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  • 1
    Electronic Resource
    Electronic Resource
    Specific inhibition of epidermal growth factor receptor tyrosine kinase by 4-anilinoquinazolines (1996)
    Springer
    Breast cancer research and treatment 38 (1996), S. 67-73 
    Details
    ISSN: 1573-7217
    Keywords: epidermal growth factor ; EGF receptor ; quinazolines ; IGF-I ; TGFα ; tyrosine kinase inhibitor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Since the mitogenic action of EGF is mediated by ligand-induced autophosphorylation of the EGF receptor (EGFR), and EGFR is commonly overexpressed in solid human tumours, inhibitors of receptor tyrosine kinase activity (RTK) could prove to be effective antitumour agents. Screening of a compound library using an EGF-RTK enzyme prepared from human tumour derived A431 cells identified a series of potent (IC50〈1µM) enzyme inhibitors. These inhibitors are quinazolines bearing a variety of substituted anilines at the 4-position. The most potent 4-anilinoquinazolines (IC50 ≅ 20nM) have small non-polar meta substituents on the aniline ring, and are competitive with ATP and non-competitive with substrate. The growth inhibitory activity of these agents was assessed in vitro using KB cells (human oral squamous tumour) grown in the absence or presence of EGF. A selected compound, 4-(3-chloroanilino)quinazoline (CAQ), inhibited EGF-stimulated growth in a concentration dependent manner and complete blockade was observed at concentrations (1–10 µM) which had no effect on basal growth. Selectivity of growth inhibition by CAQ was further exemplified in IGF1-stimulated KB cells where no effect was detected at concentrations which completely blocked EGF-stimulated growth. Similarly, CAQ blocked TGFα-stimulated growth in MCF-7 human breast cancer cells without affecting insulin-stimulated growth. These studies define a novel class of EGF-RTK inhibitors which are also potent and selective inhibitors of EGF-stimulated human tumour cell growthin vitro.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01803785
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  • 2
    Electronic Resource
    Electronic Resource
    Synthetic pyrethroid insecticides analysis by gas chromatography/mass spectrometry operated in negative-ion chemical ionization mode in soil, moss and fish tissue (1995)
    New York, NY : Wiley-Blackwell
    Rapid Communications in Mass Spectrometry 9 (1995), S. 1411-1417 
    Details
    ISSN: 0951-4198
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Physics
    Notes: A gas chromatographic/mass spectrometric method was developed for the simultaneous determination of five synthetic pyrethroid insecticides in soil, moss and fish tissue. These pyrethroids were extracted with hexane-dichloromethane by ultrasonication and cleaned up on Florisil (soil and moss) and mixed acid/base alumina (fish) columns prior to determination by gas chromatography/negative-ion chemical ionization mass spectrometry in selected ion monitoring mode. All the pyrethroids were analyzed simultaneously in a single run on a DB5-MS 15 m capillary column. Recoveries of the pyrethroids from the three matrices at fortification levels of 10, 50 and 100 μg/kg ranged from 80 to 117%. Four determinations were made at each concentration level for each matrix. The practical determination limit of the method was in the range 0.5 to 5 μg/kg depending on the compound. This method was also applied to samples obtained from a contaminated ecosystem.
    Additional Material: 5 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/rcm.1290091418
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Dose-dependent influence of Campoletis sonorensis polydnavirus on the development and ecdysteroid titers of last-instar Heliothis virescens larvae (1988)
    New York, NY [u.a.] : Wiley-Blackwell
    Archives of Insect Biochemistry and Physiology 8 (1988), S. 113-126 
    Details
    ISSN: 0739-4462
    Keywords: insect viruses ; parasitoid ; prothoracic glands ; Chemistry ; Food Science, Agricultural, Medicinal and Pharmaceutical Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology
    Notes: Campoletis sonorensis calyx fluid arrests the development of last-instar Heliothis virescens larvae and is associated with the gross degeneration of the host's prothoracic glands. Through manipulations of ovary supernatant, Campoletis sonorensis polydnavirus (CsV) was found to be the only component of calyx fluid responsible for causing host developmental arrest. Venom from C. sonorensis had no effect on host development. Suspensions of CsV were quantified, and various doses were injected into last-instar hosts. The percentage of larvae developmentally arrested was dose dependent. In addition, larvae not arrested by injection with CsV suspensions were developmentally delayed in a dose-dependent manner. Hosts were delayed in the stage in which they were injected and, after recovery, developed at normal rates. Measurements by radioimmunoassay indicated that developmental delay was due to a suppression of ecdysteroid titers. After a dose-dependent period of suppression, hemolymph ecdysteroid titers recovered and reached titers comparable to those observed in saline-injected controls. Examination of prothoracic glands from developmentally delayed larvae revealed that partial degeneration occurred. Comparisons of the number and mean size of surviving gland cells and the length of developmental delay suggested that surviving gland cells may compensate for degenerated cells by increasing their ecdysone production.
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/arch.940080205
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    Paper (German National Licenses)
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