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A concise synthesis of pyrano[3,2‐e]indole alkaloid fontanesine B by a Fischer indolization is described. This key Fischer indolization starts with the pyran‐ring and alkene intact, facilitating potential synthetic applications. Furthermore, fontanesine B and its isomer were evaluated for in vitro antiproliferative activity against human colorectal cancer cells. The isomer of fontanesine B showed higher antiproliferative activity than the natural product, fontanesine B ( 2 ). 相似文献
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Design,synthesis, pharmacological evaluation and DNA interaction studies of binuclear Pt(II) complexes with pyrazolo[1,5‐a]pyrimidine scaffold 下载免费PDF全文
Miral V. Lunagariya Khyati P. Thakor Bhargav N. Waghela Chadramani Pathak Mohan N. Patel 《应用有机金属化学》2018,32(4)
Substituted pyrazolo[1,5‐a]pyrimidine ligands were synthesized by cyclization, using 3‐(thiophen‐2‐yl)‐1H‐pyrazol‐5‐amine with substituted enones (3‐phenyl‐1‐(pyridin‐2‐yl)prop‐2‐en‐1‐one) in presence of KOH and DMF as solvent to form cyclic aromatic compounds. The substituted pyrazolo[1,5‐a] pyrimidine based binuclear PtII complexes containing neutral tetradentated ligands have general formula [Pt2(5a–5f)Cl4], (where, (5a ‐5f) = pyrazolo[1,5‐a] pyrimidine ligand). This compounds were characterized by physicochemical and spectroscopic method like elemental analyses, UV‐Visible, FT‐IR, EDX, TGA, molar conductivity, magnetic susceptibility measurements, mass spectroscopy, 1H and 13C NMR method. The square planar geometry was predicted by electronic spectral study. All PtII compounds were evaluated by antimicrobial assay, in vitro brine shrimp assay, in vivo cellular level bioassay using S. Pombe cells and anti‐tuberculosis study. LC50 (50% lethal concentration) values of compounds are observed between 6.450 ‐ 102.07 μg/mL. UV‐vis absorption titration, competitive displacement assay, molecular docking and viscosity measurement were carried out to examine the binding type and binding strength of complexes. The binding studies suggest partial intercalative binding mode of the complexes and the observed binding constant (Kb) values are found in the order of 6d > 6b > 6c > 6a > 6e > 6 f. The anti‐proliferative cytotoxicity of the synthesized PtII complexes (6a‐6f) were tested against the HCT‐116 (Human Colorectal Carcinoma) cancer cell line. 相似文献
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Dr. Jeffrey L. Gustafson Dr. Taavi K. Neklesa Carly S. Cox Dr. Anke G. Roth Dr. Dennis L. Buckley Dr. Hyun Seop Tae Dr. Thomas B. Sundberg D. Blake Stagg Dr. John Hines Prof. Donald P. McDonnell Dr. John D. Norris Prof. Craig M. Crews 《Angewandte Chemie (International ed. in English)》2015,54(33):9659-9662
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Dr. Boris Gaillard Cendrine Seguin Dr. Jean-Serge Remy Prof. Dr. Françoise Pons Dr. Luc Lebeau 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(68):15662-15679
Sixteen cationic prodrugs of the antitumor alkylphospholipid (APL) erufosine were rationally synthesized to provide original gene delivery reagents with improved cytotoxicity profile. The DNA complexation properties of these cationic lipids were determined and associated transfection rates were measured. Furthermore, the self-assembly properties of the pro-erufosine compounds were investigated and their critical aggregation concentration was determined. Their hydrolytic stability under pH conditions mimicking the extracellular environment and the late endosome milieu was measured. Hemolytic activity and cytotoxicity of the compounds were investigated. The results obtained in various cell lines demonstrate that the prodrugs of erufosine display antineoplastic activity similar to that of the parent antitumor drug but are not associated with hemolytic toxicity, which is a dose-limiting side effect of APLs and a major obstacle to their use in anticancer therapeutic regimen. Furthermore, by using lipoplexes prepared from a prodrug of erufosine and a plasmid DNA encoding a pro-apoptotic protein (TRAIL), evidence was provided for selective cytotoxicity towards tumor cells while nontumor cells were resistant. This study demonstrates that the combination approach involving well tolerated erufosine cationic prodrugs and cancer gene therapy holds significant promise in tumor therapy. 相似文献
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Dienamine and Friedel–Crafts One‐Pot Synthesis,and Antitumor Evaluation of Diheteroarylalkanals 下载免费PDF全文
María Frías Dr. José M. Padrón Dr. José Alemán 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(22):8237-8241
An asymmetric synthesis of diheteroarylalkanals through one‐pot dienamine and Friedel–Crafts reaction is presented. The reaction tolerates a large variety of substituents at different positions of the starting aldehyde and also in the indole nucleophile, and a range of diheterocyclic alkanals can be achieved. Furthermore, we have studied the antiproliferative activity of these new compounds in representative cancer tumor cell lines. 相似文献
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Novel Composite Plastics Containing Silver(I) Acylpyrazolonato Additives Display Potent Antimicrobial Activity by Contact 下载免费PDF全文
Prof. Fabio Marchetti Dr. Jessica Palmucci Prof. Claudio Pettinari Dr. Riccardo Pettinari Dr. Francesca Condello Dr. Stefano Ferraro Dr. Mirko Marangoni Prof. Alessandra Crispini Dr. Stefania Scuri Prof. Iolanda Grappasonni Prof. Mario Cocchioni Dr. Massimo Nabissi Dr. Michele R. Chierotti Prof. Roberto Gobetto 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(2):836-850
New silver(I) acylpyrazolonato derivatives displaying a mononuclear, polynuclear, or ionic nature, as a function of the ancillary azole ligands used in the synthesis, have been fully characterized by thermal analysis, solution NMR spectroscopy, solid‐state IR and NMR spectroscopies, and X‐ray diffraction techniques. These derivatives have been embedded in polyethylene (PE) matrix, and the antimicrobial activity of the composite materials has been tested against three bacterial strains (E. coli, P. aeruginosa, and S. aureus): Most of the composites show antimicrobial action comparable to PE embedded with AgNO3. Tests by contact and release tests for specific migration of silver from PE composites clearly indicate that, at least in the case of the PE, for composites containing polynuclear silver(I) additives, the antimicrobial action is exerted by contact, without release of silver ions. Moreover, PE composites can be re‐used several times, displaying the same antimicrobial activity. Membrane permeabilization studies and induced reactive oxygen species (ROS) generation tests confirm the disorganization of bacterial cell membranes. The cytotoxic effect, evaluated in CD34+ cells by MTT (3‐(4,5‐dimethylthiazole‐2‐yl)‐2,5‐diphenyltetrazoliumbromide) and CFU (colony forming units) assays, indicates that the PE composites do not induce cytotoxicity in human cells. Studies of ecotoxicity, based on the test of Daphnia magna, confirm tolerability of the PE composites by higher organisms and exclude the release of Ag+ ions in sufficient amounts to affect water environment. 相似文献