78715-56-7Relevant articles and documents
Convenient method for the synthesis and some transformations of the lithium salt of bis(diethoxyphosphoryl)fluoromethane
Martynov,Sokolov,Aksinenko,Goreva,Epishina,Pushin
, p. 1983 - 1984 (1998)
A convenient method was developed for the synthesis of the lithium salt of 1,1-bis(diethoxyphosphoryl)fluoromethane from available O,O-diethyl (chlorofluoromethyl)phosphonate, and some transformations of the resulting salt were studied.
RNAI AGENTS FOR INHIBITING EXPRESSION OF HIF-2 ALPHA (EPAS1), COMPOSITIONS THEREOF, AND METHODS OF USE
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Paragraph 0240; 0401, (2020/07/25)
The present disclosure relates to RNAi agents, for example, double stranded RNAi agents, able to inhibit HIF-2 alpha ( EPAS1 ) gene expression. Also disclosed are pharmaceutical compositions that include HIF-2 alpha RNAi agents and methods of use thereof. The HIF-2 alpha RNAi agents disclosed herein may be linked or conjugated to targeting ligands (such as compounds that have affinity for integrins, including alpha-v-beta-3 and alpha-v-beta-5 integrins) and pharmacokinetic (PK) enhancers, to facilitate the delivery to cells and tissues, including to clear cell renal cell carcinoma (ccRCC) cells and tumors. Delivery of compositions comprising the HIF-2 alpha RNAi agents in vivo provides for inhibition of HIF-2 alpha gene expression. The HIF-2 alpha RNAi agents can be used in methods of treatment of various diseases and disorders, including ccRCC.
1-(Fluoroalkylidene)-1,1-bisphosphonic acids are potent and selective inhibitors of the enzymatic activity of Toxoplasma gondii farnesyl pyrophosphate synthase
Szajnman, Sergio H.,Rosso, Valeria S.,Malayil, Leena,Smith, Alyssa,Moreno, Silvia N. J.,Docampo, Roberto,Rodriguez, Juan B.
experimental part, p. 1424 - 1433 (2012/04/04)
α-Fluorinated-1,1-bisphosphonic acids derived from fatty acids were designed, synthesized and biologically evaluated against Trypanosoma cruzi, the etiologic agent of Chagas disease, and against Toxoplasma gondii, the agent responsible for toxoplasmosis, and also towards the target parasitic enzymes farnesyl pyrophosphate synthase of T. cruzi (TcFPPS) and T. gondii (TgFPPS). Interestingly, 1-fluorononylidene-1,1-bisphosphonic acid (compound 43) proved to be an extremely potent inhibitor of the enzymatic activity of TgFPPS at the low nanomolar range, exhibiting an IC50 of 30 nM. This compound was two-fold more potent than risedronate (IC50 = 74 nM) that was taken as a positive control. This enzymatic activity was associated with a strong cell growth inhibition against tachyzoites of T. gondii, with an IC50 value of 2.7 μM.