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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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Ling Zhang, Vijaya Kumar Kannekanti, RASHEED SYED, Shao-Lin Zhang, Rong-Xia Geng and Cheng-He Zhou
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00186B, Concise Article
A series of azolylthioether quinolones were synthesized and characterized by NMR, IR, MS and HRMS spectra. All the newly prepared compounds were screened for their antimicrobial activities. Bioactive assay manifested...
 
Heather Tye, Stephan Zahn, Marco Hofmann, Michael Sanderson, Otmar Schaff, Matthias Troy, Moritz Mayer, Georg Rast, Sandeep Pal and Ulrich Guertler
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00097A, Concise Article
The insulin-like growth factor-1 receptor (IGF1R) and closely related insulin receptor (INSR) are receptor tyrosine kinases which have been postulated to play a role in the tumorigenesis of certain cancers....
 
Xiaoyan Yang, Zicheng Li, Zhenling Wang, Zitai Sang, Haiyue Long, Jianying Tang, Tao Yang, Yuanyuan Liu and Youfu Luo
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00101C, Concise Article
Monofluoro- (39), difluoro- (40) and trifluoro- (41) substituted analogues showed different biological activities, and 40 is a potent antibacterial agent in animal models.
 
Diana Castagna, Emma L. Duffy, Dima Semaan, Louise C. Young, John M. Pritchard, Simon J. F. Macdonald, David C. Budd, Craig Jamieson and Allan J. B. Watson
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00081E, Concise Article
Starting from the known LPA1 antagonist 4, three novel series of autotaxin inhibitors exemplified by 7, 8 and 9 were identified using a combination of scaffold hopping and ligand-based design.
 
Yu Zhang, Xuefeng Sun, Ningning Fan, Jianxiong Zhao, Jing Tu, Xiangmei Chen, Junyi Liu and Xiao-wei Wang
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00181A, Concise Article
A series of 5-Iodo-2-arylalkylthio-6-aryl pyrimidin-4(3H)-ones, which can be considered as S-DABO derivatives, have been synthesized and their antiviral effect on extracellular HBV DNA was evaluated using the HepAD38 cell system....
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00042D, Concise Article
99m TcO-N4IPDTC was prepared from a kit without the need for purification and would be a promising hypoxia imaging agent.
 
Barbora Servusova-Vanaskova, Ondrej Jandourek, Pavla Paterova, Jana Kordulakova, Magdalena Plevakova, Vladimir Kubicek, Radim Kucera, Vladimir Garaj, Lieve Naesens, Jiří Kuneš, Martin Dolezal and Jan Zitko
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00178A, Concise Article
A series of alkylamino derivatives of N-benzylpyrazine-2-carboxamide was designed, synthesized and assayed in vitro for their antimycobacterial, antibacterial, antifungal as well as antiviral activity. Final structures were prepared from 6-chloro...
 
Christos Papaneophytou, Polyxeni Alexiou, Athanasios Papakyriakou, Evangelos Ntougkos, Katerina Tsiliouka, Anna Maranti, Fotini Liepouri, Alexandros Strongilos, Anthi Mettou, Elias Couladouros, Elias Eliopoulos, Eleni Douni, George Kollias and George Kontopidis
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00023H, Concise Article
Inhibition of Tumor Necrosis Factor (TNF) production or function by small molecules has become a major focus in the pharmaceutical industry for the treatment of Rheumatoid Arthritis. In this study,...
 
Jin-Shuai Lan, Sai-Sai Xie, Ming Huang, Ya-Jian Hu, Ling-Yi Kong and Xiao-Bing Wang
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00124B, Concise Article
A new series of C7-substituted chromanones has been designed, synthesized and evaluated for hMAO-B inhibitory activity in vitro. Most of the studied compounds were remarkably potent and selective MAO-B inhibitors,...
 
Paweł Maria Zajdel, Vittorio Canale, Anna Partyka, Krzysztof Marciniec, Grzegorz Satała, Rafał Kurczab, Agata Siwek, Magdalena Jastrzębska-Więsek, Anna Wesołowska, Tomasz Kos, Piotr Popik and AJ Bojarski
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00166H, Concise Article
A series of alkyl/arylsulfonamide derivatives of (aryloxy)ethylpiperidines as highly potent 5-HT7 receptor antagonists has been developed through structure-based design around the previously identified compound PZ-766. This resulted in highly potent...
 
Paul O'Neill, Sitthivut Charoensutthivarakul, David Hong, Suet Leung, Peter Gibbons, Gemma Nixon, Paul Bedingfield, Stephen Ward, Giancarlo Biagini, Alex Lawrenson and Neil Berry
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00062A, Concise Article
A series of 2-pyridylquinolones has been prepared in 5-7 steps and through lead optimisation, antimalarial activity as low as 12 nM against Plasmodium falciparum (Pf) has been achieved. Compared with...
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00147A, Concise Article
Short-interfering RNAs (siRNAs) are naturally occurring biomolecules used for post-transcriptional gene regulation, and therefore hold promise as a future therapeutic by silencing gene expression of overexpressed deleterious genes. However, there...
 
Chiyu Sun, Yangsheng Li, Ailong Shi, Jingzhou Zhang, Yafei Li, Mingming Zhao, Lijuan Zhang, Huachuan Zheng, Ying Meng, Huaiwei Ding and Hongrui Song
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00092K, Concise Article
7m, as a novel Hedgehog inhibitor, interacted closely with the smoothened receptor at the co-crystallized ligand (taledegib) site.
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00157A, Concise Article
Fragment-based drug design (FBDD) has emerged as an efficient hit identification and/or optimization strategy with a higher hit rate than high-throughput screening (HTS). Whereas fragment linking is more challenging, fragment...
 
Lucia Tamborini, Federica Mastronardi, Federica Dall'Oglio, Carlo De Micheli, Birgitte Nielsen, Leonardo Lo Presti, Paola Conti and Andrea Pinto
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00159E, Concise Article
New unconventional beta and gamma dipeptides, representing conformational constrained higher homologues of glutamic acid, have been prepared and tested as new pharmacological tools to investigate the iGluR binding domain, in...
 
Xianghua Li, Xuemin Wang, Chenjun Xu, Junkai Huang, Chengniu Wang, Xinyang Wang, Liqin He and Yong Ling
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00158G, Concise Article
Novel furoxan/gemcitabine hybrids displayed significant antitumor activities, in particular 10e, which could be independent of the nucleoside transporter, release high levels of NO, and induce cell apoptosis by regulating apoptotic related proteins in tumor cells in vitro.
 
Hailong Zhang, Yuhua Jiang, Sheng-gang Zhao, Li-qin Jiang, Yan Meng, Peng Liu, Myeong Ok Kim and Shupeng Li
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00038F, Concise Article
Mesoporous silica nanoparticle (MSN)-mediated glutathione (GSH) delivery for targeted protection of dopaminergic neuronal cells.
 
Angel Guerrero, Anna Rodriguez, Hugo Gutiérrez-de-Terán, David Rodriguez, José Brea, María Isabel Loza, Gloria Rosell and M. Pilar Bosch
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00086F, Concise Article
We report the synthesis and pharmacological characterization of a new series of adenosine derivatives on the four adenosine receptors (AR). In radioligand binding assays, some of the compounds (1, 4,...
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00185D, Concise Article
A novel gold(I) complex based on an aminotriazole N-heterocylic carbene ligand represents a promising scaffold to design anticancer bioorganometallics. The complex triggered cytotoxic effects in HT-29 and MDA-MB-231 cancer cells,...
 
Mubarak H. Shaikh, Dnyaneshwar D. Subhedar, Laxman Nawale, Dhiman Sarkar, Firoz A. Kalam Khan, Jaiprakash N. Sangshetti and Bapurao B. Shingate
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00057B, Concise Article
A library of thirty one 1,2,3-triazole derivatives efficiently prepared via click chemistry and evaluated for their antitubercular, antioxidant, and cytotoxic activities.
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00139K, Concise Article
A series of new benzylideneindanone derivatives were designed, synthesized and evaluated as antitumor agents. The structure - activity relationship (SAR) studies showed that derivatives with 4,5,6-trimethoxyl on indanone moiety displayed...
 
Andrea Pancotti, Silvia Parapini, Mario Dell'Agli, Luca Gambini, corinna galli, enrico sangiovanni, Nicoletta Basilico, Enrica Bosisio, Donatella Taramelli and Sergio Romeo
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00115C, Concise Article
We have previously described several potent dual inhibitors of Plasmodium falciparum (Pf) growth characterized by the presence of statin, a β-hydroxyl amino acid able to inhibit parasite’s plasmepsins (PLM). While...
 
Fang Xie, Torsten Kniess, Christin Neuber, Winnie Deuther-Conrad, Constantin Mamat, Brian P. Lieberman, Boli Liu, Robert H. Mach, Peter Brust, Jörg Steinbach, Jens Pietzsch and Hongmei Jia
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00079C, Concise Article
Novel sigma-2 ligand 1b induced G1 phase cell cycle arrest in DU145 cells and displayed antiproliferative activity.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00016E, Concise Article
From themed collection 2015 MedChemComm Hot Articles
The putative adenosine-hA2A AR recognition pathway is suggested by a series of Supervised Molecular Dynamics (SuMD) simulations.
 
Min Guo, Yue Zheng, Rusty Starks, Clement Opoku-Temeng, Xiaochu Ma and Herman O. Sintim
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00015G, Concise Article
From themed collection 2015 MedChemComm Hot Articles
Hydrolytically stable 3-aminooxazolidinone analogs of acylhomoserine lactone quorum sensing autoinducers can modulate LuxR-type proteins and hence analogs thereof hold promise as quorum sensing modulators for diverse applications.
 

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