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MedChemComm

Research and review articles in medicinal chemistry and related drug discovery science; the official journal of the European Federation for Medicinal Chemistry
 
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Gianpiero Calabrese, Anis Daou, Aikaterini Rova, Eirini Tseligka, Ioannis S. Vizirianakis, Dimitrios G. Fatouros and John Tsibouklis
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD90004J, Correction
 
Chenze Zhang, Wenqiang Yan, Rui Zhao, Bing Xu, Xiong Fang, Mengmeng Yan, Yuzhong Zhang, Penglong Wang and Haimin Lei
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00003K, Research Article
To investigate plasma-stable neuroprotective agents, a series of new ligustrazine derivatives were synthesized by conjoining ligustrazine and phenols with ester, ether and amide bonds.
 
Federica Castriconi, Marco Paolino, Alessandro Donati, Germano Giuliani, Maurizio Anzini, Laura Mennuni, Chiara Sabatini, Marco Lanza, Gianfranco Caselli, Francesco Makovec, Maria Sbraccia, Paola Molinari, Tommaso Costa and Andrea Cappelli
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00458J, Research Article
Multivalency does not improve the binding and functional activities of ML10302 at 5-HT4 receptors.
 
Jasmina Marjanovic, Aleksandra Baranczak, Violeta Marin, Henning Stockmann, Paul Richardson and Anil Vasudevan
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C7MD00049A, Research Article
From themed collection New Talent: Americas
Determination of target engagement following drug administration under physiological conditions is essential for understanding clinical outcomes of therapeutic candidates. While the list of potential techniques that enable studies of target...
 
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00699J, Research Article
Herein, we report the synthesis, characterization and evolution of transfection efficiencies of a series of dicationic amphiphiles designed by covalent grafting of a delocalizable heterocyclic cation to a localized cation...
 
Hamid R Nasiri, Volker Zickermann , Stefan Dröse, , Robin Krishnathas and Erik Bonke
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00655H, Research Article
By probing the quinone substrate binding site of mitochondrial complex I with a focused set of quinazoline-based compounds, we identified substitution patterns as being critical for the observed inhibition. The...
 
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00697C, Research Article
Carboxymethylated and sulfated polysaccharide (CLEP and SLEP) were prepared from an exopolysaccharide obtained previously from Lachnum YM240 (LEP) by chemical modifications. Two doses (50 mg/kg and 200 mg/kg b. w.)...
 
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00646A, Research Article
This study was aimed to elucidate the therapeutic effects of oral administeration of intracellular melanin from Lachnum YM156 (LIM) on chronic renal failure (CRF) in mice. The cytotoxicity of LIM...
 
Eric Lattmann, Jintana Sattayasai, Ramesh Narayanan, Nguyen Ngoc, Danny Burrell, Tahmineh Palizdar, P N Balaram and Pornthip Lattmann
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00707D, Research Article
Arylated 5-hydroxy–pyrrol-2-ones were prepared in 2 synthetic steps from muco- chloric acid and optimised as CCK2 selective ligands using radiolabelled binding assays. CCK antagonism was confirmed for the ligands in...
 
Harmesh Singh Aojula, Shaun Clive Offerman, Manikandan Kadirvel, Osama Haitham Abusara, Jennifer L Bryant, Brian A Tefler, Gavin Brown, sally freeman, Anne White and Kaye Williams
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00691D, Research Article
Natural prenylated indoles have been proposed as potential anticancer agents. To exploit this discovery for developing new peptide therapeutics we report the first studies whereby incorporation of prenylated indoles into...
 
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00015D, Review Article
This review article summarizes the recent knowledge about the enzyme NPP1 and its inhibitors.
 
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C7MD00006E, Research Article
The peptides containing RGD and NGR-motifs display high affinity towards tumor vasculature molecular markers, integrin αvβ3 and CD13 receptors respectively. In the present study RGD and NGR peptides were conjugated...
 
Jun-Rong Duan, Han-Bo Liu, Ponmani Jeyakkumar, Gopala Lavanya, Shuo Li, Rong-Xia Geng and Cheng-He Zhou
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00688D, Research Article
A series of novel Schiff base-bridged tetrahydroprotoberberine (THPB) triazoles were designed, synthesized and characterized for the first time. Antimircobial assay showed that some of the prepared compounds exerted stronger antibacterial...
 
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C7MD00030H, Review Article
Human protein farnesyltransferase (FTase) catalyzes the addition of a C15-farnesyl lipid group to the cysteine residue located in the COOH-terminal tetrapeptide motif of a variety of important substrate proteins, including...
 
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00728G, Research Article
A series of novel quinones was synthesized by reacting tetrabromo-p-benzoquinone with amino oligo(ethylene glycol) dendrons of generation numbers g=0–2. According to the performed shake-flask experiments, their aqueous solubility (S=18 mg...
 
Klaas Verschueren, Mathias Cobbaut, Joachim Demaerel, Lina Saadah, Arnout R. D. Voet, Johan Van Lint and Wim M. De Borggraeve
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00675B, Research Article
Herein we report the synthesis of pyrazolo[3,4-d]pyrimidine analogues of 1-NM-PP1 and the identification of 3-IN-PP1 as a new potent PKD inhibitor suggesting an alternate binding mode to PKD.
 
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00581K, Review Article
Herein, we present an overview of a broad range of physico-chemical approaches able to reveal the details of protein–ligand kinetics.
 
Bi-Qun Zou, Qi-Pin Qin, Yu-Xia Bai, Qian-Qian Cao, Ye Zhang, Yan-Cheng Liu, Zhen-Feng Chen and Hong Liang
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00644B, Research Article
A new iron(III) complex with 5,7-dichloro-2-methyl-8-quinolinol (HClMQ) as ligands, i.e., [Fe(ClMQ)2Cl] (1), was synthesized and evaluated for its anticancer activity.
 
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00716C, Research Article
Single-wall carbon nanotubes with built-in peroxidase-like activity mediated by bacterial magnetic nanoparticles exert neuroprotective effects against β-amyloid fibrillation-induced neurotoxicity.
 
Behnam Nazari, Clarissa C. Forneris, Marcus I. Gibson, Kyuho Moon, Kelsey R. Schramma and Mohammad R. Seyedsayamdost
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00637J, Research Article
From themed collection New Talent: Americas
We report the largest actinomycete genome to date, which encodes >30 secondary metabolites, including the kistamicin biosynthetic gene cluster.
 
Lian-Xiang Luo, Xing-Xing Fan, Ying Li, Xia Peng, Yin-Chun Ji, Wendy Wen-Luan Hsiao, Liang Liu, Elaine Lai-Han Leung and Xiao-Jun Yao
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00643D, Research Article
We reported that mitoxantrone, an FDA approved drug for anti-cancer chemotherapy drugs, is a direct potent inhibitor of ROS1 kinase.
 
Kyle J. Eastman, Kyle Parcella, Kap-Sun Yeung, Katharine A. Grant-Young, Juliang Zhu, Tao Wang, Zhongxing Zhang, Zhiwei Yin, Brett R. Beno, Steven Sheriff, Kevin Kish, Jeffrey Tredup, Adam G. Jardel, Vivek Halan, Kaushik Ghosh, Dawn Parker, Kathy Mosure, Hua Fang, Ying-Kai Wang, Julie Lemm, Xiaoliang Zhuo, Umesh Hanumegowda, Karen Rigat, Maria Donoso, Maria Tuttle, Tatyana Zvyaga, Zuzana Haarhoff, Nicholas A. Meanwell, Matthew G. Soars, Susan B. Roberts and John F. Kadow
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00636A, Research Article
From themed collection New Talent: Americas
A series of novel 7-azabenzofurans exhibiting pan-genotype inhibition of HCV NS5B polymerase via binding to the primer grip site is presented.
 
H. L. Bolt, G. A. Eggimann, C. A. B. Jahoda, R. N. Zuckermann, G. J. Sharples and S. L. Cobb
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00648E, Research Article
The cytoxicity profiling of a series of linear peptoids against mammalian cell lines has been carried out and correlated against both antibacterial properties and hydrophobicity.
 
Paramita Sarkar, Venkateswarlu Yarlagadda, Chandradhish Ghosh and Jayanta Haldar
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00585C, Review Article
In this review, inhibitors of the cell wall biosynthetic pathway are presented with a focus on the recent advances in glycopeptide antibiotics.
 
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00683C, Research Article
Studies on FAAH inhibitory potency and metabolic stability of indolyl-substituted alkyl- and alkylpiperidine carbamates are described.
 

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18 citations
A new series of exceptionally potent quinoline derivatives 6–30 as α-glucosidase inhibitors was identified.
DOI: 10.1039/C5MD00280J
Published: 21 Aug 2015
13 citations
The newest information (2010-present) on the four main mechanisms of resistance to the broad-spectrum aminoglycoside antibiotics is presented in details.
DOI: 10.1039/C5MD00344J
Published: 21 Sep 2015
21 citations
A library of thirty one 1,2,3-triazole derivatives efficiently prepared via click chemistry and evaluated for their antitubercular, antioxidant, and cytotoxic activities.
DOI: 10.1039/C5MD00057B
Published: 12 May 2015

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