RSC Medicinal Chemistry Blog

The 2016 RSC Prizes and Awards are now open for nomination!

Nominations will close on 15 January 2016.

For more than 140 years, our Prizes and Awards programme has been acknowledging and celebrating exceptional talent in the chemical sciences, and with your support we are hoping that 2016 will even more successful!

Last year’s winners include Chemists such as Prof. Wilfred van der Donk (University of Illinois), Prof. Tim Donohoe (University of Oxford), Prof. Shuli You (Shanghai Institute of Organic Chemistry), Prof. Philip Gale (University of Southampton), Prof. Herman Overkleeft (Leiden University), Prof. Alison Ashcroft and Prof. Sheena Radford (University of Leeds).

This year we have 63 prizes and awards open for nominations of individuals, teams and organisations covering the breadth of the chemical sciences across academia, education and industry.

This year’s prizes in the field of Organic Chemistry & Chemical Biology include:

CBID (Chemistry Biology Interface Division) awards –

• George & Christine Sosnovsky Award in Cancer Therapy
• Jeremy Knowles Award
• Khorana Prize
• Norman Heatley Award
• Rita & John Cornforth Award

Organic Awards –

• Bader Award
• Bioorganic Chemistry Award
• Catalysis in Organic Chemistry Award
• Charles Rees Award
• Hickinbottom Award
• Merck Award
• Natural Product Chemistry Award
• Pedler Award
• Robert Robinson Award
• Sir Derek Barton Gold Medal
• Supramolecular Chemistry Award (Organic & Inorganic)

For 2016 our Longstaff Prize is also open – since 1881 we have awarded this prize once every three years to one of our members who has achieved the most to advance the science of chemistry.

Submit your suggestions now!

The Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry is proud to announce the winners of the Malcolm Campbell Memorial Prize for 2015. The prize has been awarded to Miles Congreve, Fiona Marshall and Malcolm Weir for the seminal contributions to G-protein-coupled receptor (GPCR) drug discovery made by Heptares Therapeutics Ltd since the company was founded in 2007.

This work has included building the world-renowned StaR© technology platform for X-ray crystallography of GPCRs and the invention of a number of clinical candidates. The winners are particularly commended on their outstanding publication record, and on their willingness to release data into the public domain.

The Malcolm Campbell Memorial prize commemorates Professor Campbell’s outstanding contributions in a broad range of chemistry and their applications to the understanding of bioactivity. The prize is awarded biennially and the 2015 prize will be presented formally to the winning team during the 18th RSC/SCI Medicinal Chemistry Symposium to be held at Churchill College in Cambridge on 13th to 16th September 2015.

The BMCS Committee wishes to express its gratitude for the high-quality entries from both academia and industry for the 2015 award.

The new year brings a host of new features in MedChemComm. The first of these is that we are now featuring articles by medicinal chemist and blogger Derek Lowe. These articles, which give opinion and insight into both the science and business sides of drug discovery, will be selected from those published in his In the Pipeline column in the Royal Society of Chemistry magazine Chemistry World, bringing this content to a new audience.

Take a look at the first article in issue 1 of MedChemComm, and look out for further announcements about new features in MedChemComm through the year.

A recent publication in MedChemComm from Doaa A. E. Issa et al.reports the synthesis and biological properties of a series of compounds containing the quinoxaline pharmacophore. Their choice of the quinoxaline motif was inspired by the antineoplastic and antimicrobial activity of other compounds containing this group.

Issa et al. synthesised a total of 15 compounds via a key hydrazino intermediate and evaluated 10 candidates at a single high dose for antitumour activity in the National Cancer Institute-60 cell screen. Compounds showing activity were further evaluated in a multi-dose assay. The team went on to assess the in vitro antibacterial activity and antifungal properties.

They found that several compounds in the series display antibacterial activity and one compound possesses both broad spectrum anticancer activity and antimicrobial activity against Pseudomonas aeruginosa.

Design, synthesis and biological evaluation of novel 1,2,4-triazolo and 1,2,4-triazino[4,3-a]quinoxalines as potential anticancer and antimicrobial agents
Doaa A. E. Issa, Nargues S. Habib and Abeer E. Abdel Wahab
Med. Chem. Commun., 2015, DOI: 10.1039/C4MD00257A

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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.

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