MedChemComm



Small molecule inhibitors in pancreatic cancer ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00447E, Review Article Jufeng Sun, Cecilia C. Russell, Christopher J. Scarlett, Adam McCluskey Pancreatic cancer (PC), with a 5-year survival of <7%, is one of the most fatal of all human cancers. There is an urgent need to develop more effective therapies to move beyond the current dire condition and paucity of PC treatment options. 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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Cyclic boronates as versatile scaffolds for KPC-2 β-lactamase inhibition ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00557A, Research Article Catherine L. Tooke, Philip Hinchliffe, Alen Krajnc, Adrian J. Mulholland, Jürgen Brem, Christopher J. Schofield, James Spencer Mono- (vaborbactam) and bi-cyclic (taniborbactam) boronate inhibitors bind KPC-2 similarly, but the latter is essentially irreversible. 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 and characterization of a novel peptide inhibitor against influenza neuraminidase ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00473D, Research Article Jianmei Chen, Shujun Feng, Yurui Xu, Xinyu Huang, Jikang Zhang, Jiao Chen, Xueying An, Yu Zhang, Xinghai Ning An optimized octapeptide (errKPAQP), exhibits nanomolar affinity to influenza neuraminidase, can notably inhibit neuraminidase activity, and protect mice from influenza infection in vivo, indicating that errKPAQP is a promising anti-influenza drug. 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 winds of change ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/D0MD90001J, Editorial Editor-in-Chief Gerhard Ecker and Executive Editor Katie Lim introduce the journal's recent name change from MedChemComm to RSC Medicinal Chemistry. 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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Argininamide-type neuropeptide Y Y1 receptor antagonists: the nature of Nω-carbamoyl substituents determines Y1R binding mode and affinity ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00538B, Research Article Jonas Buschmann, Theresa Seiler, Günther Bernhardt, Max Keller, David Wifling Replacement of the carbamoyl residue (R) in reference compound 2 by larger residues (e.g. 72) strongly affected Y1R affinity. In case of very bulky carbamoyl substituents (e.g. 78), an inverted binding mode was suggested by induced-fit docking. 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 potent CPP6–gemcitabine conjugates against human prostate cancer cell line (PC-3) ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00489K, Research Article Cristiana Correia, Cristina P. R. Xavier, Diana Duarte, Abigail Ferreira, Sara Moreira, M. Helena Vasconcelos, Nuno Vale Gemcitabine conjugation with CPP6 significantly enhanced cell growth inhibitory activity on PC-3 cells, with IC50 between 14 and 15 nM. 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 inhibitor leads of human tropomyosin receptor kinase A (hTrkA) ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00554D, Research Article Govindan Subramanian, Rajendran Vairagoundar, Scott J. Bowen, Nicole Roush, Theresa Zachary, Christopher Javens, Tracey Williams, Ann Janssen, Andrea Gonzales New hTrkA kinase domain type 2 inhibitors and mixed type 1/type 2 inhibitor leads disclosed here offers a differential starting point to investigate the disease pathophysiology. 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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meta-Substituted benzenesulfonamide: a potent scaffold for the development of metallo-β-lactamase ImiS inhibitors ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00455F, Research Article Ya Liu, Cheng Chen, Le-Yun Sun, Han Gao, Jian-Bin Zhen, Ke-Wu Yang Meta-substituted benzenesulfonamides specifically inhibit metallo-β-lactamase ImiS with an IC50 value ranging from 0.11 to 0.86 μM. 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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Hydrocortisone/cyclodextrin complex electrospun nanofibers for a fast-dissolving oral drug delivery system ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00390H, Research Article Asli Celebioglu, Tamer Uyar Hydrocortisone/cyclodextrin complex nanofibrous webs were produced via electrospinning in order to develop a fast-dissolving oral drug delivery system. 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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Macrocyclic peptidomimetics as inhibitors of insulin-regulated aminopeptidase (IRAP) ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00485H, Research Article Nicholas Barlow, Sudarsana Reddy Vanga, Jonas Sävmarker, Anja Sandström, Peta Burns, Anders Hallberg, Johan Åqvist, Hugo Gutiérrez-de-Terán, Mathias Hallberg, Mats Larhed, Siew Yeen Chai, Philip E. Thompson The IRAP inhibition of the macrocyclic peptide, HA-08 has been explored by analogue design coupled to molecular dynamics analysis. 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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Introducing a new category of activity cliffs combining different compound similarity criteria ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00463G, Research Article Huabin Hu, Jürgen Bajorath Similarity relationships. Shown are matched molecular pair (MMP) and structural isomer relationships, which provide the basis for the introduction of a new category of activity cliffs. 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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Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00441F, Research Article Xiao-Bing Wang, Fu-Cheng Yin, Ming Huang, Neng Jiang, Jin-Shuai Lan, Ling-Yi Kong Good permeability to cross the blood–brain barrier; low toxicity to PC12 cells. 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 effect of polar headgroups and spacer length on the DNA transfection of cholesterol-based cationic lipids ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00459A, Research Article Widchaya Radchatawedchakoon, Chopaka Thongbamrer, Wuttiphong Konbamrung, Phakamas Khattawee, Uthai Sakee, Wanlapa Roobsoong, Jetsumon Sattabongkot, Praneet Opanasopit, Boon-ek Yingyongnarongkul Lysine-diamine-conjugated cholesterol-based cationic lipids with different headgroups and spacer lengths were synthesized. The active lipid was studied on the basis of transfection efficiency and physicochemical properties. 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-based design and analysis of SuFEx chemical probes ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00542K, Review Article Lyn H. Jones, Jeffery W. Kelly Binding site microenvironments determine the context-dependent reactivity of sulfur(VI) fluoride-containing 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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