944901-61-5Relevant academic research and scientific papers
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems
Grillo, Alessandro,Chemi, Giulia,Brogi, Simone,Brindisi, Margherita,Relitti, Nicola,Fezza, Filomena,Fazio, Domenico,Castelletti, Laura,Perdona, Elisabetta,Wong, Andrea,Lamponi, Stefania,Pecorelli, Alessandra,Benedusi, Mascia,Fantacci, Manuela,Valoti, Massimo,Valacchi, Giuseppe,Micheli, Fabrizio,Novellino, Ettore,Campiani, Giuseppe,Butini, Stefania,Maccarrone, Mauro,Gemma, Sandra
, (2019/09/12)
Polypharmacology approaches may help the discovery of pharmacological tools for the study or the potential treatment of complex and multifactorial diseases as well as for addictions and also smoke cessation. In this frame, following our interest in the de
Synthesis, characterization and thermal behavior study of new 1,2,3-triazole derivatives containing 1,3,4-oxadiazole ring
Nahi, Riyadh J.,Kuwait, Zainab I.
, p. 416 - 422 (2019/06/05)
In this present work, a series of new 1-(substituted-phenyl)-1H-1,2,3-triazolyl-4-carboxylic acid derivatives was synthesized via copper (I) catalyzed azide-alkyne cycloaddition reaction. Since these synthesized 1,2,3-triazole compounds containing a carbo
Small Molecule Inhibition of MicroRNA miR-21 Rescues Chemosensitivity of Renal-Cell Carcinoma to Topotecan
Naro, Yuta,Ankenbruck, Nicholas,Thomas, Meryl,Tivon, Yaniv,Connelly, Colleen M.,Gardner, Laura,Deiters, Alexander
, p. 5900 - 5909 (2018/08/04)
Chemical probes of microRNA (miRNA) function are potential tools for understanding miRNA biology that also provide new approaches for discovering therapeutics for miRNA-associated diseases. MicroRNA-21 (miR-21) is an oncogenic miRNA that is overexpressed in most cancers and has been strongly associated with driving chemoresistance in cancers such as renal cell carcinoma (RCC). Using a cell-based luciferase reporter assay to screen small molecules, we identified a novel inhibitor of miR-21 function. Following structure-activity relationship studies, an optimized lead compound demonstrated cytotoxicity in several cancer cell lines. In a chemoresistant-RCC cell line, inhibition of miR-21 via small molecule treatment rescued the expression of tumor-suppressor proteins and sensitized cells to topotecan-induced apoptosis. This resulted in a >10-fold improvement in topotecan activity in cell viability and clonogenic assays. Overall, this work reports a novel small molecule inhibitor for perturbing miR-21 function and demonstrates an approach to enhancing the potency of chemotherapeutics specifically for cancers derived from oncomir addiction.
Towards smart biocide-free anti-biofilm strategies: Click-based synthesis of cinnamide analogues as anti-biofilm compounds against marine bacteria
Sall,Ayé,Bottzeck,Praud,Blache
, p. 155 - 159 (2017/12/06)
A set of triazole-based analogues of N-coumaroyltyramine was designed to discover potential leads that may help in the control of bacterial biofilms. the most potent compounds act as inhibitors of biofilm development with EC50 closed to ampicillin (EC50 =
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands
Bai, Suping,Li, Shihong,Xu, Jinbin,Peng, Xin,Sai, Kiran,Chu, Wenhua,Tu, Zhude,Zeng, Chenbo,Mach, Robert H.
supporting information, p. 4239 - 4251 (2014/06/09)
Two novel classes of compounds targeting the sigma-2 (σ2) receptor were synthesized, and their bioactivities to binding σ1 and σ2 receptors were measured. Four novel triazole carboxamide analogues, 24d, 24e, 24f, and 39c, demonstrated high affinity and selectivity for the σ2 receptor. These data suggest 11C-labeled versions of these compounds may be potential σ2-selective radiotracers for imaging the proliferative status of solid tumors.
