An expedient and eco-friendly synthesis of 1-aryl/heteroaryl-[1,2,4]-triazolo[4,3-a]quinoxalin-4(5H)-ones (4) has been accomplished via iodobenzene diacetate mediated oxidative intramolecular cyclization of 3-(2-(aryl/heteroarylidene)hydrazinyl)-quinoxalin-2(1H)-ones (3). Ten synthesized compoun...

the first enantioselective synthesis of seiridin, a phytotoxic dialkylsubstituted butenolide produced by three Seiridium species, fungi pathogenic for cypress, is described. The short sequence, which leads to optically pure compound 1, would be useful to the obtaining of larger quantities of the...

Recent analyses on fungal jasmonic acid (JA)-containing metabolites suggest a mode-of-action of these naturally occurring compounds as inactive storage pools of JA. Plants and/or fungi can catabolize JA into the bioactive jasmonyl-isoleucine (JA-Ile) that in turn activates the JA-Ile-pathway in ...

On account of the reported anticancer activity of triazolothiadiazines, we have synthesized a novel series of 6-arylsubstituted-3-[2-(4-substitutedphenyl)propan-2-yl]-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and tested for in-vitro cytotoxicity by trypan blue exclusion and MTT assay. These c...

Publisher SummaryLeupeptin, which is produced by several strains of Streptomyces, has been known as a potent inhibitor for trypsin-family proteases including trypsin, plasmin, kallikrein, and urokinase. One can obtain useful biospecific affinity adsorbents if leupeptin or its essential moiety ca...

In the present study compressive strength data and room temperature (RT) deformability of three V-rich V–Si–B alloys are reported. All alloys were taken from the VSS (V solid solution)-V3Si-V5SiB2 three-phase region of the respective phase diagram and differ in their primary solidification pha...

Although new agents have been approved for the treatment of MDS, the only curative approach is allogeneic hematopoietic stem cell transplantation (HSCT) and thus, in particular circumstances this procedure has been proposed as a treatment option for low risk patients. We have retrospectively ana...

BackgroundFLT3 mutations have been well-studied in acute myeloid leukemia (AML), and the detection of the FLT3 gene has become a clinical routine. However, it has not been fully analyzed in other hematologic malignancies, such as myelodysplastic syndromes (MDS).

Hypomethylating agent (HMA) failure myelodysplastic syndrome (MDS) patients have poor outcomes and urgent need for novel therapies. Hedgehog pathway signaling upregulation plays a central role in myeloid neoplasm pathogenesis and leukemia stem cell survival. We evaluated the efficacy and safety ...

The Ca2+-antagonistic properties of elnadipine derivatives have been quantified by means of binding experiments in bovine cerebral cortex membranes using 3H-nitrendipine. Competition experiments have shown a 308-fold concentration range of Ki-values (2.9 × 10−10 to 8.9 × 10−8) for elnadipine d...

This work describes a procedure giving cyclopentadienyl molybdenum(II) compounds bearing carboxylic acid function group. It involves synthesis of carboxylic acid ester functionalized cyclopentadienides, their coordination to molybdenum(II) precursor and saponification of ester function groups. T...

Oleanolic and ursolic acids are two ubiquitous isomeric triterpene phytochemicals known for their anticancer activity. A set of derivatives of the two compounds with a modified oxidation state and lipophylicity at C-3 and C-28 positions, were prepared and tested as anticancer agents versus the l...

A facile methodology for the synthesis of a multifunctional 4H-pyran -3-carboxylate, 2-(methacryloyloxy)ethyl 6-amino-5-cyano-2-methyl-4-phenyl-4H-pyran-3-carboxylate (1) via a single-step multicomponent reaction of 2-(methacryloyloxy)ethyl 3-oxobutanoate with an aldehyde and malononitrile utili...

Michael addition reactions of cyclic β-oxo ester and α-methyl cyano ester substrates with acceptor activated olefins were catalyzed by iron N−heterocyclic carbene (NHC) complexes of the type, {Cp[1-benzyl-3-alkyl-benzimidazol-2-ylidene]Fe(CO)2}I, where [alkyl = i-Pr (1) and Et (2)] in the pres...

A novel biocatalytic route for (S)-3-cyano-5-methylhexanoic acid, the key chiral intermediate of pregabalin, was successfully developed using whole cells of newly isolated Arthrobacter sp. ZJB-09277. Kinetic resolution of a series of rac-3-cyano-5-methylhexanoic acid esters bearing a β-stereoce...

A regioselective coupling of ethyl 2-(bromomethyl)-3-cyanoacrylate and primary amines is described to give ethyl 2-[(alkylamino)(cyano)methyl] acrylates in good yields. Whereas the conversion of allyl bromide in the presence of TEAF leads to the first synthesis of ethyl 3-cyano-2-(hydroxymethyl)...

(S)-3-Cyano-5-methylhexanoic acid ethyl ester is a valuable synthetic intermediate for pregabalin. Immobilized lipase PS from Pseudomonas cepacia was screened and shown to be the best biocatalyst for the enantioselective hydrolysis of 3-cyano-5-methylhexanoic acid ethyl ester, a racemic mixture ...

A nonradioactive, sensitive, rapid, and specific method for the determination of methionine adenosyltransferase activity has been established. In this method, the methyl group of S-adenosyl-l-methionine was enzymatically transferred to esculetin with the aid of catechol-O-methyltransferase and t...

Two potential boronate affinity chromatography ligands, catechol [2-(diisopropylamino)carbonyl]phenylboronate (I) and catechol [2-(diethylamino)carbonyl,4-methyl]phenylboronate (II) were synthesized by directed ortholithiation followed by boronation. Single crystal X-ray analyses of compounds I ...

A combinatorial library of 4-(2-hydroxyaryl)-3-nitro-4H-chromenes was synthesized in high yield by C4-SMe substitution in N-alkyl/phenyl 4-(methylthio)-3-nitro-4H-chromen-2-amines with a variety of phenols. The reaction always provided C2 substitution in the phenol ring, dictated by hydrogen bon...