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941.
Multifunctionalized tetrahydropyrimidines derivatives have been synthesized from Biginelli 3,4-dihydropyrimidin-2-(1H)-thiones (DHPMs) efficiently. The transformation includes desulfurization of DHPMs with Raney-Ni and subsequent regioselective C-2 functionalization using a variety of C-nucleophiles with simultaneous activation with ethyl chloroformate. Functionalized pyrimidine derivatives containing bulky substituents at C-2 of the pyrimidine ring are cytostatic. 相似文献
942.
Erinprit K. Singh 《Tetrahedron letters》2010,51(33):4357-579
Synthesis of nine macrocyclic peptide HDAC inhibitors and three triazole derivatives is described. HDAC inhibitory activity of these compounds against HeLa cell lysate is evaluated. The biological data demonstrate that incorporation of a triazole unit improves the HDAC inhibitory activity. 相似文献
943.
J.S. Yadav B.V. Subba Reddy Ashutosh Pratap Singh Nilanjan Majumder 《Tetrahedron letters》2010,51(17):2291-4626
Morita-Baylis-Hillman acetates undergo smooth allylic nucleophilic substitution (SN2′) with tosylmethyl isocyanide (TosMIC) in the presence of a catalytic amount of BF3·OEt2 under mild conditions to furnish trisubstituted olefins in high yields with (E)-stereoselectivity. 相似文献
944.
Sambasivarao Kotha Vittal Seema Kuldeep Singh Kodand Dinkar Deodhar 《Tetrahedron letters》2010,51(17):2301-421
Highly functionalized cage compounds have been prepared via cross-metathesis (CM) using Grubbs modified N-tolyl catalyst 7. A strategic utilization of photo-thermal metathesis and catalytic metathesis sequence for the synthesis of functionalized caged molecules has been demonstrated. 相似文献
945.
Pradeep Mathur Raj Kumar Joshi Amrendra K. Singh 《Journal of organometallic chemistry》2010,695(24):2687-2694
A facile, one pot, high yield synthesis of α,β-vinylester (1-14) and alkoxy substituted γ-lactones (15-28) has been achieved by the photochemical reaction of terminal acetylene (ferrocenyl phenyl trimethylsillyl, hexyl and cyclohexyl) with alcohol (methanol, ethanol and isopropanol) and carbon monoxide in presence of iron pentacarbonyl as a catalyst. The selectivity of the compounds depends on the time of photolysis of the reaction as well as the solvent used. A stable reaction intermediate ferrole was isolated, and further photolysis with alcohols, resulted in the formation of α,β-vinylester. All the compounds were fully characterised by spectroscopic methods and the molecular structures of compounds 1, 16, 17 and 20 were established crystallographically. 相似文献
946.
K.K. Bhasin Rishu Sukhjinder Singh H. Kumar S.K. Mehta 《Journal of organometallic chemistry》2010,695(5):648-2013
The present work reports an efficient one-pot synthesis of symmetrical pyridyl monoselenides by the reaction of bromo-/iodopyridines with the isopropylmagnesium chloride, iPrMgCl followed by quenching with selenyl chloride, SeCl2. The current methodology constitutes a convenient synthesis of bis(5-bromo-2-pyridyl) selenide (I), bis(2-bromo-5-pyridyl) selenide (II) and bis(2,5-dibromo-3-pyridyl) selenide (III) under cryogenic conditions requiring shorter time duration to give satisfactory yields. The hitherto unknown compounds have been characterized by elemental analysis and various spectroscopic techniques i.e., 1H NMR, 13C NMR, FT-IR, mass spectrometry and X-ray crystallography. 相似文献
947.
Lu W Singh AK Khan SA Senapati D Yu H Ray PC 《Journal of the American Chemical Society》2010,132(51):18103-18114
Prostate cancer is the second leading cause of cancer-related death among the American male population, and the cost of treating prostate cancer patients is about $10 billion/year in the United States. Current treatments are mostly ineffective against advanced-stage prostate cancer and are often associated with severe side effects. Driven by these factors, we report a multifunctional, nanotechnology-driven, gold nano-popcorn-based surface-enhanced Raman scattering (SERS) assay for targeted sensing, nanotherapy treatment, and in situ monitoring of photothermal nanotherapy response during the therapy process. Our experimental data show that, in the presence of LNCaP human prostate cancer cells, multifunctional popcorn-shaped gold nanoparticles form several hot spots and provide a significant enhancement of the Raman signal intensity by several orders of magnitude (2.5 × 10(9)). As a result, it can recognize human prostate cancer cells at the 50-cells level. Our results indicate that the localized heating that occurs during near-infrared irradiation can cause irreparable cellular damage to the prostate cancer cells. Our in situ time-dependent results demonstrate for the first time that, by monitoring SERS intensity changes, one can monitor photothermal nanotherapy response during the therapy process. Possible mechanisms and operating principles of our SERS assay are discussed. Ultimately, this nanotechnology-driven assay could have enormous potential applications in rapid, on-site targeted sensing, nanotherapy treatment, and monitoring of the nanotherapy process, which are critical to providing effective treatment of cancer. 相似文献
948.
949.
Munish Puri Aneet Kaur Ram Sarup Singh Anubhav Singh 《Applied biochemistry and biotechnology》2010,162(1):181-191
Response surface methodology was used to optimize the fermentation medium for enhancing naringinase production by Staphylococcus xylosus. The first step of this process involved the individual adjustment and optimization of various medium components at shake
flask level. Sources of carbon (sucrose) and nitrogen (sodium nitrate), as well as an inducer (naringin) and pH levels were
all found to be the important factors significantly affecting naringinase production. In the second step, a 22 full factorial
central composite design was applied to determine the optimal levels of each of the significant variables. A second-order
polynomial was derived by multiple regression analysis on the experimental data. Using this methodology, the optimum values
for the critical components were obtained as follows: sucrose, 10.0%; sodium nitrate, 10.0%; pH 5.6; biomass concentration,
1.58%; and naringin, 0.50% (w/v), respectively. Under optimal conditions, the experimental naringinase production was 8.45 U/mL. The determination coefficients
(R
2) were 0.9908 and 0.9950 for naringinase activity and biomass production, respectively, indicating an adequate degree of reliability
in the model. 相似文献
950.
This paper describes the synthesis and characterization of aromatic diimide–diacids (DIDAS) obtained by reacting pyromellitic
dianhydride (PMDA), 4,4′-oxo diphthalic anhydride (ODA), 1,4,5,8-naphthalene tetra carboxylic dianhydride (NTDA) with excess
of 4-aminobutyric acid (B) or 6-aminohexanoic acid (H) using N,N-dimethyl formamide (DMF) as solvent. The synthesized compounds were used as curing agents to investigate the effect of structure
on the curing and thermal behaviour of diglycidyl ether of bisphenol-A (DGEBA). Structural characterization of DIDAS was done
by using FTIR, 1H-NMR, 13C-NMR spectroscopy and elemental analysis. Curing behaviour of DGEBA in the presence of aromatic DIDAS was investigated by
differential scanning calorimetry (DSC). The peak exotherm temperature (T
P) was low in the case of DIDAS synthesized from ODA and high in the case of DIDAS synthesized from NTDA. Thermal stability
of the isothermally cured DGEBA with DIDAS was investigated using dynamic thermogravimetry in nitrogen atmosphere. The char
yield was highest for resin cured with DIDAS containing NTDA. 相似文献