摘要 :
A series of norcantharidin (NCTD) analogues have been synthesized by [3+2]1,3-dipolar cycloaddition reaction of norcantharidin derivatives of substituted aromatic amines with four nitrile oximes. All analogues have been screened f...
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A series of norcantharidin (NCTD) analogues have been synthesized by [3+2]1,3-dipolar cycloaddition reaction of norcantharidin derivatives of substituted aromatic amines with four nitrile oximes. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumor cell lines: KB, SGC-7901, HL60, Bel-7402, HO-8910, and ECA109, producing IC50 values from 0.36 µmol/L to >100 µmol/L. Compound 9d showed potency for the treatment of hepatoma, with IC50 value to Bel-7402 cell line comparable to that of norcantharidin.Key words: norcantharidin analogues, isoxazoline, growth inhibition.On a réalisé la synthèse d'une série d'analogues de la norcantharidine en procédant à une réaction de cycloaddition 1,3-dipolaire [3+2] de dérivés de la norcantharidine d'amines aromatiques substituées avec quatre oximes de nitriles. On a évalué l'activité comme inhibiteur de croissance in vitro de chacun des analogues contre un ensemble de souches de cellules tumorales: KB, SGC-7901, HL60, Bel-7402, HO-8910 et ECA109 pour lesquelles les valeurs de IC50 varient de 0,36 µmol/L à plus de 100 µmol/L. Le composé 9d présente un grand potentiel pour le traitement de l'hépatome, avec une valeur de IC50 qui, par comparaison avec celle des cellules Bel-7402, est comparable à celle de la norcantharidine.Mots-clés : analogues de la norcantharidine, isoxazoline, inhibition de la croissance. [Traduit par la Rédaction]
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摘要 :
xs1 is a male-sterile rice mutant derived from a spontaneous mutation. The floret of the mutant, consisting of 6 stamens and 1 pistil, looks the same as that of the wild type except that the filaments are long and thin and the ant...
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xs1 is a male-sterile rice mutant derived from a spontaneous mutation. The floret of the mutant, consisting of 6 stamens and 1 pistil, looks the same as that of the wild type except that the filaments are long and thin and the anthers are withered in white transparence. It is confirmed that xs1 is a no-pollen type of male-sterile mutant, for no pollen grains can be stained with I2-KI solution and the anther locules are always hollow. Anther transverse sections indicate that the mutant microspores are abnormally condensed and agglomerated to form a deeply stained cluster at the late microspore stage, which results in cessation of the vacuolation process of microspores, and, therefore, the mutant forms no functional pollens for reproduction. Genetic analysis of 4 F2 populations and 3 BC1F1 populations revealed that the mutation is controlled by a single recessive gene, termed VR1 (Vacuolation retardation 1). Screening of 432 F2 mutant individuals derived from the cross of xs1 × G603 with simple sequence repeat markers revealed that VR1 is located between the molecular markers RM17411 and RM5030, at distances of 0.7 and 1.5 cM, respectively, on chromosome 4. VR1 is a new male fertility controlling gene located on chromosome 4 in rice.
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Electrical characteristics of HfO2/SiO2 interface are comprehensively studied to clarify the intrinsic origin of flatband voltage (VFB) shift in metal-oxide-semiconductor (MOS) device with high-k/metal gate structure. A methodolog...
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Electrical characteristics of HfO2/SiO2 interface are comprehensively studied to clarify the intrinsic origin of flatband voltage (VFB) shift in metal-oxide-semiconductor (MOS) device with high-k/metal gate structure. A methodology for quantitative extraction of the interface dipole and chargers at high-k/SiO2 interface is proposed. The dipole and charges at HfO2/SiO2 interface are extracted to be about -0.38 V and -1.15×1013 cm-2, respectively. This result shows that the high density of negative charges at HfO2/SiO2 interface rather than the interface dipole are the dominant cause of the positive VFB shift in the MOS device with HfO2/SiO2 stack.
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Thermoelectric properties of lattice-matched AlInN grown by metal organic chemical vapor deposition were measured and analyzed. The n-type Al0.83In0.17N alloy exhibited thermal conductivity of 4.87 W/(m K) measured by 3ω differe...
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Thermoelectric properties of lattice-matched AlInN grown by metal organic chemical vapor deposition were measured and analyzed. The n-type Al0.83In0.17N alloy exhibited thermal conductivity of 4.87 W/(m K) measured by 3ω differential method. The Seebeck coefficient of n-Al0.83In0.17N was measured as -6.012×10-4 V/K by thermal gradient method. The sheet resistivity of n-Al0.83In0.17N was measured by using Van der Pauw method, and the electrical conductivity was measured as 2.38×104/(Ω m). The thermoelectric figure of merit (Z*T) of n-type Al0.83In0.17N was measured as 0.532 at room temperature (T=300 K). The finding indicates lattice-matched AlInN alloy on GaN as excellent material candidate for thermoelectric application.
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