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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
Impact Factor 2.319 12 Issues per Year
 
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Narisa Phummarin, Helena Boshoff, Patricia Tsang, James Dalton, Siouxsie Wiles, Barry Clifton and Brent R. Copp
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00236F, Research Article
A previous phenotypic screen by GSK identified 2-(quinolin-4-yloxy)acetamides as potent growth inhibitors of Mycobacterium tuberculosis (Mtb). We report the results of a preliminary structure-activity relationship (SAR) study of the compound...
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00328A, Research Article
Glycosylated antitumor ether lipids (GAELs) are a class of amphiphilic antitumor agents that kill cancer cells by a non-apoptotic pathway.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00378H, Research Article
Benzimidazole analogs were previously shown to inhibit sirtuin activity. Novel compound 5i was found to be a potent SIRT2 inhibitor with an IC50 value of 2.92 μM.
 
Xuefeng Sun, Ningning Fan, Weisi Xu, Yixing Sun, Xin Xie, Ying Guo, Liying Ma, Junyi Liu and Xiaowei Wang
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00311G, Research Article
Novel series of caffeoyl benzanilides have been synthesized and evaluated as dual inhibitors of HIV-1 CCR5/IN. Compound 9a exhibited the possibility of being a dual inhibitor of HIV-1.
 
Lydia Radi, Matthias Fach, Mirko Montigny, Elena Berger-Nicoletti, Wolfgang Tremel and Peter R. Wich
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C5MD00475F, Research Article
From themed collection New Talent: Europe
We evaluated different methods for a high surface PEGylation of lysozyme. The resulting lipophilic enzymes can be used for the formation of stable nanoparticles.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00006A, Research Article
In the present study, eleven glutathione-derived peptides, including Glu-Cys-His, Pro-Leu-Gly, Pro-Cys-Gly, Phe-Lys-Leu, Leu-His-Gly, Lys-Leu-Glu, Lys-Val-His, Tyr-Glu-Gly, Tyr-His-Leu, Gly-Glu-Leu and Gly-Pro-Glu, were designed.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00288A, Research Article
From themed collection DNA Encoded Libraries
Enrichment of DNA-encoded ligands under stringent, protein-denaturing conditions is enabled by crosslinking with electrophilic or photoreactive groups.
 
Jia Wang, Xiao-Yang Fan, Li-Yun Yang, Huan He, Rong Huang, Feng-Lei Jiang and Yi Liu
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00268D, Research Article
5-Fluorouracil (5-FU) was linked with mitochondria-targeting lipophilic cation F16 by three kinds of vulnerable bonds.
 
Vishnu Lal Sharma, Sonal Gupta, Deepti Pandey, Dhanaraju Mandalapu, Veenu Bala, Vikas Sharma, Mahendra Shukla, Santosh Kumar Yadav, Nidhi Singh, Swati Jaiswal, Jagdamba Prasad Maikhuri, Jawahar Lal, M. I. Siddiqi and Gopal Gupta
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00426A, Research Article
In the quest of novel scaffolds for the management of androgen sensitive prostatic disorders like prostate cancer and benign prostatic hyperplasia, a series of twenty-six aryl/heteroaryl piperazine derivatives have been...
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00362A, Research Article
This study considers how the estimated in vivo free plasma concentrations for compounds tends to vary between human, dog and rat and proposes empirical-based criteria to aid drug design.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00381H, Research Article
From themed collection 2016 MedChemComm Hot Articles
We disclose a microwave-enhanced Friedländer reaction that led to new antibacterials and biofilm-eradicators.
 
Mahyar Bonsaii, Khodayar Gholivand, Khosrou Abdi, Ali Asghar Ebrahimi Valmoozi and Morteza Khosravi
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00264A, Research Article
From themed collection 2016 MedChemComm Hot Articles
In the present work, we suggest that the role of water in the reaction of nitrogen mustards with DNA is more than what was thought before. Nitrogen mustards become activated when they are hydrated by water.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00215C, Research Article
From themed collection 2016 MedChemComm Hot Articles
A series of findings suggest that the discovery of in vivo apoptosis inducers for chemotherapy is of clinical importance.
 
Elham Rezaee Zavareh, Mahdi Hedayati, Laleh Hoghooghi Rad, Soraya Shahhosseini, Mehrdad Faizi and Sayyed Abbas Tabatabai
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00395H, Research Article
Inhibition of soluble epoxide hydrolase (sEH) enzyme leads to high levels of epoxyeicosatrienoic acids which are involved in the regulation of blood pressure and vascular inflammation. The most potent sEH...
 
Dinesh Addla, Si-Qi Wen, Wei-Wei Gao, Swetha Kameswari Maddili, Ling Zhang and Cheng-He Zhou
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00357E, Research Article
Synthesis of a series of carbazole aminothiazoles as a new type of potential antimicrobial agents, and preliminary interactions with DNA indicated a possible intercalation mechanism.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00263C, Research Article
Fatty acid biosynthesis is essential for bacterial survival.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00336B, Research Article
Carbon monoxide released from CORM-2 inhibits Crotalus atrox snake venom metalloproteinase mediated decreases in human plasma velocity of coagulation.
 
M. Klika Škopić, O. Bugain, K. Jung, S. Onstein, S. Brandherm, T. Kalliokoski and A. Brunschweiger
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00243A, Research Article
From themed collection DNA Encoded Libraries
DNA-encoded libraries based on scaffolds functionalized for DNA-compatible chemistry were synthesized by split-and-pool combinatorial chemistry. The library design was aided by a chemoinformatic filtering cascade.
 
Rupinder Kaur Gill, Ramandeep Kaur, Virender Kumar, Vivek Gupta, Gagandeep Singh and Jitender Bariwal
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00256K, Research Article
In the present study, 2-phenyl/2-phenylethynyl-3-aroyl thiophenes have been designed and evaluated as antiproliferative agents. The significant antiproliferative potential of compounds 12j and 14h were might be attributed to their potential to induce cell cycle arrest at G2/M phase.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00297H, Review Article
HDAC inhibitors are a promising group of epigenetic drugs that show the ability to induce apoptosis in cancer stem cells.
 
Christopher P. Tinworth, Hannah Lithgow and Ian Churcher
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00347H, Review Article
Research into degradation of cellular proteins induced by small molecule agents known as Protacs has gathered pace recently. This article reviews recent progress and assesses the challenges to be addressed to enable clinical evaluation of agents.
 
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00365F, Research Article
A library of 33 compounds was screened for potentiation of the antibiotic FR 900098 against the Francisella tularensis surrogate Francisella novicida.
 
Jinbao Xiang, Zhuoqi Zhang, Renzhong Fu, Robert J. Ternansky, Patricia L. Gladstone, Amy L. Allan, Fernando Donate, Graham Parry, Jose Juarez, Andrew P. Mazar and Xu Bai
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00351F, Research Article
An efficient strategy for the discovery of kinase inhibitors by a combination of diversity-oriented synthesis and selective screening was presented.
 
Xu Han, Yongying Shi, Longlong Si, Zibo Fan, Han Wang, Renyang Xu, Pingxuan Jiao, Kun Meng, Zhenyu Tian, Xiaoshu Zhou, Hongwei Jin, Xinyu Wu, Hong Chen, Yongmin Zhang, Lihe Zhang, Sulong Xiao and Demin Zhou
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00292G, Research Article
From themed collection 2016 MedChemComm Hot Articles
A total of 24 novel sialic acid–pentacyclic triterpene conjugates were synthesized and evaluated as anti-influenza virus entry inhibitors.
 
Sharan K. Bagal, Mark I. Kemp, Peter J. Bungay, Tanya L. Hay, Yoshihisa Murata, C. Elizabeth Payne, Edward B. Stevens, Alan Brown, David C. Blakemore, Matthew S. Corbett, Duncan C. Miller, Kiyoyuki Omoto and Joseph S. Warmus
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00281A, Research Article
Potent and subtype selective Nav1.8 inhibitors were designed and optimised for selectivity over hERG ion channel inhibition.
 

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13 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
8 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
20 citations
Chemically modified antisense oligonucleotides have shown persistent value both in the terms of their success as approved drugs and seminal findings, leading to numerous potential drug candidates in clinical trials.
DOI: 10.1039/C4MD00184B
Published: 01 Aug 2014

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