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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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Bernhard Wuensch, Yvonne Wenker, Michael Soeberdt, Constantin Gabriel Daniliuc, Sonja Ständer and Dirk Schepmann
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00441E, Research Article
In order to obtain novel polar kappa agonists the kappa-pharmacophoric ethylenediamine structural element was embedded in a rigid bicyclic scaffold. The pyridooxazine system was selected, since it contains polar O-...
 
Fatma A. Ragab, Helmi I. Heiba, Marwa G. El-Gazzar, Sahar M. Abou-Seri, Walaa A. El-Sabbagh and Reham M. El-Hazek
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00367B, Research Article
A novel series of thiadiazole derivatives were designed and synthesized for evaluation as selective COX-2 inhibitors in vitro and were investigated in vivo as anti-inflammatory and analgesic agents against carrageenan-induced rat paw oedema model in irradiated rats.
 
Christine A. Herdman, Tracy Strecker, Rajendra Tanpure, Zhi Chen, Alexander Winters, Jeni Gerberich, Li Liu, Ernest Hamel, Ralph Mason, David J. Chaplin, ML Trawick and Kevin G. Pinney
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00459H, Research Article
The natural products colchicine and combretastatin A-4 (CA4) have been inspirational for the design and synthesis of structurally related analogues and spin-off compounds as inhibitors of tubulin polymerization. The discovery...
 
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00456C, Research Article
Cancer prevention could be dealt with the administration of cancer chemopreventive agents (CCAs) that prevent, delay or reverse the carcinogenic process. CCAs able to induce detoxification-enzymes, especially monofunctional phase II...
 
Yonghui Wang, Ruomeng Qiu, Wenli Shi, Ting Cai, Siyu Pei, Ting Tang, Yafei Huang, Huan Wang, Liming Shao and Ju Qiu
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00427J, Research Article
A series of N-biaryl amides for Th17 cell phenotypic screening was designed and quickly prepared by microwave-assisted solid-phase organic synthesis. Structure-activity relationship of the three regions of the amides was...
 
Naresh Killi, Runali Arjun Dhakare, Amarnath Singam, Metta Lokanadham, Harshavardhan Chitikeshi and Rathna Venkata Naga Gundloori
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00380J, Research Article
Bioactive and mechanically strong nano-matrices of oil based polyesteramide blends as biomaterials.
 
Venkata Sashidhara Koneni, L. Ravithej Singh, Mohammad Shameem, Sarika Shakya, Anoop Kumar, Tulsankar Sachin Laxman, Shagun Krishna, M. I. Siddiqi, R. S. Bhatta and Dibyendu Banerjee
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00447D, Research Article
A series of new dihydropyrimidinone-semicarbazone hybrids were successfully synthesised by integrating regioselective multicomponent reaction with the pharmacophore hybridization approach. All the synthesised compounds were evaluated for their hLig1 inhibition potency...
 
David Cousin, Jihong Zhang, Marc Hummersone, Charles Matthews, Mark Frigerio, Tracey D Bradshaw and Malcolm F.G Stevens
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00384B, Research Article
Synthetic routes to 3-substituted imidazo[5,1-d]-1,2,3,5-tetrazines structurally related to temozolomide were explored. Interaction of 4-diazoimidazole-5-carboxamide with an isocyanate afforded high product yields when the isocyanate was available in acceptable purity. Alternatively,...
 
Moses Moustakim, Peter G. K. Clark, Duncan A. Hay, Darren J. Dixon and Paul E. Brennan
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00373G, Review Article
Significant progress has been made in discovering inhibitors and chemical probes of bromodomains, epigenetic readers of lysine acetylation.
 
Noorul Adawiyah, Muhammad Moniruzzaman, Siti Hawatulaila and Masahiro Goto
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00358C, Review Article
The pharmaceutical industries face a series of challenges in the delivery of many newly developed drug molecules because of their low solubility, bioavailability, stability and polymorphic conversion.
 
Faezeh Taghavi, Amir Sh. Saljooghi, Mostafa Gholizadeh and Mohammad Ramezani
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00293E, Research Article
Two broad strategies for the use of iron chelators in cancer treatment have been explored.
 
Maria E. Ourailidou, Niek G. J. Leus, Kim Krist, Alessia Lenoci, Antonello Mai and Frank J. Dekker
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00375C, Research Article
Azobenzene ortho-aminoanilides inhibit HDACs 1–3 and possess anti-inflammatory properties in murine macrophages.
 
G. Gabernet, A. T. Müller, J. A. Hiss and G. Schneider
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00376A, Review Article
Understanding the structure–activity relationships and mechanisms of action of membranolytic anticancer peptides could help them advance to therapeutic success.
 
Antonia Antoniou, Maria Chatzopoulou, Marina Bantzi, Constantinos Athanassopoulos, Athanassios Giannis and Emmanuel Pitsinos
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00354K, Research Article
The Hedgehog pathway has emerged as a favourable target to address drug resistance in cancer stem cells. Inhibitors of Gli1, the terminal effector of the pathway, are anticipated to evade...
 
Liang Guo, Wei Chen, Wenxi Fan, Qin Ma, Rongqin Sun, Guang Shao and Rihui Cao
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00360E, Research Article
A series of novel bivalent β-carbolines were synthesized and evaluated as potent angiogenesis inhibitors.
 
Ana Podolski-Renic, Zorica Milosevic, Jelena Dinic, Tijana Stankovic, Jasna Bankovic and Milica Pesic
Med. Chem. Commun., 2016, Accepted Manuscript
DOI: 10.1039/C6MD00391E, Review Article
Cancer-initiating cells referred as cancer stem cells (CSCs) retain the essential property of self-renewal and protection. The protective mechanisms enable tumour regrowth even after the application of chemotherapy that was...
 
Diego da Costa Cabrera, Sabrina B. Rosa, Franciele Saes de Oliveira, Marcelo A. G. Marinho, Caroline R. Montes D'Oca, Dennis Russowsky, Ana Paula Horn and Marcelo G. Montes D'Oca
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00425C, Research Article
Synthesis and antiproliferative activity of novel hybrid 3-substituted polyhydroquinoline-fatty acids.
 
Cornelius Hempel, Abdulkarim Najjar, Frank Totzke, Christoph Schächtele, Wolfgang Sippl, Christoph Ritter and Andreas Hilgeroth
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00329J, Research Article
Small-molecule inhibitors of cancer-relevant receptor tyrosine kinases EGFR and IGF-1R have been discovered.
 
D. C. Pryde, B. Marron, C. G. West, S. Reister, G. Amato, K. Yoger, K. Padilla, J. Turner, N. A. Swain, P. J. Cox, S. E. Skerratt, T. Ryckmans, D. C. Blakemore, J. Warmus and A. C. Gerlach
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00387G, Research Article
Potent and selective carboxamide TRPA1 antagonists were identified by high throughput screening, with efficacy demonstrated in a topical inflammation model.
 
Anna Alcaide, Laura Marconi, Ales Marek, Isabell Haym, Birgitte Nielsen, Stine Møllerud, Mikael Jensen, Paola Conti, Darryl S. Pickering and Lennart Bunch
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00339G, Research Article
Expedite synthesis of [3H]NF608 – a new subtype selective GluK1 radioligand.
 
Narisa Phummarin, Helena I. Boshoff, Patricia S. Tsang, James Dalton, Siouxsie Wiles, Clifton E. Barry 3rd and Brent R. Copp
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00236F, Research Article
New antimycobacterial 2-(quinoline-4-yloxy)acetamides were prepared, and using gene deletion and resistant mutants, we conclude that the compound class inhibits the mycobacterial cytochrome bc1 complex.
 
Elham Rezaee, Mahdi Hedayati, Laleh Hoghooghi Rad, Soraya Shahhosseini, Mehrdad Faizi and Sayyed Abbas Tabatabai
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00395H, Research Article
Amide non-urea derivatives with a dihydropyrimidinone ring as a novel secondary pharmacophore against the sEH enzyme were designed, synthesized and biologically evaluated.
 
Sonal Gupta, Deepti Pandey, Dhanaraju Mandalapu, Veenu Bala, Vikas Sharma, Mahendra Shukla, Santosh K. Yadav, Nidhi Singh, Swati Jaiswal, Jagdamba P. Maikhuri, Jawahar Lal, Mohammad I. Siddiqi, Gopal Gupta and Vishnu L. Sharma
Med. Chem. Commun., 2016, Advance Article
DOI: 10.1039/C6MD00426A, Research Article
Twenty-six piperazine derivatives were synthesized and findings revealed that compound 9a is promising candidate for management of prostatic disorders.
 
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.
 

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15 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
23 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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