SummaryDietary administration (0.1% in a chow diet for 8 days) of 5α-cholest-8(14)-en-3β-ol-15-one, a potent inhibitor of sterol biosynthesis with marked hypocholesterolemic action, to rats caused a 77% reduction in the levels of acyl coenzyme A:cholesterol acyl transferase activity of jejunal...
The metabolism of 5α-cholest-8(14)-en-3β-ol-15-one (I), a potent regulator of cholesterol (Chol) metabolism which has significant hypocholesterolemic activity upon oral administration to animals, has been investigated in male rats. After intragastric administration of [2,4-3H] I and [4-14C]Cho...
Summary5α-Cholest-8(14)-en-3β-ol-15-one, a hypocholesterolemic agent and a potent inhibitor of sterol biosynthesis, inhibited the growth of CHO-K1 cells incubated in medium containing fetal calf serum. The concentration of the oxysterol required to inhibit growth by 50% was 13 μM. Sodium olea...
N,N′-Diallylpentobarbital (DAPB) antagonized barbital (B)-induced sleep in mice and rats. DAPB [80 mg/kg, intraperitoneal (i.p.)] reduced the barbital (350 mg/kg, i.p.)-induced sleeping time to 40% of the control in mice. Twenty, 40 and 80 mg/kg, i.p. of DAPB reduced barbital-induced sleeping t...
This Letter reports the temperature dependencies of the relaxation time T1 (in the ranges: 100–440 K at 60 MHz; 20 K–RT at 24.667 MHz) and the second moment of the NMR line for protons (in the range: 100–350 K, 27 MHz) measured for a polycrystalline sample of 4-chloro-2-furfurylamino-5-sulfam...
The crystal and molecular structure of 6-(furfurylamino)-9-(tetrahydropyran-2-yl)purine (1) was determined at 150(2) K. The compound crystallizes in monoclinic P21/c space group with a = 10.5642(2), b = 13.6174(3), c = 10.3742(2) Å, V = 1460.78(5) Å3, Z = 4, R(F) = for 3344 unique reflections. T...
A simple and accurate high-performance liquid chromatography (HPLC) method was developed to measure levels of N-(4-hydroxyphenyl)retinamide (fenretinide, 4-HPR) and its main metabolite N-(4-methoxyphenyl)retinamide (4-MPR) in tissue. Following ultrasonic extraction of fresh tissue in acetonitril...
A series of 4-(N-phenyl-N′-substituted benzenesulfonyl)-6-(4-hydroxyphenyl)quinolines was designed, synthesized and evaluated for their biological potential as anticancer agents by screening the molecules against panel of five human cancer cell lines viz. HL-60, MiaPaCa-2, HCT116, PC-3 and HEP-...
Methods for developing manipulators to reach maximum number of isotropic positions are presented in this paper. The spatial 4R manipulators are directly obtained from 3R planar manipulators, and the 2-DOF 5R planar parallel manipulators are developed from four-bar mechanisms. In addition, a gene...
Cytotoxic agents from nature are presently the mainstay of anticancer chemotherapy, and the need to reinforce the arsenal of anticancer agents is highly desired. Chemical transformation studies carried out on betulinic acid, through concise 1,2,3-triazole synthesis via click chemistry approach a...
We previously reported the identification of novel oximes having 5-benzyl-2,4-thiazolidinedione with antihyperglycemic activity. We now report the synthesis and biological activity of a novel series of oximes and amides having α-substituted-β-phenylpropionic acids. In this series, we obtained ...
A novel series of 1-substituted aminomethyl-3-[1-(4-isobutylphenyl)ethyl]-4-(3-aryl-4-sydnonylidene) amino-1,2,4-triazol-5-thiones (9), was prepared from the 3-[1-(4-isobutylphenyl)ethyl]-4-(3-aryl-4-sydnonylidene) amino 5-mercapto-1,2,4-triazoles (8) by aminomethylation with formaldehyde and se...
No new and effective treatments have been approved for the treatment of esophageal squamous cell carcinoma (ESCC) in the past decade. Cisplatin and 5-fluoruracil are the most commonly used drugs for this disease. In order to develop a new class of drugs effective in our ESCC phenotypic screens, ...
In order to reveal the mechanism of microstructure evolution and crack propagation in laser-deposited Stellite 6 alloys, a quenching thermal fatigue test was conducted. Various detection methods were applied to observe differences between the coatings as deposited and after thermal fatigue. The ...
Low-carbon Stellite alloys such as Stellite 21 exhibit good high-temperature and corrosion properties but need improved wear resistance in some applications. In this research, two low-carbon Stellite alloys with highly increased molybdenum content are produced via laser cladding. The microstruct...
The Stellite-6/WC composite coatings were produced on AISI H13 hot work tool steel by laser cladding with mixture of Co-coated WC (WC-12Co) particles and Stellite-6 powder. The phase composition, microstructural characterization, high temperature wear resistance and thermal fatigue behavior of S...
Disbonding and delamination of Stellite hardfacing used in high-temperature valves have caused serious challenges in the power generation industry in recent years. To determine the microstructural factors that may contribute to the failures, Stellite 21 and Stellite 6 hardfacing alloys were depo...
In this study, Stellite 6/TiC particle composite with 10, 20, 30 and 40% wt TiC were coated on carbon steel substrate using the tungsten inert gas (TIG) process. Microstructure, phase evolution, microhardness and wear resistance of clad layers were studied using different examinations. According...
Cold spraying of Stellite 21 powder on low carbon steel is performed to investigate the effect of traverse speed on the deposition efficiency (DE) of high-temperature alloys. Based on the simulation of particles' impact temperature and velocity, the initial experiments are performed at diff...
Stellite alloys are of great interest in industries due to a unique combination of high temperature mechanical strength, outstanding wear and corrosion resistance. Different thermal spraying processes are used for deposition of Stellite alloys on industrial components. However, the investigation...
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