Journal cover: MedChemComm

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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Jiadi Gao, Cheng Fang, Zhiyan Xiao, Li Huang, Chin Ho Chen, Li-Ting Wang and Kuo-Hsiung Lee
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00412D, Concise Article
Based on a 3D-QSAR pharmacophore derived from a diverse set of known cyclin-dependent kinase 9 (CDK9) inhibitors and a composite pharmacophore extracted from the complex structure of flavopiridol (FVP)-CDK9, thirty...
 
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.
 
Michelle Gazdik, Matthew Troy O'Neill, Sash Lopaticki, Kym Lowes, Brian J Smith, Alan Cowman, Justin Boddey and Brad E. Sleebs
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00409D, Concise Article
N-Methylation of the N–Cα peptide bond is a known strategy to overcome the liabilities inherently associated with peptide-like molecules. Here, we apply this strategy to transition state mimetics that are...
 
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.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00407H, Concise Article
A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferative activity against four kinds of tumor cell lines. These compounds displayed potent antiproliferative activity. In particular, compound 3f exhibited superior antiproliferative activity against these tumor cell lines than GNA.
 
Narmada Bag, Rashi Mathur, Sweta Singh, Firasat Hussain, Ramprakash Chauhan, krishna Chuttani and Anil K Mishra
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00294F, Concise Article
The biomedical application of semiconductor quantum dots (QDs) are still limited due to the decrease in their photoluminescence (PL) after surface modification for target specificity and in vivo imaging. This...
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00272E, Concise Article
The work reports the preparation of antimicrobial spine-bone-cement with a highly controlled release formulation that was subjected to tests, involving in vitro and in vivo biological assessments such as antimicrobial effects, a cytotoxicity test, a bacterial reverse mutation (Ames) assay, a micronucleus assay, and implantation analysis.
 
Eleni Pitta, Evangelia Tsolaki, Athina Geronikaki, Jovana Petrović, Jasmina Glamočlija, Marina Soković, Emmanuele Crespan, Giovanni Maga, Shome S. Bhunia and Anil K. Saxena
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00399C, Concise Article
A series of ten thiazolidin-4-one derivatives was synthesized and evaluated for their antibacterial, antifungal and HIV-1 reverse transcriptase (RT) inhibitory activity.
 
Shinichi Kuno, Katsumi Higaki, Atsushi Takahashi, Eiji Nanba and Seiichiro Ogawa
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00270A, Concise Article
The development of chemical chaperones to decrease the inhibitory activity while increasing the enzyme enhancement activity is described.
 
Antonio Rescifina, Angela Scala, Maria Teresa Sciortino, Ivana Colao, Gabriel Siracusano, Antonino Mazzaglia, Ugo Chiacchio and Giovanni Grassi
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00364K, Concise Article
Decorated 6,6′,7,7′-tetrahydro-1H,1′H-2,3′-biindoles, such as DPIT, targeting CDK2 seem to be an attractive scaffold for development of useful anticancer drugs.
 
Md. Amirul Islam, Yuqi Zhang, Yao Wang and Shelli R. McAlpine
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00387J, Concise Article
Herein we report the synthesis and biological activity evaluation of 2,4 linked azole-containing molecules.
 
Doaa Boshra Farag, Nahla A. Farag, Ahmed Esmat, Sally A. Abuelezz, Eman Abdel-Salam Ibrahim and Dalal A. Abou El Ella
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00392F, Concise Article
Four novel series of quinazoline derivatives IIIa–c, VIa–c and their NO-hybrid molecules as nitrate esters Va–c and VIIIa–c have been synthesized and evaluated for their anti-inflammatory activity in vivo and in vitro.
 
Elizabeth Robinson, Euphemia Leung, Anna M. Matuszek, Niels Krogsgaard-Larsen, Daniel P. Furkert, Margaret A. Brimble, Alan Richardson and Jóhannes Reynisson
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00420E, Concise Article
Compounds 14 and 62 were identified using virtual screening to inhibit autophagy. The expression levels of the LC3-II and p62 autophagy proteins were used. SAR analysis revealed another active compound 38. Formation of autophagosomes was severely reduced upon dosing of 14, 38 and 62.
 
Francesca Bianchini, Chiara Calugi, Jessica Ruzzolini, Gloria Menchi, Lido Calorini, Antonio Guarna and Andrea Trabocchi
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00287C, Concise Article
A D-proline peptidomimetic targeting MMP-2 and MMP-9 was identified from a pool of compounds following enzyme inhibition kinetics and Matrigel sponge assays, showing the capacity of blocking capillary network formation in vivo.
 
Urara Hasegawa and André J. van der Vlies
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00373J, Concise Article
Hydrogen sulfide-releasing polymeric micelles enhanced pro-inflammatory responses induced by gardiquimod, a toll-like receptor 7 ligand, showing potential in immunotherapy and vaccine development.
 
Anastasiya I. Govdi, Nadezda V. Sokolova, Irina V. Sorokina, Dmitry S. Baev, Tatyana G. Tolstikova, Victor I. Mamatyuk, Dmitry S. Fadeev, Sergey F. Vasilevsky and Valentine G. Nenajdenko
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00236A, Concise Article
Betulinic acid–peptide conjugates exhibit high anti-inflammatory activity.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00281D, Concise Article
A series of quinazolinone azoles were synthesized and screened for their antimicrobial activities, and further studies of their binding behaviors with calf thymus DNA and human serum albumin were investigated.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00352G, Concise Article
Since fungal natural products biosynthesized by polyketide synthases frequently exhibit useful biological activities, identifying and understanding the mechanism of biosynthetic steps taken by PKSs are of great interest.
 
Barbara Cortese, Stefania D'Amone, Giuseppe Gigli and Ilaria Elena Palamà
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00348A, Concise Article
IM–chitosan complex encapsulated poly(ε-caprolactone) (PCL) nanoparticles are proposed for their potential in enabling more intelligent controlled release and enhancing chemotherapeutic efficiency of IM.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00257A, Concise Article
Compound 9a showed dual anticancer and antimicrobial activity and compound 16 showed a broad spectrum antimicrobial activity.
 
Victoria Vinader, Maria Sadiq, Mark Sutherland, Mengying Huang, Paul M. Loadman, Lina Elsalem, Steven D. Shnyder, Hongjuan Cui, Kamyar Afarinkia, Mark Searcey, Laurence H. Patterson and Klaus Pors
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C4MD00411F, Concise Article
Selective cytochrome P450 bioactivation of truncated azinomycin.
 

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