MedChemComm

Synthesis and antiviral activity of camphor-based 1,3-thiazolidin-4-one and thiazole derivatives as Orthopoxvirus-reproduction inhibitors ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00347E, Research Article Anastasiya S. Sokolova, Olga I. Yarovaya, Nikolay I. Bormotov, Larisa N. Shishkina, Nariman F. Salakhutdinov Camphor based heterocyclic systems containing 1,3-thiazolidin-4-one and thiazole rings showed promising antiviral activity towards Orthopoxviruses. 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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Correction: Design, synthesis, and evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D3 receptor agonists ()
Med. Chem. Commun., 2018, 9,1565-1565 DOI: 10.1039/C8MD90042F, Correction Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Yongkai Cao, Ningning Sun, Jiumei Zhang, Zhiguo Liu, Yi-zhe Tang, Zhengzhi Wu, Kyeong-Man Kim, Seung Hoon Cheon The content of this RSS Feed (c) The Royal Society of Chemistry
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How big should your screening collection be? ()
Med. Chem. Commun., 2018, 9,1397-1398 DOI: 10.1039/C8MD90041H, In the Pipeline Derek Lowe Derek Lowe's commentary on drug discovery and the pharma industry. The content of this RSS Feed (c) The Royal Society of Chemistry
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Antiplasmodial imidazopyridazines: structure–activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00382C, Research Article Peter Mubanga Cheuka, Nina Lawrence, Dale Taylor, Sergio Wittlin, Kelly Chibale Structural modifications around an antimalarial imidazopyridazine scaffold delivers analogues with improved solubility and hERG profiles. 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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Copper(II) complexes based on quinoline-derived Schiff-base ligands: synthesis, characterization, HSA/DNA binding ability, and anticancer activity ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00223A, Research Article Kun Hu, Chensi Liu, Jingui Li, Fupei Liang Three Cu(II) complexes (C1–C3) were designed and synthesized. C3, in particular, having a ligand derived from benzocaine, exhibited greater selectivity toward HeLa cells, arrested cell cycles, and promoted tumor cell apoptosis. 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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Novel hybrids derived from aspirin and chalcones potently suppress colorectal cancer in vitro and in vivo ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00284C, Research Article Shan Lu, Obinna N. Obianom, Yong Ai Novel hybrids derived from aspirin and chalcones were designed and synthesized. 7h had potent and selective anti-proliferative activity against CRC cells in vitro. 7h induced cell cycle arrest and apoptosis in CRC cells. 7h significantly inhibited the growth of implanted CRC cancer in mice. 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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Lipophilicity prediction of peptides and peptide derivatives by consensus machine learning ()
Med. Chem. Commun., 2018, 9,1538-1546 DOI: 10.1039/C8MD00370J, Research Article Jens-Alexander Fuchs, Francesca Grisoni, Michael Kossenjans, Jan A. Hiss, Gisbert Schneider Lipophilicity prediction is routinely applied to small molecules. For compounds outside the domain of classical medicinal chemistry these predictions lack accuracy, advocating the development of bespoke in silico approaches. The content of this RSS Feed (c) The Royal Society of Chemistry
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β-lactam/β-lactamase inhibitor combinations: an update ()
Med. Chem. Commun., 2018, 9,1439-1456 DOI: 10.1039/C8MD00342D, Review Article Kamaleddin H. M. E. Tehrani, Nathaniel I. Martin Antibiotic resistance caused by β-lactamase production continues to present a growing challenge to the efficacy of β-lactams and their role as the most important class of clinically used antibiotics. The content of this RSS Feed (c) The Royal Society of Chemistry
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Link between a high kon for drug binding and a fast clinical action: to be or not to be? ()
Med. Chem. Commun., 2018, 9,1426-1438 DOI: 10.1039/C8MD00296G, Review Article Georges Vauquelin Simulations show under which conditions increasing a drug’s kon can bring about faster clinical action. The content of this RSS Feed (c) The Royal Society of Chemistry
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Making figures: are you taking the best approach to maximize visibility? ()
Med. Chem. Commun., 2018, 9,1399-1403 DOI: 10.1039/C8MD90036A, Opinion Shogo Mori, Sylvie Garneau-Tsodikova We say “a figure is worth a thousand words”… Here is a concise guide and some tips towards optimizing your scientific graphics for maximum impact. The content of this RSS Feed (c) The Royal Society of Chemistry
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2-Aminobenzimidazoles as antibiofilm agents against Salmonella enterica serovar Typhimurium ()
Med. Chem. Commun., 2018, 9,1547-1552 DOI: 10.1039/C8MD00298C, Research Article William M. Huggins, T. Vu Nguyen, Nicholas A. Hahn, James T. Baker, Laura G. Kuo, Darpan Kaur, Roberta J. Melander, John S. Gunn, Christian Melander Serovars within the species Salmonella enterica are some of the most common food and water-borne pathogens worldwide. The content of this RSS Feed (c) The Royal Society of Chemistry
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Novel organophosphorus aminopyrimidines as unique structural DNA-targeting membrane active inhibitors towards drug-resistant methicillin-resistant Staphylococcus aureus ()
Med. Chem. Commun., 2018, 9,1529-1537 DOI: 10.1039/C8MD00301G, Research Article Di Li, Rammohan R. Yadav Bheemanaboina, Narsaiah Battini, Vijai Kumar Reddy Tangadanchu, Xian-Fu Fang, Cheng-He Zhou Molecular modeling of organophosphorus aminopyrimidine and the possible antibacterial mechanism. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis of novel perillyl–dihydropyrimidinone hybrids designed for antiproliferative activity ()
Med. Chem. Commun., 2018, 9,1553-1564 DOI: 10.1039/C8MD00270C, Research Article Vinicius Vendrusculo, Vanessa P. de Souza, Luiz Antônio M. Fontoura, Marcelo G. M. D'Oca, Thais P. Banzato, Paula A. Monteiro, Ronaldo A. Pilli, João Ernesto de Carvalho, Dennis Russowsky A series of fifteen novel dihydropyrimidinone hybrid compounds were synthesized in good yields via a multicomponent reaction combined with the Huisgen reaction. The content of this RSS Feed (c) The Royal Society of Chemistry
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Phenothiazine antioxidants increase mitochondrial biogenesis and frataxin levels in Friedreich's ataxia cells ()
Med. Chem. Commun., 2018, 9,1491-1501 DOI: 10.1039/C8MD00274F, Research Article Omar M. Khdour, Indrajit Bandyopadhyay, Nishant P. Visavadiya, Sandipan Roy Chowdhury, Sidney M. Hecht Two series of lipophilic phenothiazine derivatives were designed, synthesized and studied for their ability to enhance antioxidant capacity, increase frataxin levels, and induce mitochondrial biogenesis in vitro. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and biological evaluation of novel 5-chloro-N-(4-sulfamoylbenzyl) salicylamide derivatives as tubulin polymerization inhibitors ()
Med. Chem. Commun., 2018, 9,1511-1528 DOI: 10.1039/C8MD00214B, Research Article Alaaeldin M. F. Galal, Maha M. Soltan, Esam R. Ahmed, Atef G. Hanna A novel series of sulfonamide derivatives, coupled with a salicylamide scaffold, was designed and synthesized. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis, and evaluation of 4,5,6,7-tetrahydrobenzo[d]thiazole-based novel dual kinase inhibitors of CK2 and GSK3β ()
Med. Chem. Commun., 2018, 9,1472-1490 DOI: 10.1039/C8MD00321A, Research Article Triveni R. Pardhi, Manishkumar S. Patel, V. Sudarsanam, Kamala K. Vasu A rationally designed novel compound (1g) has shown significant dual kinase inhibitory activity against CK2 (1.9 μM) and GSK3β (0.67 μM). The content of this RSS Feed (c) The Royal Society of Chemistry
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Glycyrrhizic acid from licorice down-regulates inflammatory responses via blocking MAPK and PI3K/Akt-dependent NF-κB signalling pathways in TPA-induced skin inflammation ()
Med. Chem. Commun., 2018, 9,1502-1510 DOI: 10.1039/C8MD00288F, Research Article Wenfeng Liu, Shun Huang, Yonglian Li, Yanwen Li, Dongli Li, Panpan Wu, Quanshi Wang, Xi Zheng, Kun Zhang Glycyrrhizinic acid (GA), a principal component derived from licorice, is attracting considerable attention because of its broad range of bioactivities. The content of this RSS Feed (c) The Royal Society of Chemistry
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Transfection by cationic gemini lipids and surfactants ()
Med. Chem. Commun., 2018, 9,1404-1425 DOI: 10.1039/C8MD00249E, Review Article M. Damen, A. J. J. Groenen, S. F. M. van Dongen, R. J. M. Nolte, B. J. Scholte, M. C. Feiters Multivalent cationic lipids such as gemini surfactants are an alternative to viruses for intracellular delivery of nucleic acids. The content of this RSS Feed (c) The Royal Society of Chemistry
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Development of subnanomolar-affinity serotonin 5-HT4 receptor ligands based on quinoline structures ()
Med. Chem. Commun., 2018, 9,1466-1471 DOI: 10.1039/C8MD00233A, Research Article Federica Castriconi, Marco Paolino, Giorgio Grisci, Cinzia Maria Francini, Annalisa Reale, Germano Giuliani, Maurizio Anzini, Gianluca Giorgi, Laura Mennuni, Chiara Sabatini, Marco Lanza, Gianfranco Caselli, Andrea Cappelli A structure–affinity relationship study led to the discovery of 7h–j as novel 5-HT4 receptor ligands showing Ki values in the subnanomolar range. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis, and evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D3 receptor agonists ()
Med. Chem. Commun., 2018, 9,1457-1465 DOI: 10.1039/C8MD00237A, Research Article Yongkai Cao, Ningning Sun, Jiumei Zhang, Zhiguo Liu, Yi-zhe Tang, Zhengzhi Wu, Kyeong-Man Kim, Seung Hoon Cheon The dopamine D3 receptor (D3R) is a proven therapeutic target for the treatment of neurological and neuropsychiatric disorders. The content of this RSS Feed (c) The Royal Society of Chemistry
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Assessment of a bifendate derivative bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as a potential anti-metastatic agent ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00294K, Research Article Jingying Qiu, Wang Chen, Yanfei Jiang, Jing Chen, Yinpeng Zhang, Xiaoke Gu Multidrug resistance (MDR) and metastasis are major causes of mortality in patients with cancer. We recently reported a bifendate derivative bearing dibenzo[c,e]azepine scaffold (4i) as P-gp and BCRP-medicated MDR reversal... The content of this RSS Feed (c) The Royal Society of Chemistry
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Development of a [68Ga]-Ghrelin Analogue for PET Imaging of the Ghrelin Receptor (GHS-R1a) ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00210J, Research Article Carlie Charron, Mark McFarland, Savita Dhanvantari, Leonard G Luyt The ghrelin receptor is a member of the growth hormone secretagogue receptor (GHS-R) family and is present at low concentrations in tissues such as the brain, kidney, cardiovascular system, and... The content of this RSS Feed (c) The Royal Society of Chemistry
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Novel Tricyclic Glycal-based TRIB1 Inducers that Reprogram LDL Metabolism in Hepatic Cells ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00297E, Research Article Marek M Nagiec, Jeremy Duvall, Adam Skepner, Eleanor Howe, Jessica Bastien, Eamon Comer, Jean-Charles Marie, Stephen Johnston, Joseph Negri, Michelle Eichhorn, Julien Vantourout, Clary Clish, Kiran Musunuru, Michael Foley, Jose Perez, Michelle Palmer Increased expression of the Tribbles pseudkinase 1 gene (TRIB1) is associated with lower plasma levels of LDL cholesterol and triglycerides, higher levels of HDL cholesterol and decreased risk of coronary... The content of this RSS Feed (c) The Royal Society of Chemistry
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Discovery of boron-containing compounds as Aβ aggregation inhibitors and antioxidants for the treatment of Alzheimer's disease ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00315G, Research Article Chuan-Jun Lu, Jinhui Hu, Zechen Wang, Shishun Xie, Tingting Pan, Ling Huang, Xingshu Li A novel series of boron-containing compounds were designed, synthesized and evaluated as multi-target-directed ligands against Alzheimer's disease. Biological activity results demonstrated that these compounds possessed a significant ability to inhibit... The content of this RSS Feed (c) The Royal Society of Chemistry
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Protective effects of astragaloside IV against hypoxic pulmonary hypertension ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00341F, Research Article Xiaozheng Zhang, Jun Chen, Pan Xu, Xin Tian Treatment with As-IV significantly decreased mPAP, RVP and RV/(LV + S) and attenuated the development of HPH. 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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Synthesis of dihydronaphthalene analogues inspired by combretastatin A-4 and their biological evaluation as anticancer agents ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00322J, Research Article Casey J. Maguire, Zhi Chen, Vani P. Mocharla, Madhavi Sriram, Tracy E. Strecker, Ernest Hamel, Heling Zhou, Ramona Lopez, Yifan Wang, Ralph P. Mason, David J. Chaplin, Mary Lynn Trawick, Kevin G. Pinney Dihydronaphthalene analogues as potent inhibitors of tubulin polymerization, cytotoxic agents, and vascular disrupting agents (VDAs). 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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7-Deacetyl-10-alkylthiocolchicine derivatives – new compounds with potent anticancer and fungicidal activity ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00352A, Research Article Joanna Kurek, Patrycja Kwaśniewska-Sip, Krzysztof Myszkowski, Grzegorz Cofta, Marek Murias, Piotr Barczyński, Beata Jasiewicz, Rafał Kurczab Cytotoxic and fungicidal activity of 7-deacetyl-10-alkylthiocolchicine 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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Structural optimization and antibacterial evaluation of rhodomyrtosone B analogues against MRSA strains ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00257F, Research Article Liyun Zhao, Hongxin Liu, Luqiong Huo, Miaomiao Wang, Bao Yang, Weimin Zhang, Zhifang Xu, Haibo Tan, Sheng-Xiang Qiu Methicillin-resistant Staphylococcus aureus (MRSA) infections are well-known as a significant global health challenge. 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 transition to magic bullets – transition state analogue drug design ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00372F, Review Article Gary B. Evans, Vern L. Schramm, Peter C. Tyler Transition state analogue design offers a new discovery paradigm for the design of drugs and chemical probes. 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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Benzophenone: a ubiquitous scaffold in medicinal chemistry ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00300A, Review Article Khemchand Surana, Bharatkumar Chaudhary, Monika Diwaker, Satyasheel Sharma Diaryl ketones are an important scaffold in drug discovery due to their prevalence in naturally occurring bioactive compounds. This review discusses molecules containing the benzophenone moiety that have potent biological activity. 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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Novel 1,3,4-thiadiazole–chalcone hybrids containing catechol moiety: synthesis, antioxidant activity, cytotoxicity and DNA interaction studies ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00316E, Research Article Katarina Jakovljević, Milan D. Joksović, Ivana Z. Matić, Nina Petrović, Tatjana Stanojković, Dušan Sladić, Miroslava Vujčić, Barbara Janović, Ljubinka Joksović, Snežana Trifunović, Violeta Marković 1,3,4-Thiadiazole compounds containing catechol moiety and chalcone motif are synthesized and examined for antioxidant activity, cytotoxicity and DNA-binding activity. 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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Design, synthesis, and anticancer activity evaluation of irreversible allosteric inhibitors of the ubiquitin-conjugating enzyme Ube2g2 ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00320C, Research Article Chao Wang, Genbin Shi, Xinhua Ji The anticancer activity of CW3, an irreversible allosteric inhibitor of the ubiquitin-conjugating enzyme Ube2g2, and its interaction with the protein. 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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On the inhibition of capsaicin response in dorsal root ganglion neurons by nobilamide B and analogues: a structure–activity relationship study ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00304A, Research Article Oliver John V. Belleza, Jortan O. Tun, Gisela P. Concepcion, Aaron Joseph L. Villaraza Nobilamide B, a TRPV1 antagonist, and a series of Ala-substituted analogues were synthesized and their neuroactivity was assessed in a primary culture of dorsal root ganglion (DRG) neurons. 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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Targeting Brd4 for cancer therapy: inhibitors and degraders ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00198G, Review Article Yingchao Duan, Yuanyuan Guan, Wenping Qin, Xiaoyu Zhai, Bin Yu, Hongmin Liu This review summarizes recent developments of Brd4 inhibitors and degraders for cancer treatment. 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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Medicinal chemistry of acridine and its analogues ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00384J, Review Article Parteek Prasher, Mousmee Sharma ‘Acridine’ along with its functional analogue ‘Acridone’ is the most privileged pharmacophore in medicinal chemistry with diverse applications ranging from DNA intercalators, endonuclease mimics, ratiometric selective ion sensors, and P-glycoprotein inhibitors in countering the multi-drug resistance, enzyme inhibitors, and reversals of neurodegenerative disorders. 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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Platinum(II) complexes with rutaecarpine and tryptanthrin derivatives induce apoptosis by inhibiting telomerase activity and disrupting mitochondrial function ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00247A, Research Article Qi-Pin Qin, Bi-Qun Zou, Fei-Long Hu, Guo-Bao Huang, Shu-Long Wang, Yun-Qiong Gu, Ming-Xiong Tan BrTry-Pt is a telomerase inhibitor targeting the c-myc promoter, and triggered T-24 cell apoptosis, which also caused mitochondrial dysfunction and S phase arrest. 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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Porphyrins as ligands for 64copper: background and trends ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00263K, Review Article Edgar Aguilar-Ortíz, Amir R. Jalilian, Miguel A. Ávila-Rodríguez Porphyrins and 64Cu have emerged as a novel synergic option for applications in PET molecular imaging. 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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