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MedChemComm

Broadening the field of opportunity for medicinal chemists. Official journal of the European Federation for Medicinal Chemistry
Impact Factor 2.495 12 Issues per Year
 
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Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00303B, Review Article
Positron emission tomography (PET) is a modern in vivo imaging technique and an important diagnostic modality for clinical and pre-clinical research. The incorporation of a radionuclide like fluorine-18 into a...
 
Jeroen Van Soom, Giuliana Cuzzucoli Crucitti, Rafaela Gladysz, Pieter Van der Veken, Roberto Di Santo, Ingmar Stuyver, Victoria Buck, Anne-Marie Lambeir, Viktor Magdolen, Jurgen Joossens and Koen Augustyns
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00288E, Concise Article
KLK4 is a serine protease from the kallikrein family that is involved in cancer progression. The diphenyl phosphonate warhead is intended to bind irreversibly with serine proteases, but unexpectedly, very...
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00231A, Concise Article
Acetylcholinesterase is an important enzyme, currently used as therapy for controlling the effects of Alzheimer’s disease that has been accepted as one of the major threat to the elderly population....
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00247H, Concise Article
Navigating into the chemical space between MGCD0103 and SAHA using two novel histone deacetylase inhibitors.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD90042E, In the Pipeline
There are plenty of things that small molecule drugs can't touch, says Derek Lowe, and it's not for want of trying.
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00253B, Concise Article
A property-based desirability scoring scheme has been developed for kinase-focused library design and ligand-based pre-screening of large compound sets. Property distributions of known kinase inhibitors from the ChEMBL Kinase Sarfari...
 
Amelia Santos, Catarina Quintanova, Rangappa S Keri, Sergio Marques, Sandra Cardoso, M L. M. Serralheiro and Maria Gonçalves Fernandes
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00236B, Concise Article
A series of novel tacrine-cinnamate and tacrine-cinnamylidene acetate hybrids have been designed, synthesized and evaluated as multitarget compounds for the treatment of Alzheimer´s disease. Results from the assessment of their...
 
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00299K, Concise Article
Supramolecular polymer micelles (SMPMs) engineered by host-guest interaction of α-cyclodextrin (α-CD) and poly(ε-capralactone) (PCL) homopolymer have been recently reported as robust drug delivery system. The incorporation of supramolecular chemistry affords...
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00197H, Concise Article
Twenty-one nitrogen-containing heterocyclic stilbenes were synthesized. Their cytotoxicity and effect on VEGF protein secretion as well as VEGF, hTERT and c-Myc gene expression were evaluated.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00309A, Concise Article
The impact of N- and O-methylation on aqueous solubility and measured lipophilicity for several chemically diverse structural classes is described.
 
Sukhamoy Gorai, Saurav Paul, Ganga Sankaran, Rituparna Borah, Manas Kumar Santra and Debasis Manna
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00260E, Concise Article
4-Amino-1,2,5-oxadiazole derivatives has been developed as an inhibitor of AKT pleckstrin homology domain.
 
Gary Tin, Tarek Mohamed, Nyasha Gondora, Michael A. Beazely and Praveen P. N. Rao
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00274E, Concise Article
From themed collection 2015 MedChemComm Hot Articles
A group of tricyclic phenothiazines (6a, 6b and 7a–l) and phenoselenazines (12a, 12b and 13a–l) was designed, synthesized and evaluated as multi-targeting ligands aimed at the cholinergic, amyloid and oxidative stress pathways of Alzheimer's disease.
 
Mohammad Shadid, Gabriela Gurau, Julia L. Shamshina, Bei-Ching Chuang, Shumet Hailu, Emily Guan, Swapan Chowdhury, Jing-Tao Wu, Syed A. A. Rizvi, Robert Griffin and Robin D. Rogers
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00290G, Concise Article
The absorption, distribution, metabolism, and excretion (ADME) properties of a cholinium ionic liquid (IL) salt of the poorly soluble drug sulfasalazine were evaluated in both in vitro and in vivo...
 
Ahmed Kamal, Subba Rao A.V., Srinivasa Reddy Telukutla, Sowjanya Polepalli, chandrakant Bagul, Vishnuvardhan MVPS, Siddiq Pasha Shaik and Nishant Jainb
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00155B, Concise Article
Two series of 2-ethyl -6-(3’,4’,5’-trimethoxyphenyl)-5-aryl and 2-cyclopropyl -6-(3’,4’,5’-trimethoxyphenyl)-5-aryl-imidazothiadiazoles were designed, synthesized and evaluated for anti-proliferative activity in various human cancer cell lines. A common starting material 2-bromo-1-(3-,4-,5-trimethoxyphenyl)-ethanone was employed to...
 
Xu-Yao Zhang, Yi-Fei Gu, Ting Chen, Dong-Xiao Yang, Xi-Xin Wang, Bai-Ling Jiang, Kun-Peng Shao, Wen Zhao, Cong Wang, Jun-Wei Wang, Qiu-Rong Zhang and Hong-Min Liu
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00240K, Concise Article
To develop potent and selective anticancer agents, a series of novel 4-substituted 1,2-bis(4-chlorophenyl)-pyrazolidine-3,5-dione derivatives were designed and synthesized.
 
Sheo B. Singh, David E. Kaelin, Jin Wu, Lynn Miesel, Christopher M. Tan, Peter T. Meinke, David B. Olsen, Armando Lagrutta, Changqing Wei, Yonggang Liao, Xuanjia Peng, Xiu Wang, Hideyuki Fukuda, Ryuta Kishii, Masaya Takei, Takeshi Shibata, Tomoko Takeuchi, Kohei Ohata, Akinori Nishimura and Yasumichi Fukuda
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00297D, Concise Article
Substitutions around linker positions C-1 and C-2 suggest that the C-2α hydroxy group is the best for activity.
 
Wenfeng Liu, Yuan Yue, Yonglian Li, Xi Zheng, Kun Zhang and Zhiyun Du
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00308C, Concise Article
Magnolol is a major active constituent of Magnolia officinalis, which is a natural traditional Chinese medicine. Inspired by magnolol, showed a wide diversity of bioactivities, a series of magnolol derivatives...
 
Muhammad Taha, Nor Ismail Ismail, Syahrul Imran, Abdul Wadood, Fazal Rahim, Muhammad Ali and Ahsfaq Rehman
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00280J, Concise Article
A new series of quinoline derivatives 6-30 was identified as potent α-glucosidase inhibitors. These analogs exhibited inhibitory potentials (IC50 values) in the ranges between 2.60 to 102.12 μM. Among the...
 
Zhiyong Yu, James A. Brannigan, Kaveri Rangachari, William P. Heal, Anthony J. Wilkinson, Anthony A. Holder, Robin J. Leatherbarrow and Edward W. Tate
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00242G, Concise Article
From themed collection 2015 MedChemComm Hot Articles
Scaffold hopping and structure-guided optimisation led to a new class of potent Plasmodium N-myristoyltransferase inhibitors with cellular activity.
 
Mark D. Rackham, Zhiyong Yu, James A. Brannigan, William P. Heal, Daniel Paape, K. Victoria Barker, Anthony J. Wilkinson, Deborah F. Smith, Robin J. Leatherbarrow and Edward W. Tate
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00241A, Concise Article
From themed collection 2015 MedChemComm Hot Articles
Truncation converted a Plasmodium N-myristoyltransferase inhibitor into a Leishmania-selective series, leading to a potent L. donovani NMT inhibitor through structure-guided design.
 
Ainhoa Mascaraque, Wioleta Kowalczyk, Tahia Fernández, Francisca Palomares, Cristobalina Mayorga, David Andreu and Javier Rojo
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00133A, Concise Article
From themed collection 1st EFMC Young Medicinal Chemist Symposium
A GDP displaying the NP366–374 influenza A virus epitope induces an immunostimulatory effect, emerging as a potential flu vaccine.
 

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