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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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Atsushi Seki, Toshihiro Mori, Kouji Sasaki, Yoshiaki Takahashi, Toshiaki Miyake and Yuzuru Akamatsu
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00489B, Concise Article
Novel 17-membered azalides of N-methylated amine type were synthesized and their antibacterial activity was evaluated.
 
Na Liu, Diwakar Rai, Fabao Zhao, Haiyong Jia, Peng Zhan and Xinyong Liu
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00521J, Review Article
Hepatitis B is an infectious inflammatory disease of the liver, which is caused by hepatitis B virus (HBV). Nowadays, the dramatic development of new HBV inhibitors is focused on discovering...
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00401A, Concise Article
Small molecules featuring a hydroxamic acid or a benzamide zinc binding group (ZBG) are the most thoroughly studied histone deacetylase (HDAC) inhibitors. However, concerns about the pharmacokinetic liabilities of the...
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00485J, Review Article
The advent of next-generation sequencing (NGS) technology has plummeted the cost of whole genome sequencing, which has provided a long list of putative drug targets for a variety of diseases...
 
W Roy Jackson, Anh Chau, Grant Drummond, Bevyn Jarrott, Alyson Miller, Kamani Subasinghe, Christina Yan Ru Tan, Paul J White, Christine E Wright and James Ziogas
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00459K, Concise Article
Six derivatives containing mexiletine and its 2,6-dichloro analogue to which the potential antioxidant moiety isoindoline, its N-oxide and the N-hydroxy derivatives have been attached, have been evaluated as cardio-protective agents....
 
Dora B. Boggián, Patricia Cornier, Ernesto Mata, Viviana Blanck, Mariano Cárdenas and LP Roguin
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00430B, Concise Article
We described the design, synthesis and antiproliferative properties of a series of twenty 2β-methyl substituted penicillin derivatives. This analysis includes evaluation against HeLa and MCF-7 human tumor cell lines, and...
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00418C, Concise Article
A series of tris-(phenylalkyl)amines was synthesized and evaluated for affinity to 5-HT2 receptors. In general, the compounds displayed high affinity (4 of 11 analogs had Ki values < 10 nM)...
 
Li Wu, Ya Wu, Hongwei Jin, Liangren Zhang, Yujian He and XinJing Tang
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00378K, Concise Article
We report herein a possibility of modulating the structure of hairpin oligonucleotides (ODNs) with light. By using 4.4′-dihydroxyl azobenzene derivatives as suitable linker units, the hairpin conformation can be photocontrolled...
 
Jin-Shuai Lan, Long-Fei Pan, Sai-Sai Xie, Xiao-Bing Wang and Ling-Yi Kong
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00437J, Concise Article
A new series of 6-methyl-3-phenylcoumarins (3a-c and 5a-o) and 6-methyl-3-heteroarylcoumarins (5p-s) had been designed, synthesized and evaluated as monoamine oxidases inhibitors. The results demonstrated that a large proportion of the...
 
Midori A. Arai, Kenji Uemura, Nozomi Hamahiga, Naoki Ishikawa, Takashi Koyano, Thaworn Kowithayakorn, Tagrid Kaddar, Madeleine Carreau and Masami Ishibashi
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00495G, Concise Article
The first naturally occurring inhibitors of FANCF–Hes1 complex were isolated by a newly constructed protein-based high-throughput screening assay.
 
Martin Klečka, Lenka Poštová Slavětínská, Eva Tloušťová, Petr Džubák, Marián Hajdúch and Michal Hocek
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00492B, Concise Article
A series of novel 6-substituted 7-arylsulfanyl-7-deazapurine bases and nucleosides has been prepared for screening of anticancer activity. 7-Thienylsulfanyl-7-deazapurine bases exerted micromolar cytostatic affects.
 
Rajni Sharma, Santosh K. Guru, Shreyans K. Jain, Anup Singh Pathania, Ram A. Vishwakarma, Shashi Bhushan and Sandip B. Bharate
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00344F, Concise Article
The synthesis and biological evaluation of the semisynthetic analogs of glycyrrhetic acid are described.
 
Jiadi Gao, Cheng Fang, Zhiyan Xiao, Li Huang, Chin-Ho Chen, Li-Ting Wang and Kuo-Hsiung Lee
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00412D, Concise Article
Novel 5-fluoro-pyrimidine derivatives have been designed, synthesized and evaluated as potential CDK inhibitors as well as antitumor and anti-HIV agents.
 
Yoshiaki Masaki, Takeshi Inde, Tetsuya Nagata, Jun Tanihata, Takashi Kanamori, Kohji Seio, Shin'ichi Takeda and Mitsuo Sekine
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00468J, Concise Article
In this study, we have synthesized phosphorothioate derivatives of 2'-O-methyloligoribonucleotides incorporating 2′-O-methyl uridine (Um), 2′-O-methyl ribothymidine (Tm), 2′-O-methyl 2-thioudirine (s2Um), and 2′-O-methyl 2-thioribothymidine (s2Tm) residues. Their exon skipping activities were...
 
Jiang Wu, Julia Shin, Cara M. M. Williams, Kieran F. Geoghegan, Stephen W. Wright, David C. Limburg, Parag Sahasrabudhe, Paul D. Bonin, Bruce A. Lefker and Simeon J. Ramsey
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD90044H, Correction
 
Tim Potter, G Caron, Giuseppe Ermondi and Gayle Newbury
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00470A, Concise Article
Here we describe a new approach for facilitating a mechanistic understanding of high throughput Caco-2 permeability data. A large, uniform set of permeability data is reported, generated under two pH...
 
Michelle Gazdik, Matthew T. O'Neill, Sash Lopaticki, Kym N. Lowes, Brian J. Smith, Alan F. Cowman, Justin A. Boddey and Brad E. Sleebs
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00409D, Concise Article
An N-methylation strategy has been applied to transition state mimetics that are potent inhibitors of plasmepsin V to improve their physical characteristics and their ability to reduce the viability of Plasmodium parasites in culture.
 
Narmada Bag, Rashi Mathur, Sweta Singh, Firasat Hussain, Ram Prakash Chauhan, Krishna Chuttani and Anil Kumar Mishra
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00294F, Concise Article
Biotinylated dithiocarbamate ligand modified quantum dots improve targeting while maintaining the photoluminescence for efficient imaging applications.
 
Ahmed Kamal, Bharath Kumar G, Lakshma Nayak V, Santhosh Reddy Vangala, Anver Basha Shaik, Rajender Rajender and Kashi Reddy Methuku
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00400K, Concise Article
A series of imidazopyridine/imidazopyrimidine-benzimidazole conjugates (11a-t) were synthesized and evaluated for their antiproliferative activity. All these conjugates showed moderate to better cytotoxic activity against the human cervical (Hela), lung (A549),...
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00383G, Concise Article
We synthetically demonstrate that eight-membered heterocycles are the exclusive products of the reaction of acrolein with biologically relevant amines via an imino[4 + 4]cycloaddition.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00365A, Review Article
We review recent advances in our development of molecular imaging probes for PET, SPECT, and optical imaging for in vivo detection of β-amyloid plaques in the brain.
 
Jennifer L. Woodring, Gautam Patel, Jessey Erath, Ranjan Behera, Patricia J. Lee, Susan E. Leed, Ana Rodriguez, Richard J. Sciotti, Kojo Mensa-Wilmot and Michael P. Pollastri
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00441H, Concise Article
The repurposing of human tyrosine kinase inhibitor scaffolds for generation of antiparasitic agents has provided new lead compounds for tropical diseases.
 
Margherita Brindisi, Sandra Gemma, Sanil Kunjir, Luisa Di Cerbo, Simone Brogi, Silvia Parapini, Sarah D'Alessandro, Donatella Taramelli, Annette Habluetzel, Sofia Tapanelli, Stefania Lamponi, Ettore Novellino, Giuseppe Campiani and Stefania Butini
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00454J, Concise Article
Design, synthesis and molecular docking calculation studies led to the identification of novel spirocyclic peroxides with in vitro and in vivo antimalarial activity.
 
Federico Giannini, Marco Bartoloni, Lydia E. H. Paul, Georg Süss-Fink, Jean-Louis Reymond and Julien Furrer
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00433G, Concise Article
Novel dinuclear arene ruthenium trithiolato complexes containing a water-soluble peptide moiety in one of the three thiolato bridges were designed and evaluated against A2780 human ovarian cancer cells and against their cisplatin-resistant mutant A2780cisR.
 
Shikha S. Chauhan, Shashi Pandey, Rahul Shivahare, Karthik Ramalingam, Shagun Krishna, Preeti Vishwakarma, M. I. Siddiqi, Suman Gupta, Neena Goyal and Prem M. S. Chauhan
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00298A, Concise Article
Novel β-carboline–quinazolinone hybrids are able to inhibit Leishmania donovani TR (LdTR). Molecular docking studies to investigate possible binding sites were performed.
 

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