MedChemComm



Protein modification by thiolactone homocysteine chemistry: a multifunctionalized human serum albumin theranostic ()
RSC Med. Chem., 2020, Accepted Manuscript DOI: 10.1039/C9MD00516A, Research Article Tatyana Vitalievna Popova, Olesya A. Krumkacheva, Anna S. Burmakova, Anna S. Spitsyna, Olga D. Zakharova, Vladimir Aleksandrovich Lisitskiy, Igor A. Kirilyuk, Vladimir N. Silnikov, Michael Keith Bowman, Elena Bagryanskaya, Tatyana Godovikova As the most abundant protein with a variety of physiological functions, albumin has been used extensively for the delivery of therapeutic molecules. Thiolactone chemistry provides a powerful tool to prepare... The content of this RSS Feed (c) The Royal Society of Chemistry
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Identification of N-benzothiazolyl-2-benzenesulfonamides as novel ABCA1 expression upregulators ()
RSC Med. Chem., 2020, 11,411-418 DOI: 10.1039/C9MD00556K, Research Article Hongtao Liu, Xinhai Jiang, Xinfeng Gao, Wenhua Tian, Chen Xu, Ruizhi Wang, Yanni Xu, Liping Wei, Feng Cao, Wenyan Li A series of N-benzothiazolyl-2-benzenesulfonamides were designed and synthesized as novel ABCA1 expression upregulators. The content of this RSS Feed (c) The Royal Society of Chemistry
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Isoquinoline thiosemicarbazone displays potent anticancer activity with in vivo efficacy against aggressive leukemias ()
RSC Med. Chem., 2020, 11,392-410 DOI: 10.1039/C9MD00594C, Research Article Daniel L. Sun, Soumya Poddar, Roy D. Pan, Ethan W. Rosser, Evan R. Abt, Juno Van Valkenburgh, Thuc M. Le, Vincent Lok, Selena P. Hernandez, Janet Song, Joanna Li, Aneta Turlik, Xiaohong Chen, Chi-An Cheng, Wei Chen, Christine E. Mona, Andreea D. Stuparu, Laurent Vergnes, Karen Reue, Robert Damoiseaux, Jeffrey I. Zink, Johannes Czernin, Timothy R. Donahue, Kendall N. Houk, Michael E. Jung, Caius G. Radu Potent α-N-heterocyclic carboxaldehyde thiosemicarbazone (HCT) antiproliferatives were synthesized through iterative rounds of methylation and fluorination modifications, with anticancer activities being potentiated by physiological levels of copper. The content of this RSS Feed (c) The Royal Society of Chemistry
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Monitoring protein-metal binding by 19F NMR – a case study with the New Delhi metallo-β-lactamase 1 ()
RSC Med. Chem., 2020, 11,387-391 DOI: 10.1039/C9MD00416E, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Anna M. Rydzik, Jürgen Brem, Shane A. Chandler, Justin L. P. Benesch, Timothy D. W. Claridge, Christopher J. Schofield 19F protein labeling enables monitoring of metal binding to the active site of NDM-1. The content of this RSS Feed (c) The Royal Society of Chemistry
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Virulence attenuating combination therapy: a potential multi-target synergy approach to treat Pseudomonas aeruginosa infections in cystic fibrosis patients ()
RSC Med. Chem., 2020, 11,358-369 DOI: 10.1039/C9MD00566H, Review Article Elana Shaw, William M. Wuest Virulence attenuating combination therapy may be a promising approach to treating chronic P. aeruginosa infections in patients with cystic fibrosis. The content of this RSS Feed (c) The Royal Society of Chemistry
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Production of biomedical cell products: requirements for the quality of donor material and excipients of animal origin (review) ()
RSC Med. Chem., 2020, 11,349-357 DOI: 10.1039/C9MD00529C, Review Article Marina A. Vodiakova, Aliya R. Sayfutdinova, Ekaterina V. Melnikova, Artem A. Goryaev, Natalia P. Sadchikova, Vladimir I. Gegechkori, Vadim A. Merkulov Donor biological materials and excipients of animal origin are important components in the production of biomedical cell products (BMCPs). The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives ()
RSC Med. Chem., 2020, 11,378-386 DOI: 10.1039/C9MD00597H, Research Article Jelena Rupar, Vladimir Dobričić, Jelena Grahovac, Siniša Radulović, Žiga Skok, Janez Ilaš, Mara Aleksić, Jasmina Brborić, Olivera Čudina Compounds 6, 7, 8 and 9 exhibit lower or similar IC50 values compared to amsacrine and showed a lack of toxicity towards unstimulated normal human leucocytes. The content of this RSS Feed (c) The Royal Society of Chemistry
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Application of triazoles as bioisosteres and linkers in the development of microtubule targeting agents ()
RSC Med. Chem., 2020, 11,327-348 DOI: 10.1039/C9MD00458K, Review Article M. Shaheer Malik, Saleh A. Ahmed, Ismail I. Althagafi, Mohammed Azam Ansari, Ahmed Kamal Application of triazoles in the development of microtubule targeting agents. 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, 11,370-377 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. The content of this RSS Feed (c) The Royal Society of Chemistry
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Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00559E, Research Article M. I. Osella, M. O. Salazar, M. D. Gamarra, D. M. Moreno, F. Lambertucci, D. E. Frances, R. L. E. Furlan N α ,Nτ-Di-4-trifluorobenzenesulfonyl histamine inhibits α-glucosidase in vitro reversibly and selectively with a Ki value of 11.6 μM, and shows an in vivo hypoglycemic effect 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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Reversing binding sensitivity to A147T translocator protein ()
RSC Med. Chem., 2020, Advance Article DOI: 10.1039/C9MD00580C, Research Article Sophie V. Vo, Samuel D. Banister, Isaac Freelander, Eryn L. Werry, Tristan A. Reekie, Lars M. Ittner, Michael Kassiou A loss in binding affinity at A147T relative to WT TSPO is seen with most TSPO ligands. Provision of hydrogen-bonding opportunities on indole carboxamides rescues this loss in affinity. 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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