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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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Hongbin Yang, Xiao Li, Yingchun Cai, Qin Wang, Weihua Li, Guixia Liu and Yun Tang
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C7MD00074J, Research Article
Chemical subcellular localization is closely related to drug distribution in the body, and hence important in drug discovery and design. Although many in vivo and in vitro methods have been...
 
Ji Liu, Tingting WANG, Xinyang Wang, Lin Luo, Jing Guo, Yanfu Peng, Qibin Xu, Jiefei Miao, Yanan Zhang and Yong Ling
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00681G, Research Article
A series of novel β-carboline-based hydroxamate derivatives (8a−n) as HDAC inhibitors have been designed and synthesized. Most of these compounds displayed potent histone deacetylase inhibitory effects and good antiproliferative activity...
 
Sandeep Sundriyal, Patty B. Chen, Alexandra S. Lubin, Gregor A. Lueg, Fengling Li, Andrew J. P. White, Nicholas A. Malmquist, Masoud Vedadi, Artur Scherf and Matthew J. Fuchter
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00052A, Research Article
We identify key SAR features which demonstrate that high parasite vs. G9a selectivity can be achieved for the quinazoline inhibitor chemotype.
 
Nan Zhou, Tian Feng, Xin Shen, Jiahui Cui, Rangxin Wu, Libin Wang, Siwang Wang, Shengyong Zhang and Hui Chen
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00017K, Research Article
Some novel α,β-unsaturated aromatic sulfone analogs and Tempol conjugates are prepared and evaluated for their radioprotective activity, revealing that the agents have both prophylactic and mitigation effects against radiation damage.
 
S. Shaabani, C. G. Neochoritis, A. Twarda-Clapa, B. Musielak, T. A. Holak and A. Dömling
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00058H, Research Article
The discovery of a novel potent p53-MDM2 antagonistic small molecule scaffold using a mix of computational, chemistry and biophysical techniques.
 
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00703A, Research Article
We systematically evaluated size-dependent and surface-dependent penetrability of upconversion nanoparticles towards the digestive system of the mouse through fluorescent signals and X-ray imaging.
 
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C7MD00063D, Research Article
Emergence of drug resistance in Plasmodium falciparum to the available antimalarial drugs has challenged the current antimalarial treatments. New antimalarials, particularly those with novel mechanisms of action and no cross...
 
Neeraj N. Patwardhan, Laura R. Ganser, Gary J. Kapral, Christopher S. Eubanks, Janghyun Lee, Bharathwaj Sathyamoorthy, Hashim M. Al-Hashimi and Amanda E. Hargrove
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00729E, Research Article
NMR-guided evolution of the pyrazine C(5)- and C(6)-positions of amiloride reveals a tunable scaffold for selective RNA interactions.
 
Vigneshwari Subramanian, Qurrat Ul Ain, Helena Henno, Lars-Olof Pietilä, Julian E. Fuchs, Peteris Prusis, Andreas Bender and Gerd Wohlfahrt
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00701E, Research Article
Field-based proteochemometric modelling predicts activities and visualizes features, which can support the design of more selective protease inhibitors.
 
Exequiel O. J. Porta, Sebastián N. Jäger, Isabel Nocito, Galina I. Lepesheva, Esteban C. Serra, Babu L. Tekwani and Guillermo R. Labadie
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00008A, Research Article
A series of prenyl 1,2,3-triazoles were prepared from isoprenyl azides and different alkynes. Most of the compounds were active against T. cruzi and L. donovani.
 
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00025A, Research Article
It is the first reported the synthesis of 1,2-benzoxazepinone. These compounds showed excellent fungicidal activity.
 
Ibrahim Bin Sayeed, V. Lakshma Nayak, Mohd Adil Shareef, Neeraj Kumar Chouhan and Ahmed Kamal
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00043J, Research Article
A library of imidazopyridine–propenone conjugates (8a–8u) were synthesized and evaluated for their antitumor activity against four human cancer cell lines.
 
Mallikarjun Gosangi, Hithavani Rapaka, Thasneem Yoosuf Mujahid and Srilakshmi V. Patri
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00699J, Research Article
Synthesis, characterization and evaluation of transfection efficiencies of a series of dicationic amphiphiles designed to have two diverse cationic moieties mutually linked as head group of aliphatic backbone based lipids.
 
Zhifeng Chen, Hao Zhang, shien liu, Yiqian Xie, Hao Jiang, Wenchao Lu, Heng Xu, Liyan Yue, yuanyuan Zhang, Hong Ding, Kunqian Yu, Mingyue Zheng, Kaixian Chen, Hualiang Jiang and Cheng Luo
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C7MD00083A, Research Article
As a member of the bromodomain and extra terminal domain (BET) protein family, BRD4 is closely related to cancers and other diseases. Small-molecule BRD4 inhibitors have already demonstrated promising potentials...
 
Fei Zhao, Huai-Huai Dong, Yuan-Hua Wang, Tian-Yi Wang, Ze-Hao Yan, Fang Yan, Da-Zhi Zhang, Ying-Ying Cao and Yong-Sheng Jin
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00649C, Research Article
Twenty-three monoketone derivatives of curcumin were synthesized to restore the effectiveness of fluconazole against fluconazole-resistant Candida spp.. The minimal inhibitory concentration (MIC80) and the fractional inhibitory concentration index (FICI) of...
 
Yoshihiro Shuto, Simone Thum, Louisa Temme, Dirk Schepmann, Masato Kitamura and Bernhard Wünsch
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00621C, Research Article
An F-atom in the phenylalkyl side chain of GluN2B antagonists does not affect the affinity towards GluN2B receptors.
 
Hui Deng, Tom van der Wel, Richard J. B. H. N. van den Berg, Adrianus M. C. H. van den Nieuwendijk, Freek J. Janssen, Marc P. Baggelaar, Hermen S. Overkleeft and Mario van der Stelt
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00029D, Research Article
The enantioselective synthesis and structure–activity relationships of deoxy-iminosugar-based triazole ureas as dual inhibitors of DAGLα and ABHD6 were reported.
 
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00697C, Research Article
Carboxymethylated and sulfated polysaccharides (CLEP and SLEP) were prepared from an exopolysaccharide previously obtained from Lachnum YM240 (LEP) by chemical modifications.
 
Entsar Ali Saad, Mohammed Hassanien, Hatem El-Mezayen and Nada M ELmenawy
Med. Chem. Commun., 2017, Accepted Manuscript
DOI: 10.1039/C6MD00618C, Research Article
Cisplatin as a mean chemotherapy had nephro-toxicity and so tray to develop novel antitumor drug based on combination of cobalt metal ion with organic moiety. Antitumor activity of the complex...
 
A. S. Sokolova, O. I. Yarovaya, M. D. Semenova, A. A. Shtro, I. R. Orshanskaya, V. V. Zarubaev and N. F. Salakhutdinov
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00657D, Research Article
Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (−)-borneol and (−)-isoborneol as potent inhibitors of the influenza A virus.
 
S. Chaturvedi, A. Kaul, Puja P. Hazari and Anil K. Mishra
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00610H, Review Article
Development in metal based radiopharmaceuticals – review on design considerations, ongoing research and future directions.
 
Ari Miranda da Silva, Leonardo Araújo-Silva, Ana Cristina S. Bombaça, Rubem F. S. Menna-Barreto, Claudio Eduardo Rodrigues-Santos, Aurélio B. Buarque Ferreira and Solange L. de Castro
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00069C, Research Article
The trypanocidal activity of N-hexyl naphthoimidazoles (and other N-alkyl-naphthoimidazoles) is demonstrated for the first time, supporting further studies for rational chemical optimization.
 
Katherine A. Hurley, Thiago M. A. Santos, Molly R. Fensterwald, Madhusudan Rajendran, Jared T. Moore, Edward I. Balmond, Brice J. Blahnik, Katherine C. Faulkner, Marie H. Foss, Victoria A. Heinrich, Matthew G. Lammers, Lucas C. Moore, Gregory D. Reynolds, Galen P. Shearn-Nance, Brian A. Stearns, Zi W. Yao, Jared T. Shaw and Douglas B. Weibel
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C7MD00012J, Research Article
New gyramide antibiotics with reduced drug efflux and improved antibiotic activity against pathogenic bacteria.
 
A. V. Subba Rao, Bala Bhaskara Rao, Satish Sunkari, Siddiq Pasha Shaik, Bajee Shaik and Ahmed Kamal
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00562D, Research Article
A new series of 2-arylaminobenzothiazole-arylpropenone conjugates were designed based on 5F-203, synthesized and evaluated for their cytotoxic potency as well as inhibition of tubulin polymerization.
 
Med. Chem. Commun., 2017, Advance Article
DOI: 10.1039/C6MD00646A, Research Article
This study aimed to elucidate the therapeutic effects of oral administration of intracellular melanin from Lachnum YM156 (LIM) on chronic renal failure (CRF) in mice.
 

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20 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
22 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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