MedChemComm

Identification of novel N-acetylcysteine derivatives for the treatment of hepatocellular injury ()
Med. Chem. Commun., 2017, Accepted Manuscript DOI: 10.1039/C7MD00409E, Research Article Yanmei Zhao, Shourong Liu, Ruoyu He, Limin Kong, Jianjun Xi, Jingjing Sun, Yidan Shao, Xuwang Pan, Jiankang Zhang, Rangxiao Zhuang New anti-hepatocellular injury drugs with better curative effects and fewer side effects are urgently needed at present. In this study, a series of novel N-acetylcysteine (NAC) derivatives were designed, synthesized... The content of this RSS Feed (c) The Royal Society of Chemistry
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N-Heterocyclic borneol derivatives as the inhibitors of Marburg virus glycoprotein-mediated VSIV pseudotype entry ()
Med. Chem. Commun., 2017, Accepted Manuscript DOI: 10.1039/C7MD00424A, Research Article Alena Kononova, Anastasiya Sokolova, Sergey Cheresiz, Olga Yarovara, Raisa Nikitina, Alexandr Chepurnov, Andrey G. Pokrovsky, Nariman Salakhutdonov There is currently no approved antiviral therapy for treatment of Marburg virus disease (MVD). Although the filovirus infection outbreaks are quite rare, the high mortality rates in such outbreaks make... The content of this RSS Feed (c) The Royal Society of Chemistry
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Study on the interaction between the 1,4,5,8-naphthalene diimide-spermine conjugate (NDIS) and DNA using a spectroscopic approach and molecular docking ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00389G, Research Article Zhiyong Tian, Hailong Cui, He Liu, Jun Dong, Huanyang Dong, Luyao Zhao, Xueting Li, Yan Zhang, Yingying Huang, Lina Song, Longxiang Bian, Yuxia Wang, Xuejun Xu, Chaojie Wang NDIS has obvious differences from NIS in the process of its binding to DNA. 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 use of matched molecular series networks for cross target structure activity relationship translation and potency prediction ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00465F, Research Article Christopher E. Keefer, George Chang Matched molecular series (MMS) network for PDE2A, DGAT1, and HCV showing the relationships between shared MMS/target combinations. 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 highly active anti-Pneumocystis bisbenzamidines: insight into the influence of selected substituents on the in vitro activity ()
Med. Chem. Commun., 2017, 8,2003-2011 DOI: 10.1039/C7MD00445A, Research Article D. Maciejewska, J. Zabinski, M. Rezler, P. Kazmierczak, M. S. Collins, L. Ficker, M. T. Cushion A detailed SAR study with 21 pentamidine analogues was undertaken. Four new leading structures were identified. The content of this RSS Feed (c) The Royal Society of Chemistry
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A systematic analysis of atomic protein-ligand interactions in the PDB ()
Med. Chem. Commun., 2017, 8,1970-1981 DOI: 10.1039/C7MD00381A, Research Article Renato Ferreira de Freitas, Matthieu Schapira We compiled a list of 11 016 unique structures of small-molecule ligands bound to proteins representing 750 873 protein-ligand atomic interactions, and analyzed the frequency, geometry and the impact of each interaction type. The most frequent ligand-protein atom pairs can be clustered into seven interaction types. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis and preliminary antimicrobial evaluation of N-alkyl chain-tethered C-5 functionalized bis-isatins ()
Med. Chem. Commun., 2017, 8,1982-1992 DOI: 10.1039/C7MD00434F, Research Article Amandeep Singh, Nisha, Trpta Bains, Hye Jee Hahn, Nicole Liu, Christina Tam, Luisa W. Cheng, Jong Kim, Anjan Debnath, Kirkwood M. Land, Vipan Kumar Synthesis and antimicrobial evaluation of C-5 functionalized bis-isatins against pathogenic microorganisms. The content of this RSS Feed (c) The Royal Society of Chemistry
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Cu(II) immobilized on Fe3O4@APTMS-DFX nanoparticles: an efficient catalyst for the synthesis of 5-substituted 1H-tetrazoles with cytotoxic activity ()
Med. Chem. Commun., 2017, 8,1953-1964 DOI: 10.1039/C7MD00302A, Research Article Faezeh Taghavi, Mostafa Gholizadeh, Amir Sh. Saljooghi, Mohammad Ramezani The potential of Cu(II) immobilized on Fe3O4@APTMS-DFX nanoparticles as a novel magnetically recyclable heterogeneous catalyst for the synthesis of 5-substituted 1H-tetrazoles and anti-proliferative agent. The content of this RSS Feed (c) The Royal Society of Chemistry
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Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor ()
Med. Chem. Commun., 2017, 8,1965-1969 DOI: 10.1039/C7MD00320J, Research Article Richard Fjellaksel, Marc Boomgaren, Rune Sundset, Ira H. Haraldsen, Jorn H. Hansen, Patrick J. Riss In this communication, we report the synthesis and characterization of a library of small molecule antagonists of the human gonadotropin releasing hormone receptor based upon the 2-(4-tert-butylphenyl)-4-piperazinyl-benzimidazole scaffold via Cu-catalysed azide alkyne cycloaddition. The content of this RSS Feed (c) The Royal Society of Chemistry
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An agent for optical imaging of TrkC-expressing, breast cancer ()
Med. Chem. Commun., 2017, 8,1946-1952 DOI: 10.1039/C7MD00328E, Research Article Anyanee Kamkaew, Feng Li, Zheng Li, Kevin Burgess Tropomyosin receptor kinases receptor C is expressed at high levels on the surface of tumors from metastatic breast cancer, metastatic melanoma, glioblastoma, and neuroblastoma. The content of this RSS Feed (c) The Royal Society of Chemistry
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Mitochondria-targeted betulinic and ursolic acid derivatives: synthesis and anticancer activity ()
Med. Chem. Commun., 2017, 8,1934-1945 DOI: 10.1039/C7MD00248C, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Darya A. Nedopekina, Rinat R. Gubaidullin, Victor N. Odinokov, Polina V. Maximchik, Boris Zhivotovsky, Yuriy P. Bel'skii, Veniamin A. Khazanov, Arina V. Manuylova, Vladimir Gogvadze, Anna Yu. Spivak Conjugation of native triterpenoids, namely, betulinic and ursolic acids, with a lypophilic triphenylphosphonium cation led to the dramatic enhancement, as compared to betulinic acid, of their ability to trigger the mitochondrial apoptosis pathway in various types of cancer cells. The content of this RSS Feed (c) The Royal Society of Chemistry
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Encapsulation of nor-[small beta]-lapachone into poly(D,L)-lactide-co-glycolide (PLGA) microcapsules: full characterization, computational details and cytotoxic activity against human cancer cell lines ()
Med. Chem. Commun., 2017, 8,1993-2002 DOI: 10.1039/C7MD00196G, Research Article Marcilia P. Costa, Anderson C. S. Feitosa, Fatima C. E. Oliveira, Bruno C. Cavalcanti, Gleiston G. Dias, Ewerton W. S. Caetano, Francisco A. M. Sales, Valder N. Freire, Stefano Di Fiore, Rainer Fischer, Luiz O. Ladeira, Eufranio N. da Silva Junior, Claudia Pessoa Nor-[small beta]-lapachone-loaded (N[small beta]L-loaded) microcapsules were characterized. The N[small beta]L-loaded PLGA microcapsules exhibited a pronounced initial burst release. The cytotoxic activity against a set of cancer cell lines was investigated. The content of this RSS Feed (c) The Royal Society of Chemistry
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Pyrimidine nucleotides containing a (S)-methanocarba ring as P2Y6 receptor agonists ()
Med. Chem. Commun., 2017, 8,1897-1908 DOI: 10.1039/C7MD00397H, Research Article Kiran S. Toti, Shanu Jain, Antonella Ciancetta, Ramachandran Balasubramanian, Saibal Chakraborty, Ryan Surujdin, Zhen-Dan Shi, Kenneth A. Jacobson Uracil nucleotides containing a south-bicyclo[3.1.0]hexane ((S)-methanocarba) ring system in place of the ribose ring were synthesized and shown to be potent P2Y6R agonists in a calcium mobilization assay. The content of this RSS Feed (c) The Royal Society of Chemistry
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New chemical and radiochemical routes to [18F]Rho6G-DEG-F, a delocalized lipophilic cation for myocardial perfusion imaging with PET ()
Med. Chem. Commun., 2017, 8,1891-1896 DOI: 10.1039/C7MD00326A, Research Article J. A. H. Inkster, S. Zhang, V. Akurathi, A. Belanger, S. Dubey, S. T. Treves, A. B. Packard Synthesis of the tosyl precursor (2) facilitates automated synthesis of 18F-labeled rhodamine 6G, a potential PET myocardial perfusion tracer. The content of this RSS Feed (c) The Royal Society of Chemistry
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Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer ()
Med. Chem. Commun., 2017, 8,1914-1918 DOI: 10.1039/C7MD00305F, Research Article Lian-Xiang Luo, Ying Li, Yu-Zhen Niu, Yu-Wei Wang, Qian-Qian Wang, Xing-Xing Fan, Jia-Hui Xu, Liang Liu, Elaine Lai-Han Leung, Xiao-Jun Yao Herein, we reported 5067-0952, a potent ALK inhibitor with pharmacological efficacy in non-small cell lung cancers harboring the ALK fusion oncogene. The content of this RSS Feed (c) The Royal Society of Chemistry
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Tetrahydroquinolinone derivatives as potent P-glycoprotein inhibitors: design, synthesis, biological evaluation and molecular docking analysis ()
Med. Chem. Commun., 2017, 8,1919-1933 DOI: 10.1039/C7MD00178A, Research Article S. Ranjbar, O. Firuzi, N. Edraki, O. Shahraki, L. Saso, M. Khoshneviszadeh, R. Miri Tetrahydroquinolinones bearing a phenyl ring with electron-withdrawing substitution showed remarkable P-glycoprotein inhibitory activity and significantly increased rhodamine accumulation in MES-SA/DX5 cells. The content of this RSS Feed (c) The Royal Society of Chemistry
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New application of tiplaxtinin as an effective FtsZ-targeting chemotype for an antimicrobial study ()
Med. Chem. Commun., 2017, 8,1909-1913 DOI: 10.1039/C7MD00387K, Research Article Ning Sun, Yuan-Yuan Zheng, Ruo-Lan Du, Sen-Yuan Cai, Kun Zhang, Lok-Yan So, Kwan-Choi Cheung, Chao Zhuo, Yu-Jing Lu, Kwok-Yin Wong Tiplaxtinin exhibits an excellent cell division inhibitory effect with potent antibacterial activity through interacting with FtsZ. The content of this RSS Feed (c) The Royal Society of Chemistry
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Novel lead compounds in pre-clinical development against African sleeping sickness ()
Med. Chem. Commun., 2017, 8,1872-1890 DOI: 10.1039/C7MD00280G, Review Article Michael Berninger, Ines Schmidt, Alicia Ponte-Sucre, Ulrike Holzgrabe This article reviews the recent progress in drug development against the African sleeping sickness. The content of this RSS Feed (c) The Royal Society of Chemistry
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Applications and Perspectives of Nanomaterials in Novel Vaccine Development ()
Med. Chem. Commun., 2017, Accepted Manuscript DOI: 10.1039/C7MD00158D, Review Article Yingbin Shen, Tianyao Hao, Shiyi Ou, Churan Hu, Long Chen Vaccines show great potentials for both prophylactic and therapeutic use in infections, cancer, and other diseases.With the rapid development of bio-technologies and material sciences,Nanomaterials are playing essential roles in novel... The content of this RSS Feed (c) The Royal Society of Chemistry
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Development of NMR and thermal shift assays for the evaluation of Mycobacterium tuberculosis isocitrate lyase inhibitors ()
Med. Chem. Commun., 2017, Accepted Manuscript DOI: 10.1039/C7MD00456G, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Ram Bhusal, Krunal Patel, Brooke Kwai, Anne Swartjes, Ghader Bashiri, Johannes Reynisson, Jonathan Sperry, Ivanhoe K. H. Leung The enzymes isocitrate lyase (ICL) isoforms 1 and 2 are essential for Mycobacterium tuberculosis survival within macrophages during latent tuberculosis (TB). As such, ICLs are attractive therapeutic targets for the... The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and antifungal activity of novel oxazolidin-2-one linked-1,2,3-triazole derivatives ()
Med. Chem. Commun., 2017, Accepted Manuscript DOI: 10.1039/C7MD00442G, Research Article Alejandra Ramirez-Villalva, Davir Gonzalez-Calderon, Roxana Rojas-Garcia, Carlos Gonzalez-Romero, JOAQUIN TAMARIZ, Macario Morales-Rodriguez , Nieves Zavala-Segovia, Aydee Fuentes-Benites Novel oxazolidin-2-one linked-1,2,3-triazole derivatives (4a-k) were synthesized by straightforward and versatile azide-enolate (3+2) cycloaddition. The series of compounds was screened for antifungal activity against four filamentous fungi as well as... The content of this RSS Feed (c) The Royal Society of Chemistry
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Synergistic antifungal effect of cyclized chalcone derivatives and fluconazole against Candida albicans ()
Med. Chem. Commun., 2017, Accepted Manuscript DOI: 10.1039/C7MD00440K, Research Article Aijaz Ahmad, Mohmmad Younus YOUNUS Wani, Mrudula Patel, Abilio Sobral, Adriano Duse, Faisal Aqlan, Abdullah Al-Bogami The occurrence of invasive fungal diseases, particularly in immunocompromised patients is life-threatening and increases the economic burden. The rising problem of multi-drug resistance is becoming a major concern for clinicians.... The content of this RSS Feed (c) The Royal Society of Chemistry
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Cancer nanomedicine: from PDGF targeted drug delivery ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00391A, Research Article Chandrababu Rejeeth, Raju Vivek, Varukattu NipunBabu, Alok Sharma, Xianting Ding, Kun Qian An innovative approach for the distinctively efficient action of smart targeted drug delivery to a specific cell type is obtained through the modification of the surface of nanoparticles. 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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Synergism of fused bicyclic 2-aminothiazolyl compounds with polymyxin B against Klebsiella pneumoniae ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00354D, Research Article Rong Wang, Shuang Hou, Xiaojing Dong, Daijie Chen, Lei Shao, Liujia Qian, Zhong Li, Xiaoyong Xu A series of fused bicyclic 2-aminothiazolyl compounds were synthesized and evaluated for their synergistic effects with polymyxin B (PB) against Klebsiella pneumoniae (SIPI-KPN-1712). 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, Biological Evaluation and Structure-Activity Relationship of 2-Phenylaminomethylene-cyclohexane-1,3-diones as Specific Anti-tuberculosis Agents ()
Med. Chem. Commun., 2017, Accepted Manuscript DOI: 10.1039/C7MD00350A, Research Article Muzafar Rather, ALI MOHD LONE, Bisma Teli , Zubair Shanib Bhat, Paramjeet singh singh, Mubashir Maqbool, Bashir Ahmad Shairgojray, Mohd Jamal Dar Dar, Shajrul Amin, syed khalid Yousuf, bilal ahmad bhat, Zahoor Ahmad Parry The present study utilised whole cell based phenotypic screening of thousands of diverse small molecules against Mycobacterium tuberculosis H37Rv (M.tb.) and identified cyclohexane-1,3-dione based structures 5 and 6 as hits.... The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis and structure-activity relationships of (+/-)-isochaihulactone derivatives ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00310B, Research Article Yu Zhao, Po-Yen Liu, Kan-Yen Hsieh, Pei-Ling Hsu, Masuo Goto, Susan L. Morris-Natschke, Horng-Jyh Harn, Kuo-Hsiung Lee Seventeen new derivatives of (+/-)-isochaihulactone were synthesized. SAR conclusions were first established for isochaihulactone-type compounds. 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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Orthoester functionalized N-guanidino derivatives of 1,5-dideoxy-1,5-imino-D-xylitol as pH-responsive inhibitors of [small beta]-glucocerebrosidase ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00480J, Research Article Alen Sevsek, Javier Sastre Torano, Linda Quarles van Ufford, Ed E. Moret, Roland J. Pieters, Nathaniel I. Martin Alkylated guanidinium iminosugar derivatives bearing a pH sensitive orthoester moiety are potent and selective [small beta]-glucosidase 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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Cu(II), Ga(III) and In(III) Complexes of 2-Acetylpyridine N(4)-phenylthiosemicarbazone: Synthesis, Spectral Characterization and Biological Activities ()
Med. Chem. Commun., 2017, Accepted Manuscript DOI: 10.1039/C7MD00415J, Research Article Yu-Ting Wang, Yan Fang, Meng Zhao, Xue Li, Yu-Mei Ji, Qiuxia Han In this paper, synthesis and characterization of metal complexes [Cu2(L)3]ClO4 (1), [Ga(L)2]NO3[middle dot]2H2O (2) and [In(L)2]NO3[middle dot]H2O (3) (HL = 2-acetylpyridine N(4)-phenylthiosemicarbazone) was carried out, including elemental analysis, spectra analysis (IR, UV-vis,... The content of this RSS Feed (c) The Royal Society of Chemistry
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