Journal cover: MedChemComm

MedChemComm

Broadening the field of opportunity for medicinal chemists. Official journal of the European Federation for Medicinal Chemistry
Impact Factor 2.722 12 Issues per Year
 
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Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00265B, Review Article
In recent years, gold-based compounds have been proved to hold promise in chemical biology being able to selectively inhibit proteins activities in cells and, therefore, to be exploited as either...
 
Rongjun He, Yunpeng Bai, Zhi-Hong Yu, Li Wu, Andrea M. Gunawan and Zhong-Yin Zhang
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00099D, Concise Article
Mycobacterium protein tyrosine phosphatase B (mPTPB) is a potential drug target of Tuberculosis (TB). Small molecule inhibitors of mPTPB could be a treatment to overcome emerging TB drug resistance. Using...
 
Maria Serratrice, Benoit Bertrand, Esmée F. J. Janssen, Eline Hemelt, Antonio Zucca, Fabio Cocco, Maria A. Cinellu and Angela Casini
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00241E, Concise Article
A number of gold(I) complexes containing the proton pump inhibitor (PPI) lansoprazole and its reduced precursor 2-((3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methylthio)-1H-benzo[d]imidazole have been synthesized and their biological effects have been evaluated in human cancer...
 
Saulo Andrade, Claudia Teixeira, Jonas Ramos, Marcela Lopes, Rodrigo Padua, Monica Oliveira, Elaine Souza-Fagundes and Ricardo Alves
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00136B, Concise Article
We have previously reported on a study of structure-activity relationship in a series of 2,3,4-substituted oxazolidines recently discovered by our group varying the substituent at ring or stereochemistry of the...
 
Wen-Chieh Wang, Hui-Yi Shiao, Chieh-Chien Lee, Ka-Shu Fung and Hsing-Pang Hsieh
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00048J, Review Article
This review elucidates the hit-to-drug evolution design of three ALK inhibitors.
 
Derong Ding, Katerina Lichtenwalter, Hualiang Pi, Shahriar Mobashery and Mayland Chang
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00172A, Concise Article
MMP-8 has been implicated in various diseases using a reported selective MMP-8 inhibitor that is actually a broad-spectrum MMP inhibitor.
 
Aamer Saeed, Yildiz Tehseen, Hummera Rafique, Norbert Furtmann, Jürgen Bajorath, Ulrich Flörke and Jamshed Iqbal
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00206G, Concise Article
Two new series of oxothiazolidine benzoate and acetate derivatives were synthesized and evaluated as aldehyde reductase (ALR1) and aldose reductase (ALR2) inhibitors.
 
Apirat Chaikuada, Andrew Petros, Oleg Fedorov, Jing Xu and Stefan Knapp
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00237G, Concise Article
The transcriptional co-regulator ATAD2 is a prognostic marker for patient survival in many cancers. ATAD2 harbours a bromodomain which may offer an opportunity for pharmacological intervention, but its shallow, polar...
 
Sylvie Garneau-Tsodikova and Timor Baasov
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD90022G, Editorial
Welcome to the Carbohydrates themed issue of MedChemComm.
 
Glenn L. Abbott, Xing Wu, Zhufeng Zhao, Lei Guo, Vladimir B. Birman, Brian B. Hasinoff and Gary I. Dmitrienko
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00197D, Concise Article
The diazo functionality of the kinamycins may not be an absolute requirement for bioactivity.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00086B, Review Article
From themed collection Carbohydrates
New inhibitor chemotypes for glycosyltransferases, which are not structurally derived from either donor or acceptor substrate, are being reviewed.
 
Yadagiri Kommagalla, Sinziana Cornea, Robert Riehle, Vladimir Torchilin, Alexei Degterev and Chepuri V. Ramana
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00109E, Concise Article
Replacement of a central thiourea unit of PITENINs (inhibitors of the phosphatidylinositol-3 kinase (PI3K) signaling pathway) with 1,2,3-triazole, lead to increased liver microsomal stability, drug likeness and toxicity towards cancer cells.
 
Phillip P. Sharp, Jean-Marc Garnier, David C. S. Huang and Christopher J. Burns
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00182F, Concise Article
This work provides new insights into a range of acetyl-lysine mimetics as BET bromodomain inhibitors.
 
Hiren Patel, Irina Chuckowree, Peter Coxhead, Matthew Guille, Minghua Wang, Alexandra Zuckermann, Robin S. B. Williams, Mariangela Librizzi, Ronald M. Paranal, James E. Bradner and John Spencer
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00211C, Concise Article
A HDAC, kinase inhibitor hybrid, (Z)-N1-(3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-5-yl)-N8-hydroxyoctanediamide, 6, showed impressive anticancer action in a number of biochemical and cell-based assays.
 
Michele R. Richards, Michael G. Brant, Martin J. Boulanger, Christopher W. Cairo and Jeremy E. Wulff
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00168K, Concise Article
An analysis of the conformational distribution of peramivir, a potent anti-influenza compound, in solution and the solid state reveals a large conformational change required for enzyme binding.
 
Mathew C. Finniss, Kevin S. Chu, Charles J. Bowerman, J. Christopher Luft, Zishan A. Haroon and Joseph M. DeSimone
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00150H, Concise Article
Silyl ether chemistry was used as the linker for an antibody drug conjugate to release a chemotherapeutic at low pH.
 
Tihomir Tomašić, Said Rabbani, Martina Gobec, Irena Mlinarič Raščan, Črtomir Podlipnik, Beat Ernst and Marko Anderluh
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00093E, Concise Article
From themed collection Carbohydrates
We report branched α-d-mannopyranosides as potent FimH antagonists that exploit the previously unexplored lipophilic region formed by Phe142 and Ile13.
 
Hye Rim Kim, Hye Jin Lee, Yeon Ja Choi, Yun Jung Park, Youngwoo Woo, Seong Jin Kim, Min Hi Park, Hee Won Lee, Pusoon Chun, H.Y. Chung and Hyung Ryong Moon
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00171K, Concise Article
Based on the structural characteristics of the heterocyclic scaffolds of substituted benzylidene-hydantoin, -pyrrolidinedione, and -thiazolidinedione derivatives with potent tyrosinase inhibitory activity, substituted benzylidene derivatives with a 2-thiohydantoin heterocyclic scaffold were...
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00220B, Concise Article
The macrolide antibiotics erythromycin A, clarithromycin and azithromycin are all clinically important.
 
Sibaprasad Bhattacharyya, Nimit L. Patel, Ling Wei, Lisa A. Riffle, Joseph D. Kalen, G. Craig Hill, Paula M. Jacobs, Kurt R. Zinn and Eben Rosenthal
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00116H, Concise Article
The optimized synthesis and biological evaluation of panitumumab-IRDye conjugate for its potential use as an intraoperative optical imaging agent are described.
 
Asit Kumar Chakraborti, Parth Shah, Tejas Dhameliya, Rohit Bansal, Manesh Nautiyal, Damodara Naidu Kommi, Pradeep S. Jadhavar, Jonnalagadda Padma Sridevi, Yogeeswari Sriram and Dharmarajan Sriram
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00224E, Concise Article
Benzothiazole-2-carboxyarylalkylamides are reported as new class of potent anti-mycobacterial agents. Forty one target compounds have been synthesized following a green synthetic strategy using water as the reaction medium to construct...
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00057A, Concise Article
There is no fundamental difference in enthalpy–entropy compensation between dispersion and electrostatics or between quantum and molecular mechanics.
 
Patrick C. Kellish, Sunil Kumar, Todd S. Mack, Meredith Newby Spano, Mirko Hennig and Dev P. Arya
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00165F, Concise Article
From themed collection Carbohydrates
Neomycin dimers synthesized using “click chemistry” with varying functionality and length in the linker region have been shown to be effective in targeting the HIV-1 TAR RNA region of the HIV virus.
 
Jinbo Zhao, Huiping Zhao, Jessica A. Hall, Douglas Brown, Eileen Brandes, Joseph Bazzill, Patrick T. Grogan, Chitra Subramanian, George Vielhauer, Mark S. Cohen and Brian S. J. Blagg
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00102H, Concise Article
1,2,3-Triazole side chain containing coumarin and biphenyl amides were designed, synthesized and evaluated as potent Hsp90 C-terminal inhibitors, which exhibited improved anti-proliferative activities against a panel of cancer cell lines.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00081A, Review Article
From themed collection Carbohydrates
The read-through mechanism of a premature stop codon.
 

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