MedChemComm

Transfection by cationic gemini lipids and surfactants ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00249E, Review Article Mark Damen, A. J. J. Groenen, Stijn F.M. van Dongen, Roeland J.M. Nolte, B. J. Scholte, Martinus C Feiters Diseases that are linked to defective genes or mutations can in principle be cured by gene therapy, in which damaged or absent genes are either repaired or replaced by new... The content of this RSS Feed (c) The Royal Society of Chemistry
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Nucleoside triphosphate cosubstrates control the substrate profile and efficiency of aminoglycoside 3′-O-phosphotransferase type IIa ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00234G, Research Article Selina Y. L. Holbrook, Matthew S. Gentry, Oleg V. Tsodikov, Sylvie Garneau-Tsodikova The APH(3′)-IIa resistance enzyme is both substrate and cosubstrate promiscuous and the nucleoside triphosphate cofactor steers aminoglycoside substrate profile and efficiency. 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 molecule cores demonstrate non-competitive inhibition of lactate dehydrogenase ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00309B, Research Article Brooke Andrews, Richard Brian Dyer Lactate dehydrogenase (LDH) has recently garnered attention as an attractive target for cancer therapies, owing to the enzyme’s critical role in cellular metabolism. Current inhibition strategies, employing substrate or cofactor... The content of this RSS Feed (c) The Royal Society of Chemistry
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Chemical Modulation of Transcription Factors ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00273H, Review Article Bianca Wiedemann, Jörn Weisner, Daniel Rauh Transcription factors (TFs) constitute a diverse class of sequence-specific DNA-binding proteins, which are key to the modulation of gene expression. TFs have been associated with human diseases, including cancer, Alzheimer’s... The content of this RSS Feed (c) The Royal Society of Chemistry
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MicroRNA-451 Blockade Promotes Osteoblastic Differentiation and Skeletal Anabolic Effects by Promoting YWHAZ-Mediated RUNX2 Protein Stabilization ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00187A, Research Article Jieen Pan, Chenglong Huang, Gang Chen, Zhenhai Cai , Zhongwei Zhang Background: Senile osteoporosis researchers are now seeking to promote osteoblastogenesis and resultant bone formation to directly counteract age-related bone loss. Targeting microRNA (miRNA) activity in adult osteoblasts may be a... The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis, and biological evaluation of novel asymmetric naphthalene diimide derivative as anticancer agent depending on ROS generation ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00265G, Research Article Xiaojuan Xu, Senzhen Wang, Yuan Chang, Chaochao Ge, Xinna Li, Yongli Feng, Songqiang Xie, Chaojie Wang, Fujun Dai, Wen Luo Naphthalenetetracarboxylic diimide (NDI) is widely used as a photoelectric material in the field of medicine. A series of asymmetric naphthalene diimide derivatives were synthesized and evaluated for their anticancer properties... The content of this RSS Feed (c) The Royal Society of Chemistry
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Molecular insights into the interaction of Hsp90 with allosteric inhibitors targeting the C-terminal domain ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00151K, Research Article Vasantha Kumar MV, Radwan Ebna Noor, Rachel E. Davis, Zheng Zhang, Edvinas Sipavicius, Dimitra Keramisanou, Brian S. J. Blagg, Ioannis Gelis Novologues KU-32 and KU-596 bind at the C-terminal domain of Hsp90 and exploit a long-range allosteric network to modulate the chaperone cycle. 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 and pre-clinical evaluation of a potential radiotracer for PET imaging of the dopamine D3 receptor ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00094H, Research Article Megan N. Stewart, Xia Shao, Timothy J. Desmond, Taylor J. Forrest, Janna Arteaga, Jenelle Stauff, Peter J. H. Scott There is considerable interest in using PET imaging to quantify dopamine D3 receptors. We report a new D3-selective radioligand, and describe preclincial evaluation in rodent using ex vivo autoradiography and in vivo PET 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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Discovery of new FXR agonists based on 6-ECDCA binding properties by virtual screening and molecular docking ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00272J, Research Article Antonella Giancristofaro, Arménio J.M. Moura Barbosa, Alessandra Ammazzalorso, Pasquale Amoia, Barbara De Filippis, Marialuigia Fantacuzzi, Letizia Giampietro, Cristina Maccallini Maccallini, Rosa Amoroso FXR is a member of the nuclear receptor superfamily, regulates the expression of various genes involved in bile acid, lipid and glucose metabolism. Targeting FXR with small molecules has been... The content of this RSS Feed (c) The Royal Society of Chemistry
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Identification of an auxiliary druggable pocket in DNA gyrase ATPase domain using fragment probes ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00148K, Research Article Xiaojie Huang, Junsong Guo, Qi Liu, Qiong Gu, Jun Xu, Huihao Zhou Discovery of new drug binding sites on well-established targets is of great interest as it facilitates designing new mechanistic inhibitors to overcome the acquired drug resistance. The small chemical fragments... 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 structure ()
Med. Chem. Commun., 2018, Accepted Manuscript 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 Two small series of quinoline derivatives were designed starting from the previously published quinoline derivatives 7a,b in order to obtain information about their interaction with 5-HT4R binding site. Initially, the... The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00197A, Research Article Daoguang Zhang, Dongdong Tong, Dezhi Yang, Jing Sun, Fenghe Zhang, Guisen Zhao A series of AKT inhibitors possessing a piperidin-4-yl side chain was designed and synthesized. Some of them showed high AKT1 inhibitory activity and potent anti-proliferative effect on PC-3 prostate cancer... The content of this RSS Feed (c) The Royal Society of Chemistry
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Ammonium [11C]thiocyanate: revised preparation and reactivity studies of a versatile nucleophile for carbon-11 radiolabelling ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00425G, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Tom Haywood, Sara Cesarec, Steven Kealey, Christophe Plisson, Philip W. Miller Ammonium [11C]thiocyanate, produced from [11C]CS2, was used to efficiently radiolabel a range of C-11 thiocyanate and thiazolone molecules. 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 evaluation of bitopic arylpiperazine-phthalimides as selective dopamine D3 receptor agonists ()
Med. Chem. Commun., 2018, Advance Article 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. 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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Synthetic glycopeptide as a designated standard in the focused glycoproteomics to discover serum cancer biomarkers ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00162F, Research Article K. V. Yogesh, Toshiya Kamiyama, Chikara Ohyama, Tohoru Yoneyama, Kazuhiro Nouso, Satoshi Kimura, Hiroshi Hinou, Shin-Ichiro Nishimura Previous studies on the large-scale glycomics of more than 3500 human serum samples revealed that the serum glycoproteins of cancer patients often have more dominant and specific glycoforms, namely, branched... The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00212F, Research Article Niu-niu Zhang, Zhi-yong Liu, Jie Liang, Yun-xiang Tang, Lu Qian, Ya-min Gao, Tian-yu Zhang, Ming Yan m-Amidophenol derivatives were found to potently inhibit the growth of M. tuberculosis strains H37Ra and H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains. 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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Sodium–glucose cotransporter 2 (SGLT-2) inhibitors: a new antidiabetic drug class ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00183A, Review Article Paula Nogueira da Silva, Raissa Alves da Conceição, Rodolfo do Couto Maia, Maria Leticia de Castro Barbosa Novel SGLT-2 selective inhibitors, an innovative therapeutic approach for glycemia control in diabetic patients. 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 and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00156A, Research Article Sang Won Park, Suhrid Banskota, Pallavi Gurung, You Jin Jin, Han-eol Kang, Chhabi Lal Chaudhary, Sang Yeul Lee, Byeong-Seon Jeong, Jung-Ae Kim, Tae-gyu Nam Novel series of anti-inflammatory bowel disease (IBD) agent was identified through TNF-α-induced cell adhesion. 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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Generation of a long-acting fusion inhibitor against HIV-1 ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00124C, Research Article Ye Guo, Pan-Pan Zhou, Sen-Yan Zhang, Xiao-Wen Fan, Yu-Wei Dou, Xuan-Ling Shi AIDS has evolved from a fatal infectious disease to a manageable chronic disease under the treatment of anti-AIDS medications. 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 and antiplasmodial activity of purine-based C-nucleoside analogues ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00098K, Research Article Kartikey Singh, Prince Joshi, Rohit Mahar, Pragati Baranwal, Sanjeev K. Shukla, Renu Tripathi, Rama Pati Tripathi A series of purine-based homologous C-nucleoside mimics have been synthesized and evaluated for their antiplasmodial 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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Discovery of a tetrazolyl β-carboline with in vitro and in vivo osteoprotective activity under estrogen-deficient conditions ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00109J, Research Article Anirudha Karvande, Shahnawaz Khan, Irfan Khan, Deepti Singh, Vikram Khedgikar, Priyanka Kushwaha, Naseer Ahmad, Priyanka Kothari, Anupam Dhasmana, Ruchir Kant, Ritu Trivedi, Prem M. S. Chauhan β-Carboline derivative 8g prevents estrogen deficiency induced TNFα directed IKK activation and bone loss. 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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DIBI, a 3-hydroxypyridin-4-one chelator iron-binding polymer with enhanced antimicrobial activity ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00192H, Research Article M. Trisha C. Ang, Roger Gumbau-Brisa, David S. Allan, Robert McDonald, Michael J. Ferguson, Bruce E. Holbein, Matthias Bierenstiel Depriving microorganisms of bioavailable iron is a promising strategy for new anti-infective agents. 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 biological evaluation of benzimidazole–rhodanine conjugates as potent topoisomerase II inhibitors ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00278A, Research Article Penghui Li, Wenjin Zhang, Hong Jiang, Yongliang Li, Changzhi Dong, Huixiong Chen, Kun Zhang, Zhiyun Du In this study, a series of benzimidazole–rhodanine conjugates were designed, synthesized and investigated for their topoisomerase II (Topo II) inhibitory and cytotoxic 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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Design and synthesis of conformationally constraint Dyrk1A inhibitors by creating an intramolecular H-bond involving a benzothiazole core ()
Med. Chem. Commun., 2018, 9,1045-1053 DOI: 10.1039/C8MD00142A, Research Article Mohamed Salah, Mohammad Abdel-Halim, Matthias Engel We present the development of conformationally pre-organised Dyrk1A inhibitors based on the hydroxybenzothiazole urea scaffold. The content of this RSS Feed (c) The Royal Society of Chemistry
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Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: synthesis, in vitro biological evaluation and molecular docking ()
Med. Chem. Commun., 2018, 9,1054-1058 DOI: 10.1039/C8MD00057C, Research Article Wuji Sun, Shubiao Fang, Hong Yan Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive target for cancer therapy. The content of this RSS Feed (c) The Royal Society of Chemistry
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Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists ()
Med. Chem. Commun., 2018, 9,1069-1075 DOI: 10.1039/C8MD00204E, Research Article Moustafa T. Gabr, Mohammed S. Abdel-Raziq A biphenyl amide–tryptamine hybrid as a selective 5-HT2B antagonist. The content of this RSS Feed (c) The Royal Society of Chemistry
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Assessment of the trifluoromethyl ketone functionality as an alternative zinc-binding group for selective HDAC6 inhibition ()
Med. Chem. Commun., 2018, 9,1011-1016 DOI: 10.1039/C8MD00107C, Research Article Yves Depetter, Silke Geurs, Flore Vanden Bussche, Rob De Vreese, Jorick Franceus, Tom Desmet, Olivier De Wever, Matthias D'hooghe The replacement of the hydroxamic acid zinc-binding group in benzohydroxamic acid HDAC6 inhibitors by a trifluoromethyl ketone function leads to severe reduction in enzymatic and cellular activity. The content of this RSS Feed (c) The Royal Society of Chemistry
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Efficient copper-catalyzed amination of DNA-conjugated aryl iodides under mild aqueous conditions ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00185E, Research Article Yves Ruff, Frédéric Berst A practical and efficient protocol for the amination of DNA-conjugated aryl iodide using a novel ligand was developed. 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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Antitumor effects of melanin from Lachnum YM226 and its derivative in H22 tumor-bearing mice ()
Med. Chem. Commun., 2018, 9,1059-1068 DOI: 10.1039/C8MD00035B, Research Article Fang Shi, Jinglei Li, Ziyang Ye, Liuqing Yang, Tingting Chen, Xue Chen, Ming Ye LM and ALM showed notable antitumor effect in H22 tumor-bearing mice and ALM was more effective. The content of this RSS Feed (c) The Royal Society of Chemistry
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Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties ()
Med. Chem. Commun., 2018, 9,951-962 DOI: 10.1039/C8MD00070K, Research Article Michał Załuski, Katarzyna Stanuch, Tadeusz Karcz, Sonja Hinz, Gniewomir Latacz, Ewa Szymańska, Jakub Schabikowski, Agata Doroż-Płonka, Jadwiga Handzlik, Anna Drabczyńska, Christa E. Müller, Katarzyna Kieć-Kononowicz Novel tricyclic xanthine derivatives containing a basic substituent were investigated as adenosine receptor antagonists and selected drug-related properties were evaluated. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and cellular penetration properties of new phosphonium based cationic amphiphilic peptides ()
Med. Chem. Commun., 2018, 9,982-987 DOI: 10.1039/C8MD00113H, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Ezequiel Silva Nigenda, Tobias M. Postma, Mohammed Hezwani, Alin Pirvan, Susan Gannon, Carol-Anne Smith, Mathis Riehle, Rob M. J. Liskamp A new category of phosphonium based cationic amphiphilic peptides has been developed and evaluated as potential antimicrobial peptides and cell penetrating peptides. The content of this RSS Feed (c) The Royal Society of Chemistry
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The role of aryl-topology in balancing between selective and dual 5-HT7R/5-HT1A actions of 3,5-substituted hydantoins ()
Med. Chem. Commun., 2018, 9,1033-1044 DOI: 10.1039/C8MD00168E, Research Article Katarzyna Kucwaj-Brysz, Rafał Kurczab, Ewa Żesławska, Annamaria Lubelska, Małgorzata Anna Marć, Gniewomir Latacz, Grzegorz Satała, Wojciech Nitek, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik Influence of aromatic rings topology on 5-HT7/5-HT1A activity, for novel hydantoin derivatives, was examined. The content of this RSS Feed (c) The Royal Society of Chemistry
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Novel 99mTc labelled complexes with 2-nitroimidazole isocyanide: design, synthesis and evaluation as potential tumor hypoxia imaging agents ()
Med. Chem. Commun., 2018, 9,988-994 DOI: 10.1039/C8MD00146D, Research Article Qing Ruan, Xuran Zhang, Xiao Lin, Xiaojiang Duan, Junbo Zhang 99mTc-2c can be prepared by a direct labelling method without the need for heating and would be a promising probe for hypoxia imaging. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design and synthesis of novel 1,3,5-triphenyl pyrazolines as potential anti-inflammatory agents through allosteric inhibition of protein kinase Czeta (PKCζ) ()
Med. Chem. Commun., 2018, 9,1076-1082 DOI: 10.1039/C8MD00100F, Research Article Mohammad Abdel-Halim, Ashraf H. Abadi, Matthias Engel A new focused library of PKCζ inhibitors was synthesized, leading to the identification of compound 2h. Owing to its improved cellular potency in human and murine cell lines, this new lead compound opens up the possibility to evaluate allosteric PKCζ inhibitors in rat or mouse models. The content of this RSS Feed (c) The Royal Society of Chemistry
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Evaluation of A-ring fused pyridine D-modified androstane derivatives for antiproliferative and aldo–keto reductase 1C3 inhibitory activity ()
Med. Chem. Commun., 2018, 9,969-981 DOI: 10.1039/C8MD00077H, Research Article Marina P. Savić, Jovana J. Ajduković, Jovana J. Plavša, Sofija S. Bekić, Andjelka S. Ćelić, Olivera R. Klisurić, Dimitar S. Jakimov, Edward T. Petri, Evgenija A. Djurendić New A-ring pyridine fused androstanes in D-homo lactone, 17α-picolyl or 17(E)-picolinylidene series were synthesized and validated. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and preliminary anti-inflammatory and anti-bacterial evaluation of some diflunisal aza-analogs ()
Med. Chem. Commun., 2018, 9,1017-1032 DOI: 10.1039/C8MD00139A, Research Article Davide Carta, Paola Brun, Matteo Dal Pra, Giulia Bernabè, Ignazio Castagliuolo, Maria Grazia Ferlin The new diflunisal aza-analogs multi-target approach is remarkable in the treatment of infections induced by multi-drug resistant bacteria. Diflunisal aza-analogs preserved the anti-inflammatory activity and significantly potentiated the antimicrobial activity of antibiotics. The content of this RSS Feed (c) The Royal Society of Chemistry
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Live-cell fluorescence imaging: assessment of thioflavin T uptake in human epidermal carcinoma cells ()
Med. Chem. Commun., 2018, 9,946-950 DOI: 10.1039/C8MD00101D, Research Article G. S. M. Sundaram, Kristen Binz, Vedica Sharma, Melany Yeung, Vijay Sharma Live-cell imaging shows that thioflavin-T is recognized by Pgp as its transport substrate due to its either exclusion- or LY335979-induced accumulation in MDR cells. The content of this RSS Feed (c) The Royal Society of Chemistry
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An overview of recent molecular dynamics applications as medicinal chemistry tools for the undruggable site challenge ()
Med. Chem. Commun., 2018, 9,920-936 DOI: 10.1039/C8MD00166A, Review Article Ugo Perricone, Maria Rita Gulotta, Jessica Lombino, Barbara Parrino, Stella Cascioferro, Patrizia Diana, Girolamo Cirrincione, Alessandro Padova Molecular dynamics has been demonstrated to be crucial for unveiling otherwise hidden binding sites especially for the undruggable target challenge. The content of this RSS Feed (c) The Royal Society of Chemistry
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Effect of N-1 arylation of monastrol on kinesin Eg5 inhibition in glioma cell lines ()
Med. Chem. Commun., 2018, 9,995-1010 DOI: 10.1039/C8MD00095F, Research Article Itamar Luís Gonçalves, Liliana Rockenbach, Gustavo Machado das Neves, Gabriela Göethel, Fabiana Nascimento, Luciano Porto Kagami, Fabrício Figueiró, Gabriel Oliveira de Azambuja, Amanda de Fraga Dias, Andressa Amaro, Lauro Mera de Souza, Ivan da Rocha Pitta, Daiana Silva Avila, Daniel Fábio Kawano, Solange Cristina Garcia, Ana Maria Oliveira Battastini, Vera Lucia Eifler-Lima An original and focused library of dihydropyrimidin-2-thiones N-1 aryl substituted derived from monastrol was designed and synthesized in order to discover a more effective Eg5 ligand. The content of this RSS Feed (c) The Royal Society of Chemistry
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Antifungal amphiphilic kanamycins: new life for an old drug ()
Med. Chem. Commun., 2018, 9,909-919 DOI: 10.1039/C8MD00155C, Review Article Yagya Prasad Subedi, Madher N. AlFindee, Jon Y. Takemoto, Cheng-Wei Tom Chang The background is a bright-field microscopic image of Candida albicans that is inhibited by amphiphilic kanamycins FG08 and K20. The content of this RSS Feed (c) The Royal Society of Chemistry
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N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK ()
Med. Chem. Commun., 2018, 9,963-968 DOI: 10.1039/C8MD00068A, Research Article Agnese C. Pippione, Stefano Sainas, Antonella Federico, Elisa Lupino, Marco Piccinini, Michael Kubbutat, Jean-Marie Contreras, Christophe Morice, Alessandro Barge, Alex Ducime, Donatella Boschi, Salam Al-Karadaghi, Marco L. Lolli Resulting from hit-to-lead optimization, the aminopyrazole 3a is a NIK inhibitor selective over 44 kinases. The content of this RSS Feed (c) The Royal Society of Chemistry
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Discovery of indoleamine 2,3-dioxygenase inhibitors using machine learning based virtual screening ()
Med. Chem. Commun., 2018, 9,937-945 DOI: 10.1039/C7MD00642J, Research Article Hongao Zhang, Wei Liu, Zhihong Liu, Yingchen Ju, Mengyang Xu, Yue Zhang, Xinyu Wu, Qiong Gu, Zhong Wang, Jun Xu Indoleamine 2,3-dioxygenase (IDO), an immune checkpoint, is a promising target for cancer immunotherapy. The content of this RSS Feed (c) The Royal Society of Chemistry
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