MedChemComm



Indole Compounds with N-Ethyl Morpholine Moieties as CB2 Receptor Agonist for Anti-Inflammatory Management of Pain: Synthesis and Biological Evaluation ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00173E, Research Article Jiaojiao Li, jing ji, ruibo xu, zhengfu Li The CB2 receptor plays a crucial role in analgesia and anti-inflammation. To develop novel CB2 agonist with high efficacy and selectivity, a series of indole derivatives with N-ethyl morpholine moieties... The content of this RSS Feed (c) The Royal Society of Chemistry
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A focused structure-activity relationship study of psoralen-based immunoproteasome inhibitors ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00365G, Research Article Eva Shannon Schiffrer, Izidor Sosic, Andrej Šterman, Janez Mravljak, Irena Mlinarič Raščan, Stanislav Gobec, Martina Gobec The immunoproteasome is a multicatalytic protease that is predominantly expressed in cells of hematopoietic origin. Its elevated expression has been associated with autoimmune diseases, various types of cancer, and inflammatory... The content of this RSS Feed (c) The Royal Society of Chemistry
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Lipidomic analysis as a tool for identifying susceptibility to various diseases ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00364A, Review Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Valery Smirnov, Evgenii Egorenkov, Tatiana Myasnikova, Alexey Petukhov, Vladimir Gegechkori, Anna Sukhanova, Galina Ramenskaya The review is about the significance of use of lipid analysis for identifying susceptibility to deseases of various etiology. Exactly this article describes the use of lipidomic analysis in different... The content of this RSS Feed (c) The Royal Society of Chemistry
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Evaluation of anti-inflammatory activity and molecular docking study of new aza-bicyclic isoxazoline acylhydrazone derivatives ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00276F, Research Article Fernanda Virginia Barreto Mota, Marlene Saraiva de Araújo Neta, Eryvelton de Souza Franco, Isla Vanessa Gomes Alves Bastos, Larissa Cardoso Correia da Araújo, Sandra Cabral da Silva, Tatiane Bezerra de Oliveira, Eduarda Karynne Souza, Valderes Moraes de Almeida, Rafael Matos Ximenes, Maria Bernadete de Sousa Maia, Francisco Jaime Bezerra Mendonça Junior, Pascal Marchand, Antônio Rodolfo de Faria, Teresinha Gonçalves da Silva The aim of this study was to investigate the anti-inflammatory effects of two new isoxazoline-acylhydrazone derivatives. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Different solid forms for optimizing route of administration of the herpes drug Pritelivir ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00233B, Review Article Helga Ruebsamen-Schaeff, Helmut Buschmann In depth knowledge of the physicochemical properties of different salt forms and respective solvates/hydrates has a significant impact on the pharmaceutical dosage form. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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The cytotoxic potential of cationic triangulenes against tumour cells ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00305C, Research Article Euphemia Leung, Lisa I. Pilkington, Mohinder M. Naiya, David Barker, Ayesha Zafar, Chatchakorn Eurtivong, Jóhannes Reynisson Close-shelled carbocations DNA intercalators Pr-ADOTA and Pr-DAOTA are very cytotoxic against the cancer cell lines MDA-MB-231 (breast) and HCT116 (colon). To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Small antibacterial molecules highly active against drug-resistant Staphylococcus aureus ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00329K, Research Article Rajib Dey, Kathakali De, Riya Mukherjee, Sreyan Ghosh, Jayanta Haldar The rapid growth of antibiotic resistance in Staphylococcus aureus coupled with their biofilm forming ability has made the infections difficult to treat with conventional antibiotics. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Structural modification of azolylacryloyl derivatives yields a novel class of covalent modifiers of hemoglobin as potential antisickling agents ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00291J, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. A. M. Omar, T. David, P. P. Pagare, M. S. Ghatge, Q. Chen, A. Mehta, Y. Zhang, O. Abdulmalik, A. H. Naghi, M. E. El-Araby, M. K. Safo The intracellular polymerization and the concomitant sickling processes, central to the pathology of sickle cell disease, can be mitigated by increasing the oxygen affinity of sickle hemoglobin (HbS). To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00286C, Research Article Pasquale Linciano, Barbara De Filippis, Alessandra Ammazzalorso, Pasquale Amoia, Felisa Cilurzo, Marialuigia Fantacuzzi, Letizia Giampietro, Cristina Maccallini, Charlotte Petit, Rosa Amoroso PPAR agonists represent a new therapeutic opportunity for the prevention and treatment of neurodegenerative disorders, but their pharmacological success depends on favourable pharmacokinetic properties and capability to cross the BBB. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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A successful collaboration between academia, biotech and pharma led to discovery of erdafitinib, a selective FGFR inhibitor recently approved by the FDA ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD90044F, Editorial Christopher W. Murray, David R. Newell, Patrick Angibaud The winners of the Malcolm Campbell Memorial Prize for 2019 discuss the discovery of erdafitinib. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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BIM-46174 fragments as potential ligands of G proteins ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00269C, Research Article Jim Küppers, Tobias Benkel, Suvi Annala, Gregor Schnakenburg, Evi Kostenis, Michael Gütschow Fragments of BIM-46174 were synthesized and investigated as Gαq inhibitors. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Development of hydroxamate-based histone deacetylase inhibitors of bis-substituted aromatic amides with antitumor activities ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00306A, Research Article Di Ge, Lina Han, Feifei Yang, Na Zhao, Yang Yang, Hua Zhang, Yihua Chen Previously, we designed and synthesized a series of bis-substituted aromatic amide-based histone deacetylase (HDAC) inhibitors. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Non-viral transfection vectors: are hybrid materials the way forward? ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00275H, Review Article A. Gigante, M. Li, S. Junghänel, C. Hirschhäuser, S. Knauer, C. Schmuck Hybrid vectors are a remarkable strategy to address the current challenges in gene delivery. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00379G, Research Article Lars Stank, Annika Frank, Stefanie Hagenow, Holger Stark We linked 2-aminothiazoloazepane scaffolds with phenylpiperazine pharmacophores to generate bitopic dopamine receptor ligands. Highest D2R/D3R binding affinities up to pKi values of 7.74 were observed for compounds containing a 1-(2,3-dichlorophenyl)piperazinoyl... The content of this RSS Feed (c) The Royal Society of Chemistry
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Recent advances in the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00208A, Review Article Xiu-Xiu Wang, Si-Yu Sun, Qing-Qing Dong, Xiao-Xiang Wu, Wei Tang, Ya-Qun Xing This review summarizes the recent development of IDO1 inhibitors, focusing on structures, enzymatic inhibitory activity, selectivity and other biological activities. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Structural insights and binding analysis for determining the molecular bases for programmed cell death protein ligand-1 inhibition ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00326F, Research Article Rita C. Acúrcio, Carlota Leonardo-Sousa, Alfonso T. García-Sosa, Jorge A. Salvador, Helena F. Florindo, Rita C. Guedes Programmed cell death protein 1 (PD-1) and PD-ligand 1 (PD-L1) interaction plays an important role in cancer immunotherapy. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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