A mineral oil scintillator for neutron detection has been loaded with gadolinium utilizing the solubility in mineral oil of the ternary complex formed by reacting gadolinium hexanoate with tri-n-octylphosphineoxide.
An alcoholic extract of Libocedrus decurrens Torr. was found to show significant inhibitory activity when tested in vitro against cells derived from human carcinoma of the nasopharynx (KB). Systematic fractionation of the extract led to the isolation and characterization of desoxypodophyllotoxin...
An alcoholic extract of Callitris columellaris F. Muell was found to show significant inhibitory activity when tested in vitro against cells derived from human carcinoma of the naso-pharynx (KB). Systematic fractionation of the extract led to the isolation and characterization of desoxypodophyll...
A novel series of aroylthiourea derivatives of 4-β-amino-4′-O-demethyl-4-desoxy- podophyllotoxin were synthesized. Their cytotoxicities against three cancer cell lines were investigated by MTT assay. The kDNA decatenation assay indicated that compounds 5a, 5f, 5h and 5l inhibited topoisomerase...
A novel VP-16 derivative, 4β-[N -(4‴-acetyloxyl-phenyl-1‴-carbonyl)-4″-aminoanilino]-4′-O-demethyl-4-desoxypodophyllotoxin (GL3), displayed a wide range of cytotoxicity in a panel of human tumor cell lines, with half-maximal inhibitory concentration (IC50) values ranging from 0.82 to 4.88 µM...
A series of new 4β-anilino-4′-O-demethyl-4-desoxypodophyllotoxin derivatives were prepared and evaluated for their cytotoxicities against four human cancer cell lines including KB, KB/VCR, A549 and 95D. Most compounds showed better growth-inhibition activities against tested cell lines than th...
The reactivity of 1-arenesulfonyl-2-(bromomethyl)aziridines with respect to lithium dialkylcyanocuprates and lithium dialkylcuprates (Gilman reagents) has been evaluated for the first time, pointing to the conclusion that these substrates can be applied successfully as synthetic equivalents for ...
The stereoselective hydrogenation of 2-butyne-1,4-diol into cis-2-butene-1,4-diol was studied over palladium supported on metal–organic coordination polymers of different topology (methanol, 293 K, PH2 = 1 atm). 3D-metal–organic frameworks MOF-5 (Zn4O(BDC)3, BDC = benzene-1,4-dicarboxylate), I...
The vasorelaxant and cardiac effects of N-cyano-3-pyridinecarboxamidine A were compared with those of their amide (B) or thioamide (C) congener. Cyanoamidine was the most potent skeleton in comparison with amide or thioamide, and the activities of these three compounds are more selective for vas...
A combination of sulfanyl radical addition–cyclization of the oxime ethers and hydrazones connected with alkenes and subsequent conversion of a phenylsulfanylmethyl group to a carboxyl group provides a novel method for the construction of the cyclic β-amino acids. Upon treatment with thiopheno...
Nitrogen mustard (mustine) containing an established anticancer moiety (N,N-bis(2-chloroethyl)amino is the one of the most active and widely used alkylating anticancer agents but it is too polar to cross the blood–brain barrier. The present study evaluates the utility of the dihydropyridine↔pyr...
A series of novel monooxazoline-Schiff base ligands 1 has been successfully synthesized. The Cu(I)–1a complex showed excellent catalytic activities with up to 83% ee for the asymmetric α-chlorination of β-keto esters.
One of the most intriguing plant defense reactions against herbivores is the emission of volatiles as potentially attractive signals for the natural enemies of the attacking species. Like many other low and high molecular weight chemical defenses, volatile production is under the control of the ...
A novel and efficient regioselective synthesis of various arylated highly congested 7-aryl-5-methylsulfanylindan-4-carbonitriles (3a–f), methyl 7-aryl-5-methylsulfanylindan-4-carboxylates (10a–e) and 7-aryl-5-methylsulfanylindan-4-carboxylic acids (11a–e) through base-catalyzed reaction of 6-...
Using natural gas as a fuel in the road freight sector instead of diesel could cut greenhouse gas and air quality emissions but the switch alone is not enough to meet UK climate targets. A life cycle assessment (LCA) has been conducted comparing natural gas trucks to diesel, biodiesel, dimethyl ...
BackgroundWe examined the validity and responsiveness of the Depression Anxiety and Stress Scales-21 (DASS-21) in patients with COPD following an 8-week pulmonary rehabilitation program (PRP).
Various nipecotic acid derivatives are known to be potent GABA uptake inhibitors thus being useful in the treatment of a number of neurological and psychological disorders. In this paper, the first asymmetric syntheses of 6-substituted nipecotic acid derivatives are presented. The synthetic stra...
M. Bruce, R. Bukownik, A. T. Eldefrawi, M. E. Eldefrawi, R. Goodnow, Jr, T. Kallimopoulos, K. Konno, K. Nakanishi, M. Niwa and P. N. R. Usherwood. Structure-activity relationships of analogues of the wasp toxin philanthotoxin: non-competitive antagonists of quisqualate receptors. Toxicon28, 1333...
Acute lung injury (ALI) is a deadly disease without effective chemotherapy, so far. Traditional Chinese medicine andrographis herba is frequently used in the treatment of respiratory diseases. In searching for natural anti-ALI components from andrographis herba, the activities of 3-dehydroandrog...
The capabilities of 24 strains of filamentous fungi (from 11 genera) to transform dehydroandrographolide (1) were screened. The highly region-specific hydroxylation of 1 at C-9 by Cunninghamella echinulata AS 3.3400 was observed. Five products were obtained, and they were identified as 9β-hydro...
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