved in the cell cycle and DNA repair, particularly poly-ADP-ribose polymerase, DNA-dependent protein kinase and cyclin-dependent kinases.

To celebrate these, and all the other award winners, we are delighted to present this web-collection highlighting some of the best research by this year’s winners. Free access until 6^th June 2014.

Did you know?

An incredible 47 previous winners of the Royal Society of Chemistry’s Awards have gone on to win Nobel Prizes for their pioneering work, including Harry Kroto, Fred Sanger and Linus Pauling. Indeed, one of the 2012 Royal Society of Chemistry Prize winners, Arieh Warshel, was awarded the Nobel Prize in Chemistry last year.

Comments Off on Medicinal Chemistry Winners of RSC Awards

Q4 Top Ten most accessed MedChemComm articles

02 Apr 2014

By Judy Allen, Publishing Assistant.

During October, November and December, the following articles were the Top Ten most accessed:

Repairing faulty genes by aminoglycosides: Identification of new pharmacophore with enhanced suppression of disease-causing nonsense mutations
Jeyakumar Kandasamy, Dana Atia-Glikin, Valery Belakhov and Timor Baasov
Med. Chem. Commun., 2011,2, 165-171
DOI: 10.1039/c0md00195c

Recent applications of multicomponent reactions in medicinal chemistry
Paul Slobbe, Eelco Ruijter and Romano V. A. Orru
Med. Chem. Commun., 2012,3, 1189-1218
DOI: 10.1039/c2md20089a

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011,2, 1135-1161
DOI: 10.1039/c1md00134e

Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments
James R. Hitchin, Julian Blagg, Rosemary Burke, Samantha Burns, Mark J. Cockerill, Emma E. Fairweather, Colin Hutton, Allan M. Jordan, Craig McAndrew, Amin Mirza, Daniel Mould, Graeme J. Thomson, Ian Waddell and Donald J. Ogilvie
Med. Chem. Commun., 2013,4, 1513-1522
DOI: 10.1039/c3md00226h

Design, synthesis and antiproliferative activity of indole analogues of indanocine
Gemma A. Tunbridge, Joseph Oram and Lorenzo Caggiano
Med. Chem. Commun., 2013,4, 1452-1456
DOI: 10.1039/c3md00200d

Gd(iii) chelates for MRI contrast agents: from high relaxivity to “smart”, from blood pool to blood–brain barrier permeable
Chang-Tong Yang and Kai-Hsiang Chuang
Med. Chem. Commun., 2012,3, 552-565
DOI: 10.1039/c2md00279e

Diaryl- and triaryl-pyrrole derivatives: inhibitors of the MDM2–p53 and MDMX–p53 protein–protein interactions
Tim J. Blackburn, Shafiq Ahmed, Christopher R. Coxon, Junfeng Liu, Xiaohong Lu, Bernard T. Golding, Roger J. Griffin, Claire Hutton, David R. Newell, Stephen Ojo, Anna F. Watson, Andrey Zaytzev, Yan Zhao, John Lunec and Ian R. Hardcastle
Med. Chem. Commun., 2013,4, 1297-1304
DOI: 10.1039/c3md00161j

Metabolism-guided drug design
Antonia F. Stepan, Vincent Mascitti, Kevin Beaumont and Amit S. Kalgutkar
Med. Chem. Commun., 2013,4, 631-652
DOI: 10.1039/c2md20317k

Synthesis and antiproliferative activity of some 3-(pyrid-2-yl)-pyrazolines
Alexander Ciupa, Paul A. De Bank, Mary F. Mahon, Pauline J. Wood and Lorenzo Caggiano
Med. Chem. Commun., 2013,4, 956-961
DOI: 10.1039/c3md00077j

Do you have any comments or thoughts on any of these articles? Please leave these in the comment box below!

If you would like to submit an article to MedChemComm, please visit our submission site!

Comments Off on Q4 Top Ten most accessed MedChemComm articles

RSC Medicinal Chemistry Blog

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

Q1 Top Ten most accessed MedChemComm articles

Medicinal Chemistry Winners of RSC Awards

Q4 Top Ten most accessed MedChemComm articles

Links

Categories

Archives

Meta