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排序方式: 共有177条查询结果,搜索用时 15 毫秒
1.
ZHANG Zhi-Li WANG Hong-Tao WANG Xiao-Wei MA Xiao-Yan LIU Jun-Yi R.J. Griff B.T. Golding 《有机化学》2003,23(Z1):10-10
Cobalamin-dependent methionine synthase plays a crucial role in folate metabolism and such would appear to be an excellent target for rational antifolate drug design. However, to date, no anticancer agents directed at this enzyme are available, but the enzyme is efficiently and specifically inhibited by N2O and this has proven invaluable for evaluating the biochemical consequence of enzyme inhibition and for mechanistic studies. [1,2] 2,5-Diamino-4-oxo-6-(3-butenyl) pyrimidine, a key intermediate in synthetic inhibitors of methionine synthase, was first synthesized using γbutenyl-β-ketoester and guanidine carbonate (Scheme 1). [3] 相似文献
2.
Wu DY Hayes K Perl ML Barklow T Boyarski A Burchat PR Burke DL Dorfan JM Feldman GJ Gladney L Hanson G Hollebeek RJ Innes WR Jaros JA Karlen D Klein SR Lankford AJ Larsen RR LeClaire BW Lockyer NS Lüth V Ong RA Richter B Riles K Yelton JM Abrams G Amidei D Baden AR Boyer J Butler F Gidal G Gold MS Goldhaber G Golding L Haggerty J Herrup D Juricic I Kadyk JA Levi ME Nelson ME Rowson PC Schellman H Schmidke WB Sheldon PD Trilling GH Wood DR Schaad T 《Physical review D: Particles and fields》1990,41(7):2339-2342
3.
Ong RA Weir AJ Abrams GS Amidei D Baden AR Barklow T Boyarski AM Boyer J Burchat PR Burke DL Butler F Dorfan JM Feldman GJ Gidal G Gladney L Gold MS Goldhaber G Golding L Haggerty J Hanson G Hayes K Herrup D Hollebeek RJ Innes WR Jaros JA Juricic I Kadyk JA Karlen D Klein SR Lankford AJ Larsen RR LeClaire BW Levi M Lockyer NS Lüth V Nelson ME Perl ML Petersen A Richter B Riles K Rowson PC Schaad T Schellman H Schmidke WB Sheldon PD Trilling GH Wood DR Yelton JM 《Physical review letters》1988,60(25):2587-2590
4.
Klein SR Himel TM Abrams G Amidei D Baden AR Barklow T Boyarski AM Boyer J Burchat PR Burke DL Butler F Dorfan JM Feldman GJ Gidal G Gladney L Gold MS Goldhaber G Golding L Haggerty J Hanson G Hayes K Herrup D Hollebeek RJ Innes WR Jaros JA Juricic I Kadyk JA Karlen D Lankford AJ Larsen RR LeClaire BW Levi M Lockyer NS Lüth V Matteuzzi C Nelson ME Ong RA Perl ML Petersen A Richter B Riles K Rowson PC Schaad T Schellman H Schmidke WB Sheldon PD Trilling GH de la Vaissiere C Wood DR Yelton JM 《Physical review letters》1987,58(7):644-647
5.
Gidal G Boyer J Butler F Cords D Abrams GS Amidei D Baden AR Barklow T Boyarski AM Burchat P Burke DL Dorfan JM Feldman GJ Gladney L Gold MS Goldhaber G Golding LJ Haggerty J Hanson G Hayes K Herrup D Hollebeek RJ Innes WR Jaros JA Juricic I Kadyk JA Karlen D Klein SR Lankford AJ Larsen RR LeClaire BW Levi ME Lockyer NS Lüth V Matteuzzi C Nelson ME Ong RA Perl ML Richter B Riles K Rowson PC Schaad T Schellman H Schmidke WB Sheldon PD Trilling GH de la Vaissière C Wood DR Yelton JM Zaiser C 《Physical review letters》1987,59(18):2016-2019
6.
3-Methyl-2-butenenitrile (1) cyclodimerised on treatment with lithium diisopropylamide in dimethoxyethane at temperatures between ?78°C and 0°C to 3-amino-4-cyano-1,5,5-trimethyl-1,3-cyclohexadiene (2) the structure of which was established by acid hydrolysis to the known 4-cyano-1,5,5-trimethyl-1-cyclohexene-3-one (3). 相似文献
7.
Fred C Cantillana T Henderson AP Golding BT Törnqvist M 《Rapid communications in mass spectrometry : RCM》2004,18(18):2177-2184
Isoprene (2-methylbuta-1,3-diene) is a multi-site carcinogen in rodents. To evaluate the role of the diepoxide metabolite (1,2:3,4-diepoxy-2-methylbutane) in carcinogenesis, measurements of in vivo doses of the diepoxide are needed. The in vivo dose may be inferred from levels of reaction products with hemoglobin (Hb adducts). This report presents in vitro studies of the adduct formation by the diepoxide of isoprene with valinamide and oligopeptides as model compounds of N-terminal valines in hemoglobin (Hb). In the reaction with valinamide it was shown that isoprene diepoxide forms as the main product a ring-closed adduct, which is a pyrrolidine derivative [N,N-(2,3-dihydroxy-2-methyl-1,4-butadiyl)valinamide, MPyr-Val]. The analysis was performed by gas chromatography/mass spectrometry (GC/MS) (EI and PICI) after acetylation. The ring-closed adduct was also identified by liquid chromatography/electrospray ionization mass spectrometry (LC/ESI-MS) as the main product in the reaction between isoprene diepoxide and standard hepta- or (2H8)octapeptides, corresponding to the N-terminal peptides of the alpha-chains in mouse and rat Hb. These peptides, alkylated with isoprene diepoxide, to be used as internal standards and calibration standards for quantification of MPyr-adduct levels in vitro and in vivo, were analyzed with respect to the degree of MPyr-alkylation by two independent methods, amino acid analysis and HPLC-UV; similar results were obtained using these methods. A method for measurement of Hb adducts as modified peptides, used earlier to measure a similar adduct to N-terminal valines in Hb from the diepoxide of 1,3-butadiene, has in the present work been tested for application to isoprene diepoxide. The method is based on tryptic degradation of globin and LC/ESI-MS analysis of N-terminal Pyr-heptapeptides of the Hb alpha-chain enriched by HPLC. MPyr-adduct levels in isoprene diepoxide alkylated hemolysate from mouse erythrocytes incubated with different concentrations of isoprene diepoxide (2 and 10 mM) for 1 h were quantified. The adduct level was about 50 nmol/g alpha-chain Hb per mM x h. From the adduct levels the rate constant of isoprene diepoxide for reaction with N-terminal valine was calculated to be about 1.6 times faster than for diepoxybutane. 相似文献
8.
de la Vaissiere C Luth V Abrams GS Amidei D Baden AR Barklow T Boyarski AM Boyer J Breidenbach M Burchat P Burke DL Butler F Dillon JW Dorfan JM Feldman GJ Gidal G Gladney L Gold MS Goldhaber G Golding LG Hanson G Haggerty J Herrup D Himel T Hollebeek RJ Innes WR Jaros JA Juricic I Kadyk JA Klein SR Lankford AJ Larsen RR LeClaire BW Levi ME Lockyer NS Matteuzzi C Nelson ME Ong RA Perl ML Richter B Ross MC Rowson PC Schaad T Schellman H Schmidke WB Sheldon PD Trilling GH Yelton JM Wood DR 《Physical review letters》1985,54(19):2071-2074
9.
NiCl(2)(dppe)-catalyzed cross-coupling of aryl mesylates, arenesulfonates, and halides with arylboronic acids 总被引:2,自引:0,他引:2
An investigation of the NiCl(2)(dppe)-, NiCl(2)(dppb)-, NiCl(2)(dppf)-, NiCl(2)(PCy(3))(2)-, and NiCl(2)(PPh(3))(2)-catalyzed cross-coupling of the previously unreported aryl mesylates, and of aryl arenesulfonates, chlorides, bromides, and iodides containing electron-withdrawing and electron-donating substituents with aryl boronic acids, in the absence of a reducing agent, is reported. NiCl(2)(dppe) was the only catalyst that exhibited high and solvent-independent activity in the two solvents investigated, toluene and dioxane. NiCl(2)(dppe) with an excess of dppe, NiCl(2)(dppe)/dppe, was reactive in the cross-coupling of electron-poor aryl mesylates, tosylates, chlorides, bromides, and iodides. This catalyst was also efficient in the cross-coupling of aryl bromides and iodides containing electron-donating substituents. Most surprisingly, the replacement of the excess dppe from NiCl(2)(dppe)/dppe with excess PPh(3) generated NiCl(2)(dppe)/PPh(3), which was found to be reactive for the cross-coupling of both electron-rich and electron-poor aryl mesylates and chlorides. Therefore, the solvent-independent reactivity of NiCl(2)(dppe) provides an inexpensive and general nickel catalyst for the cross-coupling of aryl mesylates, tosylates, chlorides, bromides, and iodides with aryl boronic acids. 相似文献
10.
Tatiana A. Shmigol Samantha Hammond James B. Phillips James I. Bruce Alexander J. MacRobert Mikhail V. Malakhov Jon P. Golding 《Photochemistry and photobiology》2013,89(1):139-149
Phthalocyanine photosensitizers are effective in anticancer photodynamic therapy (PDT) but suffer from limited solubility, limited cellular uptake and limited selectivity for cancer cells. To improve these characteristics, we synthesized isopropylidene‐protected and partially deprotected tetra β‐glycosylated zinc (II) phthalocyanines and compared their uptake and accumulation kinetics, subcellular localization, in vitro photocytotoxicity and reactive oxygen species generation with those of disulfonated aluminum phthalocyanine. In MCF‐7 cancer cells, one of the compounds, zinc phthalocyanine {4}, demonstrated 10‐fold higher uptake, 5‐fold greater PDT‐induced cellular reactive oxygen species concentration and 2‐fold greater phototoxicity than equimolar (9 μm ) disulfonated aluminum phthalocyanine. Thus, isopropylidene‐protected β‐glycosylation of phthalocyanines provides a simple method of improving the efficacy of PDT. 相似文献