7-Chloro-9-(2'-chlorophenyl)-2,3-dihydroacridin-4(1H)-one (3a) and 7-chloro-9-(2'-fluorophenyl)-2,3-dihydroacridin-4-(1H)-one (3b) were synthesized from 2-amino-2′,5-dichlorobenzophenone (1a) and 2-amino-5-chloro-2'-fluorobenzophenone (1b) respectively with 1,2-cyclohexanedione (...

PIM kinase family (PIM-1, PIM-2 and PIM-3) is an appealing target for the discovery and development of selective inhibitors, useful in various disease conditions in which these proteins are highly expressed, such as cancer. The significant effort put, in the recent years, towards the development...

Two series of novel 2-arylvinyl-naphtho[2,3-d]imidazol-3-ium iodide derivatives and 2-arylvinyl-naphtho[2,3-d]imidazol-3-ium bromide derivatives were designed and synthesized by the structural combination of YM155 with stilbenoids. All compounds were tested for anti-proliferative activity agains...

A series of 4-(1-aryl-5-chloro-2-oxo-1,2-dihydro-indol-3-ylideneamino)-N-substituted benzenesulfonamide derivatives (1–20) was synthesized and evaluated for its in vitro antimicrobial and anticancer activities. Antimicrobial results indicated that compounds N-(4-(1-benzoyl-5-chloro-2-oxoindolin...

Highly efficient poly functionalized pyrrolo[3,2-a]carbazoles via ring contraction through rearrangement and intramolecular Michael addition reaction using one pot multicomponent reaction (MCR) is reported for the first time. Free radical scavenging and anticancer activities were determined by D...

Three, unsymmetrical metal-free azaphthalocyanines (AzaPc) were prepared using the statistical condensation of 5,6-bis(diethylamino)-pyrazine-2,3-dicarbonitrile (A) and the pyrazinedicarbonitrile (B) substituted with alkylamine chains bearing one or two hydroxy groups. The desired AAAB type, met...

(Z)-4-(4-Methoxyphenoxy)-4-oxobut-2-enoic acid and its solid rare earth complexes LnL3·2H2O (Ln = La, Eu, Tb) were synthesized and characterized by means of MS, elemental analysis, FTIR, 13C NMR and TG–DTA. The IR and 13C NMR results show that the carboxylic groups in the complexes coordinated...

A series of 1,3,4-thiadiazole derivatives of 2-(4-formyl-2-methoxyphenoxy) acetic acid (6a–s) were synthesized by cyclization of carboxylic acid group of 2-(2-methoxy-4-(3-oxo-3-substituted phenylprop-1-enyl)phenoxy) acetic acid (4a–s) with thiosemicarbazide in the presence of POCl3 or PPA. Th...

Cysteine-dependant aspartyl protease (caspase) activation has been implicated as a part of the signal transduction pathway leading to apoptosis. It has been postulated that caspase-3 inhibition could attenuate cell damage after an ischemic event and thereby providing for a novel neuroprotective ...

Mixtures of equal amounts of the erythro and threo forms of the phenolic arylglycerol β-aryl ether 1-(4-hydroxy-3-methoxyphenyl)-2-(2-methoxyphenoxy)-1,3-propanediol were oxidized (i) with laccases from Trametes versicolor, Agaricus bisporus, Myceliophthora thermophila and Rhus vernicifera, (ii...

Kinetic resolution of rac-1,2-diols using the biocatalyst Burkholderia cepacia lipase (BCL) immobilized on a biodegradable binary blend support of hydroxypropyl methyl cellulose(HPMC)/polyvinyl alcohol (PVA) has been investigated. The immobilization technique improved enzyme activity significant...

Acinetobacter sp. utilized 3(o-methoxyphenoxy)1,2-propanediol as the sole source of carbon. Acinetobacter sp. tolerated as much as 20 mM of the substrate. The utilization of guaiacol glyceryl ether (GGE) by Acinetobacter sp. was influenced by glucose, sucrose, ammonium sulphate, ammonium nitrate...

Chiral 3-aryloxy-1,2-propanediols of >98% ee can be obtained in high yield by the nucleophilic addition of substituted phenols to chiral glycidol in the presence of triethylamine catalys followed by recrystallization in absolute ethanol. Several enantiopure compounds of pharmaceutical significan...

1,2-Propanediol and 3-aryloxy/alkyloxy derivatives thereof are bulk commodities produced directly from glycerol. Glycosylation is a promising route for their functional diversification into useful fine chemicals. Regioselective glucosylation of the secondary hydroxyl in different 1,2-propanediol...

4-Ethoxy-1,1,1-trifluoro-3-buten-2-one reacts with triethyl phosphite on heating to give a [4 + 2 cycloaddition product 2,2,2-triethoxy 2,3-dihydro-3-ethoxy-5-trifluoromethyl-1,2λ5-oxaphospholene. Its hydrolysis yields, ultimately, a 2-oxo-2-hydroxy-2, 3-dihydro-3-hydroxy 5-trifluoromethyl-1,2λ...

4-Ethoxy-1,1,1-trifluoro-3-buten-2-one (1) reacts with phenylmagnesium bromide to give ethoxy group substitution products while the reaction of 1 with organozinc compounds gives products arising from 1,2-addition to the carbonyl group. Enone 1 reacts with electron-rich aromatic systems such as i...

1,3-Dipolar cycloaddition (1,3-DC) reaction of 4-ethoxy-1,1,1-trifluoro-3-buten-2-one 1 with nitrile oxides was studied. It was found that besides its CC participating in the formation of isoxazole rings, trifluoromethyl activated CO also underwent 1,3-DC reaction with nitrile oxides to afford 1...

Three compounds, 2a, 2b, and 2c have been synthesized by an analogy with glaziovine 1 which has been claimed to have anxiolytic properties similar to diazepam. The intermediates indanones 5 have been obtained according to conventional (for 5a) or less conventional procedure (5b) and then convert...

The size distributions of aerosols can provide evidences for their sources and formation processes in the atmosphere. Size-segregated aerosols (9-sizes) were collected in urban site (Raipur: 21.2°N and 82.3°E) in central India during winter of 2012–2013. The samples were analyzed for dicarbox...

Aerosol samples were collected in autumn 2007 on day- and nighttime basis in the northern receptor site of Beijing, China. The samples were analyzed for total carbon (TC) and water-soluble dicarboxylic acids (C2–C12), oxocarboxylic acids (C2–C9), glyoxal and methylglyoxal to better understand ...