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MedChemComm

Broadening the field of opportunity for medicinal chemists. Official journal of the European Federation for Medicinal Chemistry
Impact Factor 2.626 12 Issues per Year
 
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Victoria Vinader, Maria Sadiq, Mark Sutherland, Mengying Huang, Paul Loadman, Lina Elsalem, Steve Shnyder, Hongjuan Cui, Kamyar Afarinkia, Mark Searcey, L H Patterson and Klaus Pors
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00411F, Concise Article
A deactivated alkene precursor (IC50 = 81 µM) to the azinomycin epoxide natural product can be bioactivated by several cytochromes P450 (CYP) to generate antiproliferative metabolites with increased potency (IC50...
 
Francesca Bianchini, Chiara Calugi, Jessica Ruzzolini, Gloria Menchi, Lido Calorini, Antonio Guarna and Andrea Trabocchi
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00287C, Concise Article
A D-proline peptidomimetic targeting MMP-2 and MMP-9, being involved during tumor cell invasion and angiogenesis, was identified from a pool of compounds following enzyme inhibition kinetics and zymography, clearly highlighting...
 
Urara Hasegawa and André J van der Vlies
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00373J, Concise Article
Polymeric micelles for therapeutic delivery of hydrogen sulfide (H2S) were developed. The micelles released H2S in murine macrophages and enhanced proinflammatory responses induced by a Toll-like receptor 7 ligand, gardiquimod....
 
Michael. S. Christodoulou, Adeline Thomas, Stéphane Poulain, Melita Vidakovic, Maija Lahtela-Kakkonen, Daumantas Matulis, Philippe Bertrand, Eva Bartova, Christophe Blanquart, Emmanuel Mikros, Nikolas Fokialakis, Daniele Passarella, Rachid Benhida and Nadine Martinet
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00268G, Review Article
From themed collection Epigenetics
Why is it relevant to propose epigenetic “Nutricures” to prevent diseases linked with ageing?
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00312H, Concise Article
Hierarchical structure-based virtual screening against the sphingosine kinase 1(SphK1) binding pocket was performed. 25 compounds were selected for biological evaluation. Compound 25 exhibited comparable SphK1 and SphK2 inhibitory activities and anti-proliferative effects on U937 cells to the positive control N,N-dimethylsphingosine (DMS) 1. Further molecule dynamic (MD) simulations revealed the binding mode between SphK1 and 25.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00363B, Review Article
Quorum quenching compounds blocked quorum sensing system of bacteria by several mechanisms (a, b, c and d).
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00264D, Concise Article
This research aims to synthesize lipophilic berberine derivatives and evaluate their antiglioma effects on C6 and U87 cells.
 
Chiara Nardon, Giulia Boscutti, Lisa Dalla Via, Paola Ringhieri, Vito Di Noto, Giancarlo Morelli, Antonella Accardo and Dolores Fregona
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00299G, Concise Article
A sparingly water-soluble gold(III) complex was encapsulated in micelles functionalized with the CCK8-targeting moiety for the selective delivery of an anticancer drug.
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00407H, Concise Article
A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferation activity against four kinds of tumor cell lines. The compounds 3c, 3f,...
 
Doaa Boshra Farag, Nahla Ahmed Farag, Ahmed Esmat, Sally A. Abuelezz, Eman Abdel-Salam Ibrahim and Dalal A. Abou El Ella
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00392F, Concise Article
Four novel series of 1-substituted-3-(2-methyl-4-oxo-4H-quinazolin-3-yl) urea and/or thiourea IIIa-c, 4-substituted-N-(2-methyl-4-oxo-4H-quinazolin-3-yl) benzene sulfonamide VIa-c and their NO-hybrid molecules as nitrate esters Va-c, VIIIa-c have been synthesized and evaluated for their anti-inflammatory...
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00266K, Concise Article
A series of tetrazole derivatives were synthesized and characterized by NMR, IR, MS and HRMS spectroscopy.
 
Daniela Rossi, Annamaria Marra, Marta Rui, Erik Laurini, Maurizio Fermeglia, Sabrina Pricl, Dirk Schepmann, Bernhard Wuensch, Marco Peviani, Daniela Curti and Simona Collina
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00349G, Concise Article
To investigate the role of chirality in the ligand–σ1 receptor interaction, a series of enantiomeric arylalkylaminoalcohols and arylpyrrolidinols was evaluated by means of both in silico and in vitro studies.
 
Deepak Kumar, Garima Khare, Beena, Saqib Kidwai, Anil K. Tyagi, Ramandeep Singh and Diwan S. Rawat
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00288A, Concise Article
A series of isoniazid–amidoether derivatives was synthesized and screened for their antimycobacterial activity in vitro and in vivo.
 
Yu'ning Song, Hao Xu, Wenmin Chen, Peng Zhan and Xinyong Liu
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00284A, Review Article
Abstract: Privileged structures could bind to diverse targets with high affinity, thus benefiting the discovery of novel bioactive agents. 8-Hydroxyquinoline derivatives represented an important type of "privileged structure" possessing a...
 
Manish Singh, Sandhya Bansal, Somanath Kundu, Priyanshu Bhargava, Ashima Singh, Rajender Motiani, Radhey Shyam, Vedagopuram Sreekanth, Sagar Sengupta and Avinash Bajaj
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00223G, Concise Article
We report a structure-activity relationship of lithocholic acid amphiphiles for their anticancer activities against colon cancer. We synthesized ten cationic amphiphiles differing in nature of cationic charged head groups using...
 
Guilherme A. M. Jardim, Tiago T. Guimarães, Maria do Carmo F. R. Pinto, Bruno C. Cavalcanti, Kaio M. de Farias, Claudia Pessoa, Claudia C. Gatto, Divya K. Nair, Irishi N. N. Namboothiri and Eufrânio N. da Silva Júnior
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00371C, Concise Article
Naphthoquinone-based chalcone hybrids were synthesized and evaluated for their cytotoxic activity against four cancer cell lines and PBMC. Some of the hybrids exhibited promising anticancer activity with IC50 values < 1 μM.
 
Fei Ye, Liyi Zhang, Lu Jin, Mingyue Zheng, Hualiang Jiang and Cheng Luo
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00256C, Review Article
From themed collection Epigenetics
Nucleic acid methylation is one of the most important epigenetic modifications that have been studied intensively for the past several decades.
 
Qian Chu, Raymond E. Moellering, Gerard J. Hilinski, Young-Woo Kim, Tom N. Grossmann, Johannes T.-H. Yeh and Gregory L. Verdine
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00131A, Concise Article
A systematic study on cell penetration by stapled peptides.
 
Valentine Nenajdenko, Anastasiya Govdi, Nadezhda Sokolova, Irina Sorokina, Sergey Vasilevsky, Dmitry Baev, Tatyana Tolstikova, Victor Mamatyuk and Dmitry Fadeev
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00236A, Concise Article
The modification of betulinic acid derivatives bearing an ethynyl group at the C-3 position by different azidopeptides using Cu(I)-catalyzed alkyne-azide cycloaddition has been described. All obtained compounds were tested for...
 
Shuangling Chen, Yuji Wang, Shan Li, Yaonan Wang, Ming Zhao, Haimei Zhu, Jianhui Wu and Shiqi Peng
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00331D, Concise Article
Thrombosis is a pathological condition and has been one of the most prominent causes of morbidity and mortality, poly-α,β-aspartic acid is a biodegradable polymer, and RGD-tetrape- ptides target thrombus. These...
 
Tihomir Tomašič, Dominik Nabergoj, Sanja Vrbek, Nace Zidar, Žiga Jakopin, Aleš Žula, Žiga Hodnik, Marko Jukič, Marko Anderluh, Janez Ilaš, Marija Sollner Dolenc, Jean Peluso, Geneviève Ubeaud-Séquier, Christian D. Muller, Lucija Peterlin Mašič and Danijel Kikelj
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00286E, Concise Article
Structural modification of the marine alkaloid oroidin resulted in improved apoptosis inducing activity in HepG2 and THP-1 cell lines.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00325J, Concise Article
Click-chemistry based design and efficient synthesis of podophyllotoxin–chalcone conjugates as potential topoisomerase-II inhibitors towards the development of better anticancer leads.
 
F. Esra Önen-Bayram, Kerem Buran, Irem Durmaz, Barkin Berk and Rengul Cetin-Atalay
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00306C, Concise Article
Modification at the 2-position of the apoptosis-inducing compound ALC 67 enables tuning of its physicochemical properties.
 
Barbara Cortese, Stefania D'Amone, Giuseppe Gigli and Ilaria Elena Palamà
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00348A, Concise Article
Imatinib Mesylate (IM) is an inhibitor that targets the tyrosine kinase activity of BCR-ABL present in Chronic Myeloid Leukemia (CML). Here, IM-Chitosan complexes encapsulated poly(ε-caprolactone) (PCL) nanoparticles (NPs) are recommended...
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00281D, Concise Article
A series of novel quinazolinone azoles were synthesized and characterized by NMR, IR, MS and HRMS spectra. Bioactive assay showed that some target compounds exhibited significant antimicrobial potency. Especially, nitroimidazole...
 

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