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The reversible acetylation of histones is critical for regulation of eukaryotic gene expression. The histone deacetylase inhibitors trichostatin (TSA, 1), MS-275 (2) and suberoylanilide hydroxamic acid (SAHA, 3) arrest growth in transformed cells and in human...
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1,1-Dialkyl(1,1-diaryl)-4-R-1-silacyclohexadienyl anions ( 1 ) are available by ether cleavage of the corresponding, 1,1-dialkyl(1,1-diaryl)-4-methoxy-4-R-1-silacyclohexa-2,5-dienes ( 4 ), or by deprotonation of the...
Monosubstituted phosphinic acids are esterified with orthosilicates in excellent yields. Phosphinylidene-containing acids react selectively under these conditions, while disubstituted phosphinic acids and phosphonic acids remain unchanged. One-pot procedures...
Isomerization of 2-methyl-3-butenenitrile to 3-pentenenitrile is catalyzed by nickel π-allyl cyanide complexes. The C−CN bond breaking is a key step in the catalytic mechanism, as evidenced by in situ NMR monitoring and DFT studies.
An intramolecular olefin keto-carbene cycloaddition reaction created the bicyclo[3.1.0]hexane template 10 that was necessary for the synthesis of carbocyclic amine 15. This amine is a direct precursor to a family of rigid nucleosides that are conformationally...
Per- O -silylated galactosyl iodides undergo α-glycosidation with fully functionalized glycolipids producing biologically relevant conjugates.
Six new donor–acceptor copolymers based on benzobisthiazole and various donor moieties (dithienosilole, dithienopyrrole, cyclopentadithiophene, carbazole, benzodithiophene, and bithiophene) were synthesized, characterized, and used in field-effect transistors...
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A new series of bile acid-based trioxanes 23a–d, 24a–d, 25a–d, 26a, 26b, and 26d have been synthesized and assessed for their antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice by oral route. The antimalarial activity of these...
The thermodynamic stabilities of the Gd III complexes of five hexadentate ligands which incorporate catecholate and hydroxypyridonate subunits with a range of basicities have been determined. The most stable Gd III complex at a physiological pH of 7.4 was...
The first direct borylation of a C–H bond at the 4-position of pyrene was achieved using [Ir(COD)Cl] 2 /dtbpy as the catalyst precursor and B 2 pin 2 as the boron source. The position-related photophysical properties of pyrene derivatives are reported.
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A practical synthesis of 11-membered C 2-symmetric binaphthyl ketone (R)-1, a catalyst for asymmetric epoxidation, was developed. (±)-1,1'-Binaphthyl-2,2'-dicarboxylic acid [(±)-6] was efficiently resolved by (R)-(-)-1-cyclohexylethylamine to give (R)-6 in...