MedChemComm

What is medicinal chemistry? - Demystifying a rapidly evolving discipline! ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD90030A, Opinion Selina Y. L. Holbrook, Sylvie Garneau-Tsodikova Opinion article summarizing answers to this broad and controversial question obtained from over 60 people from "all walks of life", including people from academia and industry, ranging from graduate students to established researchers and professors. 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: Environment-sensitive turn-on fluorescent probes for p53-MDM2 protein-protein interaction ()
Med. Chem. Commun., 2017, 8,1727-1727 DOI: 10.1039/C7MD90031G, Correction Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Tingting Liu, Yan Jiang, Zhenzhen Liu, Jin Li, Kun Fang, Chunlin Zhuang, Lupei Du, Hao Fang, Chunquan Sheng, Minyong Li The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and molecular docking studies of xanthone attached amino acids as potential antimicrobial and anti-inflammatory agents ()
Med. Chem. Commun., 2017, 8,1706-1719 DOI: 10.1039/C7MD00209B, Research Article Xing Chen, Jing Leng, K. P. Rakesh, N. Darshini, T. Shubhavathi, H. K. Vivek, N. Mallesha, Hua-Li Qin A series of novel xanthone conjugated amino acids were synthesised and characterised by analytical and spectroscopic methods. The content of this RSS Feed (c) The Royal Society of Chemistry
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Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring ()
Med. Chem. Commun., 2017, 8,1697-1705 DOI: 10.1039/C7MD00296C, Research Article Dominik Heimann, Corinna Lueg, Henk de Vries, Bastian Frehland, Dirk Schepmann, Laura H. Heitman, Bernhard Wunsch Three pairs of regioisomeric 1,2,4- and 1,3,4-oxadiazoles were synthesized as selective CB2 ligands. Although the 1,3,4-oxadiazoles should have better physicochemical and pharmacokinetic properties, their CB2 affinity was reduced. The content of this RSS Feed (c) The Royal Society of Chemistry
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On-DNA Pd and Cu promoted C-N cross-coupling reactions ()
Med. Chem. Commun., 2017, 8,1614-1617 DOI: 10.1039/C7MD00289K, Research Article Xiaojie Lu, Sarah E. Roberts, George J. Franklin, Christopher P. Davie We developed unprecedented Pd and Cu(I) promoted C-N cross-coupling reactions between a DNA-conjugated aryl iodide and primary amines. The content of this RSS Feed (c) The Royal Society of Chemistry
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Discovery of human lactate dehydrogenase A (LDHA) inhibitors as anticancer agents to inhibit the proliferation of MG-63 osteosarcoma cells ()
Med. Chem. Commun., 2017, 8,1720-1726 DOI: 10.1039/C7MD00222J, Research Article Aiping Fang, Qi Zhang, Haibo Fan, Yaying Zhou, Yuqin Yao, Yue Zhang, Xiaojun Huang A novel inhibitor with good inhibitory potency (IC50 = 0.33 [small mu ]M) against LDHA, which reduces the growth of MG-63 cancer cells (EC50 = 3.35 [small mu ]M), was reported herein. The content of this RSS Feed (c) The Royal Society of Chemistry
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Recent advances in combretastatin based derivatives and prodrugs as antimitotic agents ()
Med. Chem. Commun., 2017, 8,1592-1603 DOI: 10.1039/C7MD00227K, Review Article Zaki S. Seddigi, M. Shaheer Malik, A Prasanth Saraswati, Saleh A. Ahmed, Ahmed O. Babalghith, Hawazen A. Lamfon, Ahmed Kamal The dynamic and crucial role of tubulin in different cellular functions rendered it a promising target in anticancer drug development. The content of this RSS Feed (c) The Royal Society of Chemistry
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Development of selective agents targeting serotonin 5HT1A receptors with subnanomolar activities based on a coumarin core ()
Med. Chem. Commun., 2017, 8,1690-1696 DOI: 10.1039/C7MD00281E, Research Article K. Ostrowska, D. Grzeszczuk, M. Gluch-Lutwin, A. Grybos, A. Siwek, L. Dobrzycki, B. Trzaskowski A screening of 18 compounds identified five coumarin derivatives with subnanomolar activity against the 5HT1A receptor. The content of this RSS Feed (c) The Royal Society of Chemistry
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Environment-sensitive turn-on fluorescent probes for p53-MDM2 protein-protein interaction ()
Med. Chem. Commun., 2017, 8,1668-1672 DOI: 10.1039/C7MD00287D, Research Article Tingting Liu, Yan Jiang, Zhenzhen Liu, Jin Li, Kun Fang, Chunlin Zhuang, Lupei Du, Hao Fang, Chunquan Sheng, Minyong Li A series of small-molecule fluorescent probes were designed and synthesized for detecting and imaging p53-MDM2 interaction in the human lung cancer cell line A549. The content of this RSS Feed (c) The Royal Society of Chemistry
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Extraction of antioxidant and antiproliferative ingredients from fruits of Rubus chingii Hu by active tracking guidance ()
Med. Chem. Commun., 2017, 8,1673-1680 DOI: 10.1039/C7MD00240H, Research Article Tian-Tian Zhang, Ya-Jun Liu, Li Yang, Jian-Guo Jiang, Jing-Wen Zhao, Wei Zhu Rubus chingii Hu, namely "Fu-pen-zi" in Chinese, has been used as a functional food in China for a long time. The content of this RSS Feed (c) The Royal Society of Chemistry
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Biscarbene gold(I) complexes: structure-activity-relationships regarding antibacterial effects, cytotoxicity, TrxR inhibition and cellular bioavailability ()
Med. Chem. Commun., 2017, 8,1681-1689 DOI: 10.1039/C7MD00269F, Research Article Claudia Schmidt, Bianka Karge, Rainer Misgeld, Aram Prokop, Mark Bronstrup, Ingo Ott Biscarbene gold(I) complexes were prepared and evaluated for their effects against cancer cells and pathogenic bacteria. The content of this RSS Feed (c) The Royal Society of Chemistry
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Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners ()
Med. Chem. Commun., 2017, 8,1659-1667 DOI: 10.1039/C7MD00247E, Research Article Romain Duroux, Antonella Ciancetta, Philip Mannes, Jinha Yu, Shireesha Boyapati, Elizabeth Gizewski, Said Yous, Francisco Ciruela, John A. Auchampach, Zhan-Guo Gao, Kenneth A. Jacobson Functionalized antagonist probes of the A2A adenosine receptor. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis, and biological evaluation of new thiazolo[5,4-d]pyrimidine derivatives as potent antiproliferative agents ()
Med. Chem. Commun., 2017, 8,1655-1658 DOI: 10.1039/C7MD00165G, Research Article Zhong-Hua Li, Xue-Qi Liu, Peng-Fei Geng, Jin-Lian Ma, Tao-Qian Zhao, Hao-Ming Wei, Bin Yu, Hong-Min Liu The thiazolo[5,4-d]pyrimidine derivative 7i exhibited potent inhibition against MGC-803 and HGC-27 with IC50 values of 4.64 and 5.07 [small mu ]M, respectively and around 12-fold selectivity between MGC-803 and GES-1. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and evaluation of oxindoles as promising inhibitors of the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1 ()
Med. Chem. Commun., 2017, 8,1640-1654 DOI: 10.1039/C7MD00226B, Research Article Saurav Paul, Ashalata Roy, Suman Jyoti Deka, Subhankar Panda, Gopal Narayan Srivastava, Vishal Trivedi, Debasis Manna Structurally simple C3-substituted oxindoles showed inhibitory activity against the immunosuppressive indoleamine-2,3-dioxygenase-1 (IDO1) enzyme. The content of this RSS Feed (c) The Royal Society of Chemistry
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Discovery of potential antifungal triazoles: design, synthesis, biological evaluation, and preliminary antifungal mechanism exploration ()
Med. Chem. Commun., 2017, 8,1631-1639 DOI: 10.1039/C7MD00112F, Research Article Yuan Zhang, Guri L. V. Damu, Sheng-Feng Cui, Jia-Li Mi, Vijai Kumar Reddy Tangadanchu, Cheng-He Zhou Synthesis of novel triazole-type miconazole analogues as potential antifungal agents and molecular modeling with CYP51 and experimental investigation with DNA suggested the possible antimicrobial mechanism. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis, molecular modeling and biological evaluation of aza-flavanones as [small alpha]-glucosidase inhibitors ()
Med. Chem. Commun., 2017, 8,1618-1630 DOI: 10.1039/C7MD00162B, Research Article Sivaprasad Kasturi, Sujatha Surarapu, Chandra Chary Bathoju, Srinivas Uppalanchi, Shubham Dwivedi, Yogeeswari Perumal, Dilep Kumar Sigalapalli, Bathini Nagendra Babu, Krishna S. Ethiraj, Jaya Shree Anireddy An efficient acid catalyzed methodology has been employed to synthesize a variety of aza-flavanones and their [small alpha]-glucosidase inhibitory activity is evaluated using acarbose, miglitol and voglibose as reference standards. The content of this RSS Feed (c) The Royal Society of Chemistry
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Developments of bioorthogonal handle-containing photo-crosslinkers for photoaffinity labeling ()
Med. Chem. Commun., 2017, 8,1585-1591 DOI: 10.1039/C7MD00217C, Review Article Haijun Guo, Zhengqiu Li "Minimalist" photo-crosslinkers (L3-L6) applied in affinity-based proteome profiling and bioimaging for target identification of small molecules. The content of this RSS Feed (c) The Royal Society of Chemistry
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Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region ()
Med. Chem. Commun., 2017, 8,1604-1613 DOI: 10.1039/C7MD00213K, Research Article Robin A. Fairhurst, Thomas Knoepfel, Catherine Leblanc, Nicole Buschmann, Christoph Gaul, Jutta Blank, Inga Galuba, Jorg Trappe, Chao Zou, Johannes Voshol, Christine Genick, Peggy Brunet-Lefeuvre, Francis Bitsch, Diana Graus-Porta, Pascal Furet Structurally diverse covalent and non-covalent series of selective FGFR4 inhibitors have been identified. The content of this RSS Feed (c) The Royal Society of Chemistry
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One-pot synthesis, anti-tumor evaluation and structure-activity relationships of novel 25-OCH3-PPD derivatives ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00358G, Research Article Fan-Zhi Qu, Chen Zhao, Jia-Qing Cao, Yan Zhang, Yu-Qing Zhao Based on the fact that 25-OCH3-PPD, a natural ginsengenin isolated from the leaves of Panax ginseng, is a promising lead compound, novel 25-OCH3-PPD derivatives were synthesized to find more potent anti-tumor agents by a simple and facile synthetic method. 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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Integrating docking scores and key interaction profiles to improve the accuracy of molecular docking: towards novel B-RafV600E inhibitors ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00229G, Research Article Chun-Qi Hu, Kang Li, Ting-Ting Yao, Yong-Zhou Hu, Hua-Zhou Ying, Xiao-Wu Dong A set of ninety-eight B-RafV600E inhibitors was used for the development of a molecular docking based QSAR model using linear and non-linear regression models. 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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An insight into tetrahydro-[small beta]-carboline-tetrazole hybrids: synthesis and bioevaluation as potent antileishmanial agents ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00125H, Research Article Pooja Purohit, Anand Kumar Pandey, Deepti Singh, Pradeep Singh Chouhan, Karthik Ramalingam, Mahendra Shukla, Neena Goyal, Jawahar Lal, Prem M. S. Chauhan A series of tetrahydro-[small beta]-carboline tetrazole derivatives have been synthesized utilizing the Ugi-tetrazole reaction and were identified as potential antileishmanial chemotypes. 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 biological evaluation of chalcone-linked pyrazolo[1,5-a]pyrimidines as potential anticancer agents ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00193B, Research Article Chandrakant Bagul, Garikapati Koteswara Rao, Venkata Krishna Kanth Makani, Jaki R. Tamboli, Manika Pal-Bhadra, Ahmed Kamal A series of chalcone-linked pyrazolo[1,5-a]pyrimidines was synthesized and evaluated for antiproliferative 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 lead compounds in pre-clinical development against African sleeping sickness ()
Med. Chem. Commun., 2017, Advance Article 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. 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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Click chemistry-assisted synthesis of triazolo linked podophyllotoxin conjugates as tubulin polymerization inhibitors ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00273D, Research Article M. V. P. S. Vishnuvardhan, Saidi Reddy V., Kunta Chandrasekhar, V. Lakshma Nayak, Ibrahim Bin Sayeed, Abdullah Alarifi, Ahmed Kamal A series of new triazolo linked 4[small beta]-amidopodophyllotoxin conjugates (9a-l) were synthesized using click chemistry and evaluated for their antitumor 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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Structure-optimized dihydropyranoindole derivative GIBH-LRA002 potentially reactivated viral latency in primary CD4+ T lymphocytes of chronic HIV-1 patients ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00327G, Research Article Qing Yang, Yuyang Ding, Fengling Feng, Enxiang Pan, Xiaozhen Fan, Xiuchang Ma, Ling Chen, Junling Zhao, Caijun Sun Based on structure modification and a high-throughput Jurkat-Lat cell screening model, we found that GIBH-LRA002 effectively reactivated the latent proviruses but without inducing systemic activation, making this compound attractive for potentially treating HIV-1 infection. 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 surface capped mesoporous silica nanoparticles for pH-stimuli responsive drug delivery applications ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00270J, Research Article Madhappan Santha Moorthy, Subramanian Bharathiraja, Panchanathan Manivasagan, Kang Dae Lee, Junghwan Oh Herein, we propose a "host-guest" complexation-based mesoporous silica drug carrier, MSNs@Mela@TTM, for pH-responsive drug delivery applications in cancer therapy. 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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MAO inhibitory activity of bromo-2-phenylbenzofurans: synthesis, in vitro study, and docking calculations ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00311K, Research Article G. L. Delogu, F. Pintus, L. Mayan, M. J. Matos, S. Vilar, J. Munin, J. A. Fontenla, G. Hripcsak, F. Borges, D. Vina Monoamine oxidase (MAO) is an enzyme responsible for metabolism of monoamine neurotransmitters which play an important role in brain development and function. 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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Polyhydroxyalkanoates as biomaterials ()
Med. Chem. Commun., 2017, Advance Article DOI: 10.1039/C7MD00252A, Review Article Bhagyashri S. Thorat Gadgil, Naresh Killi, Gundloori V. N. Rathna Polyhydroxyalkanoates are being explored exponentially for biomedical application. The collative reported information on polyhydroxyalkanoates may serve as a guide to attain novel biomaterials. 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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