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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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Esra Filiz ONEN BAYRAM, Kerem Buran, Irem Durmaz, Barkin Berk and Rengul Cetin-Atalay
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00306C, Concise Article
Cancer results from unregulated cell growth. Reactivating the process of the programmed cell death, i.e. apoptosis, is a classical anticancer therapeutic strategy. The apoptosis-inducer property of the (2RS,4R)-2-phenyl-3-propynoyl-thiazolidine-4-carboxylic acid ethyl...
 
Maria Giovanna Chini, Claudia Ferroni, Vincenza Cantone, Paolo Dambruoso, Greta Varchi, Antonella Pepe, Katrin Fischer, Oliver Werz, Carlo Pergola, Ines Bruno, R Riccio and Giuseppe Bifulco
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00319E, Concise Article
We report a new potent revisited version of a triazole-based inhibitor obtained by structure-based drug design on the human mPGES-1 crystal structure. Moreover, we disclosed the substitution with a halogen...
 
Junhua Wang, Feng'e Sun, Leiqiang Han, Xuben Hou, Xiaole Pan, Renshuai Liu, Weiping Tang and Hao Fang
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00203B, Concise Article
From themed collection Epigenetics
Histone deacetylase (HDAC) is a clinically validated target for anti-tumor therapy. In order to increase HDAC inhibition and efficiency, we developed a series of novel substituted purine hydroxamic acids as...
 
Jaida Begum, Gergely Varga, Tibor Docsa, Pal Gergely, Joseph M Hayes, László Juhász and László Somsák
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00335G, Concise Article
Following our recent study of N-(β-D-glucopyranosyl)-oxadiazole-carboxamides (Polyák et al., Biorg. Med. Chem. 2013, 21, 5738) revealed as moderate inhibitors of glycogen phosphorylase (GP), in silico docking calculations using Glide have...
 
Paul Brennan, Katherine England, Anthony Tumber, Tobias Krojer, Giuseppe Scozzafava, Stanley Ng, Michelle Daniel, Aleksandra Szykowska, KaHing Che, Frank von Delft, Nicola A Burgess-Brown, Akane Kawamura and Christopher J Schofield
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00291A, Concise Article
From themed collection Epigenetics
A potent inhibitor of the JmjC histone lysine demethylase KDM2A (pIC50 7.2) with excellent selectivity over representatives from other KDM subfamilies has been developed; the discovery that a triazolopyridine compound...
 
Ying Liu, Yanan Liu, Licong Yang, Chengwen Cao, Yanhui Zhou and Jie Liu
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00201F, Concise Article
In this study, two similar ruthenium(II) complexes 1 and 2 were synthesized to explore their selectivity for binding loop isomers of the c-myc G-quadruplex.
 
Bruce A Lefker, Julia Shin, Cara Williams, Kieran F Geoghegan, Stephen W Wright, David Limburg, Paul Bonin, Simeon Ramsey, Jiang Wu and Parag Sahasrabudhe
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00259H, Concise Article
From themed collection Epigenetics
Bromodomain-containing proteins form the signal-reading element of a principal system for the control of gene expression in eukaryotes. Their potential as targets for selective drug action is increasingly being assessed...
 
Mohamed Ettaoussi, Basile Pérès, Christian Jarry, Viviane Pallage, Olivier Nosjean, Jean A. Boutin, Arnaud Gohier, Clotilde Mannoury la Cour, Daniel-Henri Caignard, Philippe Delagrange, Pascal Berthelot and Saïd Yous
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD90033B, Correction
 
Matthieu Schapira and Renato Ferreira de Freitas
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00269E, Review Article
From themed collection Epigenetics
PRMT inhibitors can compete with cofactor, substrate, or bind at allosteric sites found in the active or inactive states.
 
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00325J, Concise Article
A series of new compounds consisting of epipodophyllotoxin-chalcone hybrids was synthesized towards the development of better anticancer lead molecules. These hybrids consist of structurally different but functionally similar topoisomerase-II inhibitors...
 
Nitipol Srimongkolpithak, Sandeep Sundriyal, Fengling Li, Masoud Vedadi and Matthew J. Fuchter
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00274A, Concise Article
From themed collection Epigenetics
With the aim of discovering novel G9a inhibitory chemotypes, we have identified a new quinoline inhibitor scaffold and better defined the pharmacophoric features of the central heterocycle.
 
Ahmed Kamal, Vangala Santhosh Reddy, Karnewar Santosh, G. Bharath Kumar, Anver Basha Shaik, Rasala Mahesh, Sumit. S. Chourasiya, Ibrahim Bin Sayeed and Srigiridhar Kotamraju
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00228H, Concise Article
A library of imidazothiadiazole–chalcone conjugates were synthesised and investigated for their cytotoxic activity against various human cancer cell lines. Some of the tested compounds like 7a, 7b, 11a and 11b exhibited promising anticancer activity.
 
P. J. Bindu, K. M. Mahadevan, T. R. Ravikumar Naik and B. G. Harish
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00185K, Concise Article
A series of simple quinoline–chalcone conjugates have been synthesized and evaluated for their nucleolytic activity. The compounds 3c and 3d exhibited promising DNA binding and DNA photocleavage studies.
 
Koen Jansen, Hans De Winter, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Anne-Marie Lambeir, Ingrid De Meester, Koen Augustyns and Pieter Van der Veken
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00167B, Concise Article
The first selective, non-peptide derived inhibitors of FAP are presented.
 
Craig J. Kutz, Steven L. Holshouser, Ethan A. Marrow and Patrick M. Woster
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00283K, Concise Article
From themed collection Epigenetics
Compounds 6 and 7 represent the first reversible LSD1 inhibitors with minimal cytotoxicity in vitro.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00255E, Review Article
A review of the synthesis and biological activity of α-bromo-phosphonate groups as phosphate bioisosteres.
 
Saulo F. Andrade, Claudia S. Teixeira, Jonas P. Ramos, Marcela S. Lopes, Rodrigo M. Pádua, Mônica C. Oliveira, Elaine M. Souza-Fagundes and Ricardo J. Alves
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00136B, Concise Article
Rigidification of the structure of 2,3,4-trisubstituted oxazolidines enhances the activity against LNCaP cells without affecting normal cell proliferation.
 
Hongjun Jin, Jinda Fan, Xiang Zhang, Junfeng Li, Hubert P. Flores, Joel S. Perlmutter, Stanley M. Parsons and Zhude Tu
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00240G, Concise Article
The σ1 receptor is an important target for CNS disorders.
 
Yakub E. Kadernani, Frank T. Zindo, Erika Kapp, Sarel F. Malan and Jacques Joubert
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00244J, Concise Article
A series of adamantane-derived compounds, structurally similar to NGP1-01, were synthesised and showed significant dual NMDA receptor and VGCC inhibitory activities.
 
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00282B, Concise Article
Design and synthesis of novel anti-HIV-1 NNRTIs based on a pyrazolo[4,3-d]isoxazole backbone scaffold.
 
R. A. Kotelnikova, A. V. Smolina, V. V. Grigoryev, I. I. Faingold, D. V. Mischenko, A. Yu. Rybkin, D. A. Poletayeva, G. I. Vankin, V. L. Zamoyskiy, I. I. Voronov, P. A. Troshin, A. I. Kotelnikov and S. O. Bachurin
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00194J, Concise Article
Water soluble fullerene derivatives I and II were shown to behave as promising neuroprotective agents that improve cognitive functioning in animals.
 
Ravindra M. Kumbhare, Tulshiram L. Dadmal, T. Anjana Devi, Dinesh Kumar, umesh kosurkar, Debabrata chowdhury chowdhury, killari appalanaidu, Y. Khageswara Rao, janki ramana and Manika Pal Bhadra
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00279B, Concise Article
A series of isoxazole derivatives of 6-fluoro-N-(6-methoxybenzo[d]thiazol-2-yl)benzo[d]thiazol-2-amine and N-(pyrimidin-2-yl)benzo[d]thiazol-2-amine were synthesized and evaluated for their cytotoxicity. These compounds exhibited anti-cancer activity against Colo-205, U 937, MCF-7 and A549 cancer cell...
 
Malinda Salim, Hiroyuki Minamikawa, A Sugimura and Rauzah Hashim
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00085D, Review Article
Vesicles formed by self-assembly of lipids and surfactants are increasingly recognised as carriers for drug delivery applications in disease targeting and many other biomedical-related areas, demonstrable by the growing number...
 
Sandhya Bansal, Manish Singh, Saqib Kidwai, Priyanshu Bhargava, Ashima Singh, Vedagopuram Sreekanth, Ramandeep Singh and Avinash Bajaj
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00303A, Concise Article
Tuberculosis faces major challenges for its cure due to a) long treatment period, b) emergence of drug resistance bacteria, and c) poor patient compliance. Disrupting the membrane integrity of mycobacteria...
 
Desi Pan, Qian-Jiao Yang, Xin Fu, Song Shan, Jing-Zhong Zhu, Kun Zhang, Zhi-Bing Li, Zhi-Qiang Ning and Xian-ping Lu
Med. Chem. Commun., 2014, Accepted Manuscript
DOI: 10.1039/C4MD00350K, Review Article
From themed collection Epigenetics
Tumorigenesis is maintained through a complex interplay of multiple cellular biological processes and is regulated to some extent by epigenetic control of gene expression. Targeting one signaling pathway or biological...
 

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