72918-18-4Relevant academic research and scientific papers
A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790Mmutant with improved pharmacokinetic properties
Yu, Lei,Huang, Minhao,Xu, Tianfeng,Tong, Linjiang,Yan, Xiao-e,Zhang, Zhang,Xu, Yong,Yun, Caihong,Xie, Hua,Ding, Ke,Lu, Xiaoyun
supporting information, p. 1107 - 1117 (2016/12/30)
Structural optimization of pyrido[2,3-d]pyrimidin-7-ones was conducted to yield a series of new selective EGFRT790Minhibitors with improved pharmacokinetic properties. One of the most promising compound 9s potently suppressed EGFRL858R/T790Mkinase and inhibited the proliferation of H1975?cells with IC50values of 2.0?nM and 40?nM, respectively. The compound dose-dependently induced reduction of the phosphorylation of EGFR and downstream activation of ERK in NCI[sbnd]H1975?cells. It also exhibited moderate plasma exposure after oral administration and an oral bioavailability value of 16%. Compound 9s may serve as a promising lead compound for further drug discovery overcoming the acquired resistance of non-small cell lung cancer (NSCLC) patients.
The synthesis of non-symmetrical stilbene analogs of trans-resveratrol using the same Pd catalyst in a sequential double-Heck arylation of ethylene
Nobre, Sabrina M.,Muniz, Mauro N.,Seferin, Marcus,Da Silva, Wagner M.,Monteiro, Adriano L.
experimental part, p. 289 - 293 (2012/01/04)
We have developed a sequential and selective Pd-catalyzed double-Heck arylation of ethylene that results in non-symmetrical nitro-stilbene analogs of trans-resveratrol at excellent yields. A catalytic system consisting of Pd(OAc)2 and P(o-tolyl)3 permitted us to carry out the two consecutive Heck arylations without losing activity from the first to the second Heck reaction. After the first Heck arylation of ethylene, no isolation or additional catalyst loading is required for the second Heck arylation reaction. This protocol was applied to the synthesis of methylated trans-resveratrol, which was obtained at a 65% overall yield.
Preparative fluorous mixture synthesis of diazonium-functionalized oligo(phenylene vinylene)s
Jian, Huahua,Tour, James M.
, p. 3396 - 3424 (2007/10/03)
(Chemical Equation Presented) A series of building blocks for the synthesis of oligo(phenylene vinylene)s (OPVs) and hybrid oligomers were prepared, and alternating Heck coupling and Horner-Wadswoth-Emmons (HWE) reactions were used to couple the building blocks. Model studies were carried out to optimize the reaction strategies. The products were made to bear aryl diazonium functionalities that allow them to be used as surface grafting moieties in hybrid silicon/molecule assemblies. A library of OPV and hybrid oligomer tetramers was synthesized using fluorous mixture synthesis (FMS). The fluorous tags, which are secondary amines bearing different numbers of fluorine atoms, were synthesized and used as phase tags in mixture synthesis. The tags and substrates were anchored together by triazene linkages. The mixture synthesis was monitored by analytical HPLC on a fluorous column, and isolation of final OPV and hybrid oligomer tetramers was achieved by preparative HPLC. At the end of the FMS, after demixing, the tagged products were detagged by cleaving the triazene linkage and generating a series of aryl diazonium compounds. The fluorous tags could be recovered and reused. The NMR spectra of the 1-aryl-3,3-dialkyltriazenes are discussed.
Contrast media
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, (2008/06/13)
The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents of formula I wherein n is 0 or 1, and where n is 1 each C6R5moiety may be the same or different; X denotes a bond or a group providing a 1
Iodinated x-ray contrast media
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, (2008/06/13)
The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula C6R6wherein three non-adjacent R groups are iodine and the remaining R groups are non-ionic, hydrophilic moieties, said compou
Contrast media
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, (2008/06/13)
The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula I STR1 (wherein n is 0 or 1, and where n is 1 each C6 R5 moeity may be the same or different; each group R is a hydrogen atom,
Contrast media
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, (2008/06/13)
The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula I STR1 (wherein n is 0 or 1, and where n is 1 each C6 R5 moeity may be the same or different; each group R is a hydrogen atom,
