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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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Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00227C, Concise Article
Inspired by curcumin-a natural traditional Chinese medicine, sulindac-based compound was designed and synthesized. The anti-inflammatory activity of sulindac-based compound was evaluated in TPA-induced mouse ear edema model. In comparison with...
 
Nermin S. Abdou, Rabah A. T. Serya, Ahmed Esmat, Mai F. Tolba, Nasser S. M. Ismail and Khaled A. M. Abouzid
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00127G, Concise Article
A novel series of pyrazolo[3,4-d]pyrimidine derivatives were designed, synthesized and evaluated for their antiproliferative activity.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD90028J, In the Pipeline
Late stage functionalisation can seem supernaturally powerful, says Derek Lowe – if you've got the nerve to try it.
 
Barbara De Filippis, Mariangela Agamennone, Alessandra Ammazzalorso, Isabella Bruno, Alessandra D'Angelo, Mauro Di Matteo, Marialuigia Fantacuzzi, Letizia Giampietro, Antonella Giancristofaro, Cristina Maccallini and Rosa Amoroso
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00151J, Concise Article
A new series of gemfibrozil analogues conjugated with trans-stilbene were synthesized and evaluated with the aim of developing new PPARα agonists.
 
John Mann, Peter Taylor, Colin Dorgan, Peter Johnson, Francis X. Wilson, Richard Vickers, Aaron Dale and Stephen Neidle
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00238A, Review Article
Academic drug discovery is playing an increasingly important role in the identification of new therapies for a wide range of diseases. There is no one model that guarantees success. We...
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00228A, Concise Article
Curves showing two different trials of killing a MRSA strain with [Cp*IrCl(cis-1,2-diaminocyclohexane)]Cl.
 
Justyna Sikorska, Luca Codutti, Lars Skjærven, Bettina Elshorst, Rebeca Saez-Ameneiro, Andrea Angelini, Peter Monecke and Teresa Carlomagno
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00116A, Concise Article
INPHARMA, an NMR-based method that determines ligand binding poses, allows finding novel scaffolds as inhibitors of a target protein.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00171D, Concise Article
Compounds 12g, 12i and 12l modulate pro-inflammatory cytokine production by inhibiting monocyte differentiation.
 
Qi Guan, Dongjie Feng, Zhaoshi Bai, Yuanhang Cui, Daiying Zuo, Min'an Zhai, Xuewei Jiang, Wenbo Zhou, Kai Bao, Yingliang Wu and Weige Zhang
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00150A, Concise Article
A microwave-assisted synthesis method of building a 1,2,4-oxadiazole skeleton was developed.
 
S. D. Lucas, M. P. Carrasco, L. M. Gonçalves, R. Moreira and R. C. Guedes
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00164A, Concise Article
From themed collection 1st EFMC Young Medicinal Chemist Symposium
Aurones were discovered as sub-micromolar HNE inhibitors. The activity is rationalized by a C-shape conformation that allows tight binding to HNE S1 and S2 pockets.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00169B, Concise Article
Discovery of new benzimidazoles as potent dual AT1 and ETA receptor antagonists with the novel N-(1H-tetrazol-5-yl)-amide fragment.
 
Narsimha Penthala, Leena Maddukuri, Shraddha Thakkar, Nikhil Reddy Madadi, Gauri Lamture, Robert Eoff and Peter Crooks
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00219B, Concise Article
trans-Cyanocombretastatin A-4 (trans-CA-4) analogues have been structurally modified to afford their more stable CA-4-(2H)-1,2,3-triazole analogues. Fifteen novel, stable 4-heteroaryl-5-aryl-(2H)-1,2,3-triazole CA-4 analogues (8a-i, 9 and 11a-e) were evaluated for anti-cancer activity...
 
Alla Zablotskaya, Izolda Segal, Athina Geronikaki, Galina Kazachonokh, Yuris Popelis, Irina Shestakova, Vizma Nikolajeva and Daina Eze
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00140D, Concise Article
The observed coupling of high anticancer and antimicrobial activity for novel lipid-like compounds 9, 10 and 13 based on the 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole scaffold can be important as a basis for further drug development.
 
Zhe Wang, Peng Zou, Chenglong Li, Wenfei He, Bing Xiao, Qilu Fang, Wenbo Chen, Suqing Zheng, Yunjie Zhao, Yuepiao Cai and Guang Liang
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD90030A, Correction
 
Ling Zhang, Kannekanti Vijaya Kumar, Syed Rasheed, Shao-Lin Zhang, Rong-Xia Geng and Cheng-He Zhou
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD90029H, Correction
 
Dipti Kakkar, Shweta Dumoga, Rohit Kumar, Krishna Chuttani and Anil Kumar Mishra
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00104H, Concise Article
The design of pegylated SLNs for efficient entrapment and delivery of methotrexate at tumour sites in order to overcome its bioavailability and blood retention issues.
 
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00108K, Concise Article
To clarify the biophysical and/or physicochemical mechanism of anaesthesia, we investigated the influence of dibucaine hydrochloride (DC·HCl), a local anaesthetic, on raft-like domains in ternary liposomes composed of dioleoylphosphatidylcholine (DOPC), dipalmitoylphosphatidylcholine (DPPC) and cholesterol (Chol).
 
Lili Dong, Suqing Zheng, Yali Zhang, Xin Jiang, Jianzhang Wu, Xiaoqing Zhang, Xiaoou Shan, Dandan Liang, Shilong Ying, Jianpeng Feng and Guang Liang
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00113G, Concise Article
Acute Lung Injury (ALI), one of severe diseases with high mortality, cannot be tackled by any effective therapies so far. Hence it has received extensive concern nowadays. Considerable experimental and...
 
Qianzhi Ding, Chanjuan Li, Ling Wang, Yali Li, Huihao Zhou, Qiong Gu and Jun Xu
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00149H, Concise Article
For the first time, NB and RP were successfully employed to predict FXR agonists. Two new FXR agonists were identified with the models, and confirmed with cell-based experiments.
 
Anna Bujak, Filip Stefaniak, Daria Zdzalik, Paulina Grygielewicz, Barbara Dymek, Marcin Zagozda, Pawel Gunerka, Monika Lamparska-Przybysz, Krzysztof Dubiel, Maciej Wieczorek and Karolina Dzwonek
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00090D, Concise Article
TRAF-2 and NCK-interacting kinase (TNIK) is a serine-threonine kinase with a proposed role in Wnt/β-catenin and JNK pathways. It has been implicated in Wnt-mediated colorectal carcinogenesis, and TNIK coding gene...
 
Dimpy Kalia, Anil Kumar K.S., Gajanand Meena, Kashmir Prasad Sethi, Rohit Sharma, Priyanka Trivedi, Shaheb Raj Khan, Ajay Singh Verma, Shyam Singh, Sandeep Sharma, Kuldeep K Roy, Ruchir Kant, Manju Yasodha Krishnan, Bhupendra N. Singh, Sudhir Sinha, Vinita Chaturvedi, Anil K Saxena and Dinesh K Dikshit
Med. Chem. Commun., 2015, Accepted Manuscript
DOI: 10.1039/C5MD00131E, Concise Article
One of the most significant breakthroughs in the battle against tuberculosis is the recent approval of the quinoline compound, TMC207, for the treatment of drug-resistant tuberculosis. To gain insight into...
 
Yuya Hirakawa, Rie Wakabayashi, Ayaka Naritomi, Masato Sakuragi, Noriho Kamiya and Masahiro Goto
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00168D, Concise Article
Solid-in-oil nanodispersions allowed cancer antigens to penetrate into skin to induce antigen-specific cancer immunity.
 
Duncan A. Hay, Catherine M. Rogers, Oleg Fedorov, Cynthia Tallant, Sarah Martin, Octovia P. Monteiro, Susanne Müller, Stefan Knapp, Christopher J. Schofield and Paul E. Brennan
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00152H, Concise Article
From themed collection 1st EFMC Young Medicinal Chemist Symposium
We describe potent and selective inhibitors of the BRD7 and BRD9 bromodomains intended for use as chemical probes to elucidate the biological roles of BRD7 and BRD9 in cells.
 
Xiaoqing Miao, Ye Li, Ian Wyman, Simon M. Y. Lee, Donal H. Macartney, Ying Zheng and Ruibing Wang
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00189G, Concise Article
Cucurbit[7]uril significantly enhanced in vitro and in vivo uptake of coumarin-6, on an epithelial cell model and a zebrafish model.
 
Yongcong Lv, Mengyuan Li, Sufen Cao, Linjiang Tong, Ting Peng, Lixin Wei, Hua Xie, Jian Ding and Wenhu Duan
Med. Chem. Commun., 2015, Advance Article
DOI: 10.1039/C5MD00191A, Concise Article
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive strategy for the treatment of cancer.
 

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