Archive for March, 2012

HOT: Substituted oxines inhibit endothelial cell proliferation and angiogenesis

In this HOT OBC paper Jun O. Liu and co-workers at Johns Hopkins University School of Medicine report structure–activity relationship studies of two oxines, which have been previously identified as hits in a high-throughput screen aimed at finding new anti-angiogenic agents, by characterising different analogues in human umbilical vein endothelial cell assays. In addition they have determined the effects of a subset of oxine derivatives on human methionine aminopeptidase and sirtuin 1 activities in endothelial cells and screened a selection of the potent inhibitors of human umbilical vein endothelial cells against two other malignant cells.

Through this they have been able to identify new oxine derivatives that exhibit improved inhibitory activity against endothelial cell proliferation, and furthermore, have made the surprising finding that subtle structural alterations can lead to dramatic changes in the mechanism of action of the resulting derivatives.

For all the in-depth details of this study check out this paper today! It’s free to access for the next 4 weeks!

Substituted oxines inhibit endothelial cell proliferation and angiogenesis
Shridhar Bhat, Joong Sup Shim, Feiran Zhang, Curtis Robert Chong and Jun O. Liu
Org. Biomol. Chem.,  2012, 10, 2979–2992
DOI: 10.1039/C2OB06978D

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HOT: Fluorimetric probe detects both Mg2+ and DNA

In this HOT OBC paper Heiko Ihmels and colleagues at University of Siegen present the fluorimetric detection of Mg2+ and DNA with 9-(alkoxyphenyl)benzo[b]-quinolizinium derivatives. Although there are quite a few fluorescent probes that enable the detection of different analytes from the same class of compounds, probes that allow optical detection of different types of analytes are much rarer. In this paper Heiko Ihmels et al. show that a benzo[b]quinolizinium-benzo-15-crown-5 ether conjugate can be used for the detection of both Mg2+ and DNA by a significant light-up effect and with different emission wavelengths for the two different analytes.

The authors investigated the light-up mechanism by comparison with the photophysical properties of methoxyphenyl-substituted benzo[b]quinolizinium reference compounds, revealing that the position of the methoxy functionality had a significant influence on the emission properties of the donor–acceptor systems.

Find the full paper here. It’s FREE to access for the four weeks, so why not take a peek!

Fluorimetric detection of Mg2+ and DNA with 9-(alkoxyphenyl)benzo[b]quinolizinium derivatives
Maoqun Tian, Heiko Ihmels and Shite Ye
Org. Biomol. Chem., 2012, 10, 3010–3018
DOI: 10.1039/C2OB06948B

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Modern microwave chemistry opportunities to develop new antibiotics and antiviral drugs on OBC Issue 14’s cover

Welcome to OBC issue 14, 2012

On the cover features work by Mats Larhed et al. at Uppsala University, Sweden, who describe in this highly topical review the use of controlled microwave heating in discovery chemistry to combat four of the most prevalent and serious infectious diseases: tuberculosis, HIV/AIDS, malaria and hepatitis C.

This Perspective highlights the large number of diverse chemical transformations that can be accomplished using controlled and automated single-mode microwave heating.

Why not read it now, it will be FREE to access for the next 6 weeks!

 

 

 Microwave-assisted synthesis of small molecules targeting the infectious diseases tuberculosis, HIV/AIDS, malaria and hepatitis C
Johan Gising, Luke R. Odell and Mats Larhed
Org. Biomol. Chem., 2012, Advance Article
DOI: 10.1039/C2OB06833H, Perspective

Also in this issue, a Hot Article by Robert M. Strongin et al. on a cysteine selective indicator based on a seminaphthofluorescein, and much more!

View the full issue here

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HOT: Sensing cysteine only for health tests

A sensing system to detect cysteine (Cys), an essential amino acid, has been developed by scientists in the US and China. Elevated levels of Cys have been associated with neurotoxicity, while Cys deficiency is involved in a number of other disorders.

The sensing system works as a fluorescent chemodosimeter, which displays discrimination for cysteine over commonly occurring analytes that would be expected to co-exist in real samples, such as homocysteine and glutathione. Moreover, the system is desirable in that it displays off-to-on response to the target analyte and does so at a desirable long wavelength, which minimises potential interference by endogenous chromophores.

Due to its simplicity and very high selectivity, this chemodosimeter can be used to detect Cys at physiological levels.

Highly rated by the reviewers and Editorial office alike, this article has been selected as ‘Hot’ and will be FREE to access for the next 4 weeks – why not read it now!

A seminaphthofluorescein-based fluorescent chemodosimeter for the highly selective detection of cysteine
Xiaofeng Yang, Yixing Guo and Robert M. Strongin
Org. Biomol. Chem., 2012, Advance Article
DOI: 10.1039/C2OB25178G, Communication

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HOT: Probing the effects of a novel post-translational modification on synaptic protein binding

In this HOT OBC Communication Mark E. Graham, Richard J. Payne and co-workers probe the effect of a recently discovered post-translational modification of threinine of the assembly protein AP180, a protein which plays a crucial role in clathrin coated vesicle formation in synaptic vesicle endocytosis.


Using pull down experiments on AP180 peptide fragments they aimed to explore how binding to proteins in rat brain lysate is influenced by this modification.

Read the article to find out more about the peptides used and the effect of this modification on the affinity towards synaptic proteins.

Go on, it’s FREE to access for the next 4 weeks!

 

 
Synthesis and protein binding studies of a peptide fragment of clathrin assembly protein AP180 bearing an O-linked β-N-acetylglucosaminyl-6-phosphate modification
Mark E. Graham, Robin S. Stone, Phillip J. Robinson and Richard J. Payne
Org. Biomol. Chem., 2012, 10, 2545-2551
DOI: 10.1039/C2OB07139H

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Asymmetric catalytic Mannich-type reaction of hydrazones using Zn(II) complexes on the cover of OBC issue 13

The cover of this week’s OBC features work from Min Shi et al. at Shanghai Institute of Organic Chemistry and Texas Tech University, who have used chiral zinc(II)–imidazoline–phosphine complexes in a novel catalytic system for the asymmetric Mannich-type difluorination of hydrazones with difluoroenoxysilanes.

Asymmetric catalytic Mannich-type reaction of hydrazones with difluoroenoxysilanes using imidazoline-anchored phosphine ligand–zinc(II) complexes
Zhiliang Yuan, Liangyong Mei, Yin Wei, Min Shi, Padmanabha V. Kattamuri, Patrick McDowell and Guigen Li
Org. Biomol. Chem., 2012, 10, 2509-2513
DOI: 10.1039/C2OB07022G

Read the full Communication; it is FREE to access for the next 6 weeks.

This issue also contains:

A Perspective review article: On a so-called “kinetic anomeric effect” in chemical glycosylation, by Ian Cumpstey

as well as the HOT article:

Synthesis and protein binding studies of a peptide fragment of clathrin assembly protein AP180 bearing an O-linked β-N-acetylglucosaminyl-6-phosphate modification
Mark E. Graham, Robin S. Stone, Phillip J. Robinson and Richard J. Payne

If you liked these why not have a look at the rest of the issue here

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Top ten most accessed articles in January

This month sees the following articles in Organic & Biomolecular Chemistry that are in the top ten most accessed:

Asymmetric organocatalytic formation of protected and unprotected tetroses under potentially prebiotic conditions
Laurence Burroughs, Paul A. Clarke, Henrietta Forintos, James A. R. Gilks, Christopher J. Hayes, Matthew E. Vale, William Wade and Myriam Zbytniewski
Org. Biomol. Chem., 2012, 10, 1565-1570
DOI: 10.1039/C1OB06798B

Total synthesis of (+)-anamarine
Krishnammagari Suresh Kumar and Cirandur Suresh Reddy
Org. Biomol. Chem., 2012, 10, 2647-2655
DOI: 10.1039/C2OB06940G

Olefin cross-metathesis for the synthesis of heteroaromatic compounds
Timothy J. Donohoe, John F. Bower and Louis K. M. Chan
Org. Biomol. Chem., 2012, 10, 1322-1328
DOI: 10.1039/C2OB06659A

Highly selective, naked-eye and fluorescent “off-on” probe for detection of histidine/histidine-rich proteins and its application in living cell imaging
Shenyi Zhang, Chunmei Yang, Weiping Zhu, Bubing Zeng, Youjun Yang, Yufang Xu and Xuhong Qian
Org. Biomol. Chem., 2012, 10, 1653-1658
DOI: 10.1039/C2OB06520G

Direct C–H cross-coupling approach to heteroaryl coumarins
Minsik Min, Bomi Kim and Sungwoo Hong
Org. Biomol. Chem., 2012, Advance Article
DOI: 10.1039/C2OB07137A

Bioinspired organocatalytic asymmetric reactions
Luca Bernardi, Mariafrancesca Fochi, Mauro Comes Franchini and Alfredo Ricci
Org. Biomol. Chem., 2012, Advance Article
DOI: 10.1039/C2OB07037E

Imidazole derivatives: A comprehensive survey of their recognition properties
Pedro Molina, Alberto Tárraga and Francisco Otón
Org. Biomol. Chem., 2012, 10, 1711-1724
DOI: 10.1039/C2OB06808G

An iterative Shimizu non-aldol approach for the stereoselective synthesis of C13-C22 fragment of callystatin A
Sandip A. Pujari and Krishna P. Kaliappan
Org. Biomol. Chem., 2012, 10, 1750-1753
DOI: 10.1039/C2OB06838A

Organocatalytic stereoselective synthesis of passifloricin A
Pradeep Kumar, Menaka Pandey, Priti Gupta and Dilip D. Dhavale
Org. Biomol. Chem., 2012, 10, 1820-1825
DOI: 10.1039/C2OB06711K

Direct preparation of thiazoles, imidazoles, imidazopyridines and thiazolidines from alkenes
Timothy J. Donohoe, Mikhail A Kabeshov, Akshat H. Rathi and Ian E. D. Smith
Org. Biomol. Chem., 2012, 10, 1093-1101
DOI: 10.1039/C1OB06587D

Why not take a look at the articles today and blog your thoughts and comments below.

Fancy submitting an article to Organic & Biomolecular Chemistry? Then why not submit to us today or alternatively email us your suggestions.

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Room temperature syntheses of substituted beta-fluorofurans on the cover of OBC issue 12

On the cover this week is work by Roman Dembinski et al. at Oakland University and Eastern Illinois University, highlighting facile synthetic methods for the preparation of 3-fluorofurans, 3-bromo-4-fluorofurans, and 3-fluoro-4-iodofurans in good yields and at room temperature.

Read all about the synthetic sequences employed: this article will be FREE to access for a period of 6 weeks.

Room temperature syntheses of entirely diverse substituted β-fluorofurans
Yan Li , Kraig A. Wheeler and Roman Dembinski
Org. Biomol. Chem., 2012, 10, 2395-2408
DOI: 10.1039/C1OB06693E

Also in this issue, take a look at a hot article by Taku Shoji et al. presenting  novel developments in the field of donor-acceptor chromophores, which can be synthesised using the [2+2] cycloaddition-cycloreversion (CA/CR) reaction; or read a timely Perspective showcasing recent advancement in the stereoselective synthesis of 2-C-branched sugar analogs, by Torsten Linker et al., and much more!

View the full issue here

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Join ICPO21: 21st IUPAC International Conference on Physical Organic Chemistry

The Organic Division of the RSC on behalf of IUPAC is now inviting contributions to ICPO21: 21st IUPAC International Conference on Physical Organic Chemistry to be held 9 – 13 September 2012 at Durham University.

The submission deadline dates are:

 

  • Oral abstracts               23 March 2012
  • Poster abstracts           13 July 2012

 

Key topics that will be covered in the meeting include:

  • Physical underpinnings
  • Mechanism and Catalysis
  • Supramolecular and Systems Chemistry

 

Why join ICPOC21?

A broad range of scientists from across the whole community who share a quantitative perspective on chemistry will be there, providing an opportunity to discuss and celebrate the current status, development, and the future of physical organic chemistry.

 

In addition to outstanding plenary sessions, there will be three parallel sessions over the five days comprising invited lectures and contributed talks, as well as poster sessions.

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