89277-85-0Relevant academic research and scientific papers
Palladium-Catalyzed Phosphorylation of Aryl Mesylates and Tosylates
Fu, Wai Chung,So, Chau Ming,Kwong, Fuk Yee
supporting information, p. 5906 - 5909 (2015/12/11)
The first general palladium catalyst for the phosphorylation of aryl mesylates and tosylates is reported. The newly developed system exhibits excellent functional group compatibility. For instance, free amino, keto, ester, and amido groups, as well as het
Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors
Németh, Gábor,Greff, Zoltán,Sipos, Anna,Varga, Zoltán,Székely, Rita,Sebestyén, Mónika,Jászay, Zsuzsa,Béni, Szabolcs,Nemes, Zoltán,Pirat, Jean-Luc,Volle, Jean-No?l,Virieux, David,Gyuris, ágnes,Kelemenics, Katalin,áy, éva,Minarovits, Janos,Szathmary, Susan,Kéri, Gy?rgy,Orfi, László
, p. 3939 - 3965 (2014/06/09)
Although there is a significant effort in the design of a selective CDK9/CycT1 inhibitor, no compound has been proven to be a specific inhibitor of this kinase so far. The aim of this research was to develop novel and selective phosphorus containing CDK9/CycT1 inhibitors. Molecules bearing phosphonamidate, phosphonate, and phosphinate moieties were synthesized. Prepared compounds were evaluated in an enzymatic CDK9/CycT1 assay. The most potent molecules were tested in cell-based toxicity and HIV proliferation assays. Selectivity of shortlisted compounds against CDKs and other kinases was tested. The best compound was shown to be a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activity.
STAT3 DIMERIZATION INHIBITORS
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Page/Page column 65; 66; 67, (2014/05/24)
The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as wel
An improved procedure for the synthesis of aryl phosphonates by palladium-catalysed cross-coupling of aryl halides and diethyl phosphite in polyethylene glycol
Wang, Ping,Lu, Jie,Zhang, Zhan-Hui
, p. 359 - 361 (2013/07/26)
A general and greener protocol for the synthesis of aryl phosphonates by the cross-coupling of aryl halides and diethyl phosphite using tetrakis(triphenylphosphine)palladiume/triethylamine/polyethylene glycol 600 [Pd(PPh3)4/ Et3N/PEG 600] as an efficient catalytic system has been developed. This procedure also avoids hazardous solvents and is therefore an eco-friendly alternative to the existing methods.
Development of new N-arylbenzamides as STAT3 dimerization inhibitors
Urlam, Murali K.,Pireddu, Roberta,Ge, Yiyu,Zhang, Xiaolei,Sun, Ying,Lawrence, Harshani R.,Guida, Wayne C.,Sebti, Said M.,Lawrence, Nicholas J.
supporting information, p. 932 - 941 (2013/07/27)
The O-tosylsalicylamide S3I-201 (10) was used as a starting point for design and synthesis of novel STAT-3 dimerization inhibitors with improved drug-like qualities. The phosphonic acid 12d and salicylic acids 13f, 13g with a shorter amide linker lacking
Direct synthesis of amino-substituted aromatic phosphonates via palladium-catalyzed coupling of aromatic mono-and dibromides with diethyl phosphite
Bessmertnykh, Alla,Douaihy, Christiane Morkos,Guilard, Roger
supporting information; experimental part, p. 738 - 739 (2011/04/21)
An efficient Pd-catalyzed carbon-phosphorus bond-forming route is described for the direct synthesis of diethyl arylphosphonates bearing amino and alkylamino groups on the aromatic ring. Copyright
Design and synthesis of small molecule glycerol 3-phosphate acyltransferase inhibitors
Wydysh, Edward A.,Medghalchi, Susan M.,Vadlamudi, Aravinda,Townsendd, Craig A.
scheme or table, p. 3317 - 3327 (2010/03/26)
The incidence of obesity and other diseases associated with an increased triacylglycerol mass is growing rapidly, particularly in the United States. Glycerol 3-phosphate acyltransferase (GPAT) catalyzes the ratelimiting step of glycerolipid biosynthesis, the acylation of glycerol 3-phosphate with saturated long-chain acyl-CoAs. In an effort to produce small molecule inhibitors of this enzyme, a series of benzoic and phosphonic acids was designed and synthesized. In vitro testing of this series has led to the identification of several compounds, in particular 2-(nonylsulfonamido)benzoic acid (15g), possessing moderate GPAT inhibitory activity in an intact mitochondrial assay.
Aromatic nucleophilic polysubstitution by sequential SRN1 reactions
Beugelmans, Rene,Chbani, Mohamed
, p. 290 - 305 (2007/10/02)
Substitution of aromatics (benzene, naphthalene and pyridine) by two or three distinct nucleophiles derived from phosphonates and/or thiolates can be performed by sequential photosimulated SRN1 reactions whose radical chain mechanism is compatible with the successively introduced substituents. aromatic polysubstitution / SRN1 mechanism / disubstituted aromatic / trisubstituted aromatic / distinct substituent
Phosphorus analogues of γ-aminobutyric acid, a new class of anticonvulsants
Cates,Li,Yakshe,et al.
, p. 654 - 659 (2007/10/02)
A series of phosphorus compounds, designed as analogues of γ-aminobutyric acid (GABA) in that they possess a P=O moeity separated by three atoms from an amino or acetamido group, was synthesized and tested by using in vitro GABA(A) and GABA(B) receptor bi
PREPARATION D'AMINOPHENYL-, NITROPHENYL-, PYRIDYL-, ET QUINOLYLPHOSPHONATES SOUS PHOTOSTIMULATION OU ASSISTANCE METALLIQUE; ACCES AUX ACIDES AMINOPHOSPHONIQUES CORRESPONDANTS
Bulot, J. J.,Aboujaoude, E. Elia,Collignon, N.,Savignac, P.
, p. 197 - 204 (2007/10/02)
Our aim was to study the aromatic nucleophilic substitution between the sodium anion of diethylphosphite and several halogenated substrates like: iodo-anilines, iodo-nitrobenzenes, bromo- and iodopyridines, bromoquinoline.Two coupling processes have been evaluted.The first one is the photostimulated nucleophilic substitution (SRN1), the second the promoted arylation by transition metals.We obtain good results with the first method which is efficient and simple; by contrast the second one has given only few positive results.We describe five aromatic aminophosphonic acids.
