37465-31-9Relevant articles and documents
Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a γδ-T lymphocytes-mediated activation mechanism
Simoni, Daniele,Gebbia, Nicola,Invidiata, Francesco Paolo,Eleopra, Marco,Marchetti, Paolo,Rondanin, Riccardo,Baruchello, Riccardo,Provera, Stefano,Marchioro, Carla,Tolomeo, Manlio,Marinelli, Luciana,Limongelli, Vittorio,Novellino, Ettore,Kwaasi, Aaron,Dunford, James,Buccheri, Simona,Caccamo, Nadia,Dieli, Francesco
, p. 6800 - 6807 (2008)
A small series of aminobisphosphonates (N-BPs) structurally related to zoledronic acid was synthesized with the aim of improving activity toward activation of human γδ T cells and in turn their in vivo antitumor activity. The absence of the 1-OH moiety, together with the position and the different basicity of the nitrogen, appears crucial for antitumor activity. In comparison to zoledronic acid, compound 6a shows a greater ability to activate γδ T cells expression (100 times more) and a proapoptotic effect that is better than zoledronic acid. The potent activation of γδ T cells, in addition to evidence of the in vivo antitumor activity of 6a, suggests it may be a new potential drug candidate for cancer treatment.
Synthesis of functionalized bisphosphonates via click chemistry
Skarpos, Hanna,Osipov, Sergey N.,Vorob'Eva, Daria V.,Odinets, Irina L.,Lork, Enno,Roeschenthaler, Gerd-Volker
, p. 2361 - 2367 (2007)
An efficient general synthetic approach giving the possibility for facile, rapid and cheap access to a wide range of novel nitrogen-bisphosphonates (N-BPs) as potent drug candidates, based on the reaction of mono- and bis-propargyl-substituted bisphosphon
(2-Aminobenzothiazole)-Methyl-1,1-bisphosphonic acids: Targeting matrix metalloproteinase 13 inhibition to the bone
Laghezza, Antonio,Piemontese, Luca,Brunetti, Leonardo,Caradonna, Alessia,Agamennone, Mariangela,Loiodice, Fulvio,Tortorella, Paolo
, p. 1 - 14 (2021/02/05)
Matrix Metalloproteinases (MMPs) are a family of secreted and membrane-bound enzymes, of which 24 isoforms are known in humans. These enzymes degrade the proteins of the extracellular matrix and play a role of utmost importance in the physiological remodeling of all tissues. However, certain MMPs, such as MMP-2, -9, and -13, can be overexpressed in pathological states, including cancer and metastasis. Consequently, the development of MMP inhibitors (MMPIs) has been explored for a long time as a strategy to prevent and hinder metastatic growth, but the important side effects linked to promiscuous inhibition of MMPs prevented the clinical use of MMPIs. Therefore, several strategies were proposed to improve the therapeutic profile of this pharmaceutical class, including improved selectivity toward specific MMP isoforms and targeting of specific organs and tissues. Combining both approaches, we conducted the synthesis and preliminary biological evaluation of a series of (2-aminobenzothiazole)-methyl-1,1-bisphosphonic acids active as selective inhibitors of MMP-13 via in vitro and in silico studies, which could prove useful for the treatment of bone metastases thanks to the bone-targeting capabilities granted by the bisphosphonic acid group.
Challenging synthesis of bisphosphonate derivatives with reduced steric hindrance
Chiminazzo, Andrea,Sperni, Laura,Fabris, Fabrizio,Scarso, Alessandro
, (2021/04/12)
An alternative approach is reported for the synthesis of methyl ester protected bisphosphonate building blocks, such as methylene bisphosphonate, vinylidenebisphosphonate and aryl substituted prochiral vinylidenebisphosphonates, that cannot be obtained directly from dimethyl phosphite and dichloromethane.
PHOSPHONATE CONJUGATES AND USES THEREOF
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Paragraph 0089, (2020/07/31)
Phosphonate conjugates, preferably, bisphosphonate conjugates; methods of inhibiting Ron receptor tyrosine kinase and methods of treatment of bone destruction due to cancer or other conditions utilizing the provided phosphonate conjugates.
