Francesca Burgoyne – Page 3 – RSC Medicinal Chemistry Blog

Author Archive

Tracking immune cell migration on the cover of Issue 11

04 Nov 2011

On the cover of Issue 11 is a hot article from Mark Bradley and coworkers on a method to track innate immune cell migration in vivo using dye-labelled peptoids.

Far red and NIR dye-peptoid conjugates for efficient immune cell labelling and tracking in preclinical models
Kevin Dhaliwal, Géraldine Escher, Asier Unciti-Broceta, Neil McDonald, A. John Simpson, Chris Haslett and Mark Bradley
Med. Chem. Commun., 2011, 2, 1050-1053
DOI: 10.1039/C1MD00171J

Also in this issue is Ying-Wei Yang’s review on biocompatible nanovalves for drug delivery and release:

Towards biocompatible nanovalves based on mesoporous silica nanoparticles
Ying-Wei Yang
Med. Chem. Commun., 2011, 2, 1033-1049
DOI: 10.1039/C1MD00158B

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New compound class for treating hepatitis C virus

31 Oct 2011

Researchers from Biotica, UK have discovered a new compound class called sangamides with the potential to treat hepatitis C. Sangamides are amide derivatives of sanglifehrin A – a cyclophilin-binding polyketide natural product. Non-immunosuppressive analogues of sanglifehrin A are currently under development as hepatitis C virus therapies, but suffer from lengthy synthetic processes, and some adverse affects including drug-drug interactions.

The newly developed sangamides display improved potency and good pharmcokinetic properties that make them potentially suitable for once-a-day oral treatment of chronic hepatitis C infection. Download the article for the full details:

Sangamides, a new class of cyclophilin-inhibiting host-targeted antivirals for treatment of HCV infection
Steven J. Moss, Michael Bobardt, Pieter Leyssen, Nigel Coates, Udayan Chatterji, Xie Dejian, Teresa Foster, Jinlun Liu, Mohammad Nur-e-Alam, Dipen Suthar, Chen Yongsheng, Tony Warneck, Ming-Qiang Zhang, Johan Neyts, Philippe Gallay, Barrie Wilkinson and Matthew A. Gregory
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C1MD00227A

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Current progress in inhibiting Stat5 protein signalling

14 Oct 2011

This mini-review from Patrick Gunning et al. looks at progress made towards inhibiting Stat5, a member of the Stat family of signalling proteins, that is connected to many cancers, including acute myeloid leukemias and prostate cancer.

Areas covered include both direct and indirect inhibition:

Bcr/Abl inhibitors
FLT3 inhibitors
Jak2 inhibitors
truncation inhibitors
Binding to DNA
Disrupting dimerisation

Inhibitors of Stat5 protein signalling
Abbarna A. Cumaraswamy, Aleksandra Todic, Diana Resetca, Mark D. Minden and Patrick T. Gunning
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00175B

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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

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

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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RSC e-membership launched

02 Sep 2011

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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MedChemmComm article on PAM in the press

27 Aug 2011

MedChemComm has been making the headlines again!

The recently published article by Chris Easton and colleagues at the Australian National University entitled “Potent and selective inhibitors of human peptidylglycine α-amidating monooxygenase” was picked-up by several news outlets, including Medical News Today:

Love Hormone Oxytocin Inspires New Small-cell Lung Cancer Treatment Research
One in Every 28 Australians Are Diagnosed With Lung Cancer, Says Study
Lung cancer breakthrough yields new love hormone insights
Sex gives clues to new lung cancer treatment
Enzyme PAM Linked to Small Cell Lung Cancer: Study

Congratulations to Professor Easton and team!

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Designing CETP inhibitors for prevention of coronary heart disease

16 Aug 2011

Coronary heart disease has been shown to be related to low levels of high-density lipoprotein cholesterol (HDL-C) in blood plasma, and consequently methods of controlling HDL-C levels are sought to reduce the risk of heart disease. Inhibition of the cholesteryl ester transfer protein (CETP) – the protein that transports cholesteryl esters from high-density lipoprotein (HDL) to low- and very low-density lipoproteins (LDLs and VLDLs) – has shown potential as a therapy.

Tarun Jha and a team from Jadavpur University have performed studies on a series of 2-arylbenzoxazoles to define the structural requirements of a good CETP inhibitor. The 2D QSAR study using using PCR, PLS and MLR techniques and kNN-MFA 3D QSAR results have generated a pharmacophore that they hope will provide a good scaffold for the design of future potent CETP inhibitors.

Download the paper today to read the details of their findings – it’s free to access until the end of 2011:

Chemometric modeling and pharmacophore mapping in coronary heart disease: 2-arylbenzoxazoles as cholesteryl ester transfer protein inhibitors
Dhritiman Jana, Amit Kumar Halder, Nilanjan Adhikari, Milan Kumar Maiti, Chanchal Mondal and Tarun Jha
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00135C

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Progress on lamellarins

01 Aug 2011

This review article from Mercedes Álvarez and colleagues at The Center for Biomedical Research Network in Bioengineering, Biomaterials and Nanomedicine, Barcelona, have reviewed the recent developments in studies on lamellarins and their analogues.

Lamellarins are a family of marine pyrrole alkaloids, which have attracted interest as anti-tumour agents. The review encompasses synthetic strategies for total synthesis, structure–activity relationships and studies on mechanisms of biological action, mainly in the context of anti-tumor activity.

Download the full article here:

Progress on lamellarins
Daniel Pla, Fernando Albericio and Mercedes Álvarez
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00003A

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Top ten most accessed articles in May

26 Jul 2011

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

Identification of target family directed bioisosteric replacements
Anne Mai Wassermann and Jürgen Bajorath
Med. Chem. Commun., 2011, 2, 601-606, DOI: 10.1039/C1MD00066G

Synthesis and biological evaluation of tetrazole containing compounds as possible anticancer agents
Chebolu Naga Sesha Sai Pavan Kumar, Dusmant Kumar Parida, Amlipur Santhoshi, Anil Kumar Kota, Balasubramanian Sridhar and Vaidya Jayathirtha Rao
Med. Chem. Commun., 2011, 2, 486-492, DOI: 10.1039/C0MD00263A

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, 1, 309-318, DOI: 10.1039/C0MD00135J

Computational ligand-based rational design: role of conformational sampling and force fields in model development
Jihyun Shim and Alexander D. MacKerell, Jr.
Med. Chem. Commun., 2011, 2, 356-370, DOI: 10.1039/C1MD00044F

N1-Benzyl substituted cambinol analogues as isozyme selective inhibitors of the sirtuin family of protein deacetylases
Federico Medda, Thomas L. Joseph, Lisa Pirrie, Maureen Higgins, Alexandra M. Z. Slawin, Sonia Lain, Chandra Verma and Nicholas J. Westwood
Med. Chem. Commun., 2011, 2, 611-615, DOI: 10.1039/C1MD00023C

Antimycobacterial activity of spirooxindolo-pyrrolidine, pyrrolizine and pyrrolothiazole hybrids obtained by a three-component regio- and stereoselective 1,3-dipolar cycloaddition
Stephen Michael Rajesh, Subbu Perumal, J. Carlos Menéndez, Perumal Yogeeswari and Dharmarajan Sriram
Med. Chem. Commun., 2011, 2, 626-630, DOI: 10.1039/C0MD00239A

Synthesis and SAR studies of benzimidazole derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Focus to detune hERG inhibition
Pradip K. Sasmal, Sanjita Sasmal, Chandrasekhar Abbineni, B. Venkatesham, P. Tirumala Rao, M. Roshaiah, Ish Khanna, V. J. Sebastian, J. Suresh, Manvendra P. Singh, Rashmi Talwar, Dhanya Shashikumar, K. Harinder Reddy, Thomas M. Frimurer, Øystein Rist, Lisbeth Elster and Thomas Högberg
Med. Chem. Commun., 2011, 2, 385-389, DOI: 10.1039/C1MD00015B

Glycosylated porphyrin derivatives and their photodynamic activity in cancer cells
Seenuvasan Vedachalam, Bo-Hwa Choi, Kalyan Kumar Pasunooti, Kun Mei Ching, Kijoon Lee, Ho Sup Yoon and Xue-Wei Liu
Med. Chem. Commun., 2011, 2, 371-377, DOI: 10.1039/C0MD00175A

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

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