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1.
New glycosyl derived ligand and its complexes, with SnCl4·5H2O (1) and (CH3)2SnCl2(2) were synthesized and characterized by spectroscopic (IR, 1H, 13C, and 119Sn NMR, UV-vis, ESI-MS) and analytical methods. Interaction studies of 1 and 2 with CT DNA were studied by using various biophysical techniques, which showed high binding affinity of 2 with CT DNA. In vitro cytotoxicity of complexes 1 and 2 were evaluated against different human cancer cell lines of different histological origins by employing SRB Assay. The organotin(IV) complex 2 exhibited remarkable activity against DWD (oral cancer) cell lines with GI50 values <10 μg/ml. Complex 2 induced apoptosis of DWD cell line at a very low concentration of 1-4 μg/mL.  相似文献   

2.
Five new polyketide derivatives, 6′-hydroxypestalotiopsone C (1), acropyrone (2), bicytosporone D (3), waol acid (4), and pestalotiopene C (5), together with seven known metabolites (612), were obtained from extracts of the endophytic fungus Acremonium strictum, isolated from the mangrove tree Rhizophora apiculata. The structures of the isolated compounds were elucidated on the basis of comprehensive NMR and MS analysis. Compounds 6, 7, and 9 showed moderate cytotoxic activity against human cisplatin-sensitive (IC50 values 27.1, 76.2, and 8.3 μM, respectively) and resistant A2780 cell lines (IC50 values 12.6, 30.1, and 19.0 μM, respectively), whereas only 9 exhibited antibacterial activity against Staphylococcus aureus (MIC value 14.3 μM).  相似文献   

3.
The titanocene complexes [TiCp2(Cl)R] (1), [TiCp2(Cl)SR] (2), [TiCp2(SR)2] (3) with R = benzothienyl (BT) A and dibenzothienyl (DBT) B, were synthesized and the molecular structures of [TiCp2(Cl)DBT] (1B) and [TiCp2(Cl)SDBT] (2B) confirmed by single crystal X-ray diffraction studies. The dibenzothiophene rings are planar and for 1B in the plane of the titanium and chloro ligand. The chloro ligand is in a trans position to the sulfur atom with respect to the titanium-carbon bond. The complexes were studied for their electronic and structural features and preliminary tests were conducted for their tumor inhibiting properties against HeLa and COLO 320M tumor cell lines. These antitumor activities were compared against those observed for titanocene dichloride (S-01) under similar conditions and the highest antitumor activity was recorded for 2B.  相似文献   

4.
New palladium(II) and platinum(II) complexes containing bis(2-pyridylmethyl)amine (bpma) and saccharinate (sac), [Pd(bpma)(sac)](sac)·2H2O (1), [Pt(bpma)(sac)](sac)·2H2O (2), [Pd(bpma)Cl](sac)·2H2O (3) and [Pt(bpma)(sac)]Cl·1.5H2O (4), were synthesized and characterized by elemental analysis, IR, NMR and TG-DTA. A single-crystal X-ray analysis of 3 and 4 proved a distorted square-planar geometry around the metal ions with one tridentate bpma ligand and one Cl or sac monoanion. The [Pd(bpma)Cl]+ ions in 3 form dimers by intermolecular N-H?Cl and Pd?Pd interactions. The cations reside in the centers of a hydrogen-bonded honeycomb network formed by the uncoordinated sac ions and the lattice water molecules, while the cations of 4 are connected by N-H?Cl and OW-H?O hydrogen bonds into one-dimensional chains. Cyclic planar tetrameric and trimeric water clusters were observed in 3 and 4, respectively. Cytotoxicity of 1-4 was tested against A549, C6 and CHO cells. Although 2 and 4 have no cytotoxicity, the best results were achieved for 1 and 3. In particular, the cyctotoxic activity of 3 is comparable to cisplatin.  相似文献   

5.
The copper(I) catalyzed cycloaddition reaction of N-Boc propargyl amine (dipolarophile) 1 with benzyl azide (1,3-dipole) 2 was found to proceed smoothly in t-BuOH/H2O at room temperature, to furnish the corresponding 1,4-disubstituted-[1,2,3]-triazole-derived N-Boc amine 3 in good yield. Deprotection of 3 with trifluoroacetic acid and addition of the trifluoroacetate salt 4 in the presence of triethylamine, with a series of methoxyvinyl(trifluoromethyl)ketones 10-14, gave the corresponding β-aminovinyl trifluoromethylated ketones 15-19 in moderate to good yields. Two copper(II) complexes, one monomer and one dimer with chlorine double bridge, 20 and 21, respectively, were also prepared and their crystal structure determined. β-Aminovinyl trifluoromethylated ketones 15-17 and complexes 20 and 21 have been screened as potential antifungal agents and the antimalarial activity of 15 and 16 were tested against two Plasmodium falciparum strains (3D7 and W2).  相似文献   

6.
Three new sulfur-containing alkaloids, polycarpaurines A (1), B (2), and C (3) were isolated from the tropical ascidian Polycarpa aurata collected in Indonesia, together with six known compounds (4-9). The structures of new compounds were assigned on the basis of their spectral data. Compounds 1, 3, 4, and 8 inhibited colony formation of Chinese hamster V79 cells with EC50 values of 6.8, 8.6, 3.8, and 10 μM, respectively. Compounds 2 and 7 showed modest activity against V79 cells (EC50>10 μM).  相似文献   

7.
Xing-Yun Chai 《Tetrahedron》2008,64(24):5743-5747
Four rare isoryanodane diterpenoids namely itols A-D (1-4) and two isoryanodane glucosides (5 and 6) were isolated from the bark and twigs of Itoa orientalis. Their structures were determined by NMR and MS techniques and the structure of 1 was confirmed by a single-crystal X-ray diffraction. These six diterpenoids obviously showed insecticidal activity against Spodoptera exigua, with LC50 28.62 ppm for 1 and 52.76 ppm for 2, respectively. In anti-inflammatory assay, compounds 1 and 4-6 showed anti-COX-2 activity, with inhibitory rates of 54.7-78.3% at 10 μM.  相似文献   

8.
Six new guignardins A–F (16) were isolated from the cultures of endophytic fungus Guignardia sp. KcF8 derived of a mangrove plant Kandelia candel, along with three known analogues, palmarumycins C1 (7), BG1 (8), and JC1 (9). Compounds 2, 3, 7, and 8 showed antimicrobial activities. Compounds 57 exhibited significant cytotoxicities against 10 human tumor cell lines. Compound 3 also displayed significant inhibitory activity against human protein tyrosine phosphatase 1B and histone deacetylase silent information regulator T1enzymes, two key targets for the treatment of diabetes. This is the first report on the anti-PTP1B and anti-SIRT1 activities of spirodioxynaphthalenes.  相似文献   

9.
Two novel chlorinated sorbicillinoids named chloctanspirones A (1) and B (2), possessing an unprecedented bicyclo[2.2.2]octane-2-spiro cyclohexane skeleton, together with their quasi-precursors terrestrols K (3) and L (4), two additional new chlorinated compounds, were isolated from a marine sediment derived fungus Penicillium terrestre. Their structures including absolute stereochemistries were elucidated by analysis of NMR, MS data, and TDDFT CD calculations. The cytotoxic effects of 1-4 were preliminarily evaluated in HL-60 and A-549 cells. Compound 1 was active against both HL-60 and A-549 cells with IC50s 9.2 and 39.7 μM, respectively, while 2 showed weaker activity only against HL-60 cells (IC50 37.8 μM).  相似文献   

10.
We report the synthesis, characterization, and cytotoxic and antimalarial activity of ferrocene-indole hybrids 8-14. The 2-phenylindole scaffold was chosen because of its potent antimitotic activity and ferrocene was chosen following the development of ferrocifens, ferrocene derivatives of tamoxifen, which are prototypes of a new family of organometallic anti-estrogens. Ferrocene-indole hybrids 8-14 and their corresponding organic analogues 1-7 showed only moderate antimalarial activities, while ferrocene-indole hybrids 11 and 12 showed excellent in vitro activities against the A549 human carcinoma cell line, with IC50 values of 5 and 7 μM respectively. These ferrocene-indole hybrids were up to 25-fold more potent as cytotoxic agents than their purely organic analogues.  相似文献   

11.
The reactions of hexachlorocyclotriphosphazatriene, N3P3Cl6, with N-alkyl-N-ferrocenylmethylethylene diamines, FcCH2NH(CH2)2NHR1 [R1 = Me (1) and Et (2)], and sodium [3-(N-ferrocenylmethylamino)-1-propanoxide] (3) produce spirocyclic monoferrocenyl tetrachlorophosphazenes (1a3a). The tetrapyrrolidinophosphazenes (1b3b) are prepared from the reactions of corresponding phosphazenes (1a3a) with excess pyrrolidine. The reaction of 1a with excess morpholine affords geminal-morpholino phosphazene (1c), whilst the reactions of 2a and 3a give diethylaminotrimorpholino (2c) and fully substituted morpholino products (3c), respectively. The structural investigations of the compounds are examined by Fourier transform IR, MS, 1H, 13C, 31P NMR, DEPT, HETCOR, and HMBC techniques. The crystal structures of 3b and 3c are determined using X-ray crystallography. Cyclic voltammetric and chronoamperometric data show that compounds 1a3a, 1b3b, and 1c3c exhibit electrochemically reversible one-electron oxidation of Fc redox centers which are hardly affected by the substituents on the phosphazene ring. The compounds 1b, 2b, 3b, and 3c are screened for antibacterial activities against Gram-positive and Gram-negative bacteria and for antifungal activities against yeast strains. In addition, the antituberculosis activities (in vitro) of these compounds are evaluated against INH-susceptible reference strain M. tuberculosis H37Rv, and six multi-drug resistant clinical M. tuberculosis isolates. Compound 2b is found to be the most active against the susceptible the reference strain. In addition, 1b, 2b, and 3c are active against all the multidrug-resistant clinical isolates at the highest concentrations. Gel electrophoresis data indicate that the compounds promote the formation of strand breaks in plasmid DNA. Almost all the concentrations lost of supercoiled DNA suggests that the compound 3b is very efficient plasmid-modifier. The compounds inhibit BamHI cleavage of pUC18 DNA while restricting HindIII.  相似文献   

12.
Four new compounds, two lignans; lucidenal and lucidanin (1 and 2), one alkaloid (3), and one flavanone (4) together with 26 known compounds (530), were isolated from the twigs of Feroniella lucida. The structures of the new compounds were determined on the basis of spectroscopic analyses. Lucidenal 1 showed cytotoxicity against HuCCA-1, A549, MOLT-3 and HepG2 cancer cell lines with IC50 values of 4.27, 9.59, 2.31, and 6.50 μg/mL, respectively. A plausible biosynthetic pathway of 1 was proposed.  相似文献   

13.
The reactions of hexachlorocyclotriphosphazene, N3P3Cl6, with mono (1 and 2) and bis(4-fluorobenzyl) diamines (3-5), FPhCH2NH(CH2)nNHR (RH or FPhCH2-), produce mono (1a and 2a) and bis(4-fluorobenzyl) monospirocyclophosphazenes (3a-5a). The tetraaminomonospirocyclophosphazenes (1b-2d) are obtained from the reactions of the partly substituted phosphazenes (1a and 2a) with excess pyrrolidine, morpholine and 1,4-dioxa-8-azaspiro[4,5]decane (DASD), respectively. The tetrachlorobis(4-fluorobenzyl) monospirocyclophosphazenes (4a and 5a) with excess pyrrolidine, morpholine and DASD afford the fully substituted bis(4-fluorobenzyl) monospirocyclophosphazenes (4b, 4d-5d) in boiling THF. In addition, monochlorobis(4-fluorobenzyl) monospirocyclophosphazenes (4e and 4f) have also been isolated from the reactions with excess morpholine and DASD in boiling THF. The structural investigations of the compounds have been verified by elemental analyses, MS, FTIR, 1H, 13C, 19F (for 1d and 2d), 31P NMR, HSQC and HMBC techniques. The crystal structures of 3a, 4a, 5a and 2b have been determined by X-ray crystallography. The compounds 2a-5a, 1b-2d, 4b, 4d-5d, 4e and 4f have been screened for antibacterial effects on bacteria and for antifungal activity against yeast strains. The compounds 1b and 4b showed antimicrobial activity against three species of bacteria, Bacillus subtilis, Bacillus cereus and Staphylococcus aureus, and two fungi, Candida albicans and Candida tropicalis. Minimum inhibitory concentrations (MIC) were determined for 1b and 4b. The MIC values were found to be 5000 μM for each bacteria. The most effective compound, 4b has exhibited activity with a MIC of 312 μM for C. albicans and 625 μM for C. tropicalis. DNA-binding and the nature of the interaction with pBR322 plasmid DNA are studied. All of the compounds induce changes on the DNA mobility and intensity. Prevention of HindIII digestion with the compounds indicates that the compounds bind with AT nucleotides in DNA.  相似文献   

14.
A novel C-27 norwithasteroid, withaphysanolide A (1) containing a pyran ring was isolated from the aerial parts of Physalis divericata. Four known withaphysalins (2-5) and five physalins (6-10) were also isolated. The structural assignment for 1 was done based on spectroscopic and single-crystal X-ray diffraction data. Logical biosynthetic pathways were postulated. Compounds 6, 7, and 10 displayed potent cytotoxic activity against HCT-116 and H460 human cancer cell lines, with IC50 values less than 2.0 μM.  相似文献   

15.
16.
Two novel diterpenoids, luanchunins A (1) and B (2), along with their precursor, kamebakaurin (3), had been isolated from the stems and leaves of Isodon rubescens var. lushanensis. Their structures were elucidated on the basis of extensive spectroscopic analyses. Compounds 1 and 2 showed potent cytotoxic activity against HL-60 with IC50 values of 4.81 μM and 3.52 μM, respectively. Plausible pathways for the biosynthesis of 1 and 2 were also postulated.  相似文献   

17.
Seven new diterpenes, jiadifenoic acids J–P (17), two new sesquicarane sesquiterpenes, sesquicaranoic acids A and B (8 and 9), and four known compounds, were isolated from the stems of Illicium jiadifengpi. The trans-fused A/B ring junction in diterpenes was deduced from NMR data analysis and confirmed by single-crystal X-ray crystallography of 3. The absolute configurations of compounds 1 and 5 were determined using the Mo2(OAc)4-induced circular dichroism (ICD) method. Compounds 8 and 9 are a pair of C-10 epimers, and their absolute configurations were confirmed by analyzing their CD and ICD data. All of the isolated compounds were evaluated in vitro for their antiviral activities against Coxsackie virus B3 (CVB3). Among the isolated compounds, 4, 5, 7, 10, and 11 exhibited reasonable activity against CVB3, with IC50 values of 7.0–22.2 μmol/mL and selective index values (SI=TC50/IC50) of 49.3, 37.1, 31.3, 45.6 and 40.9, respectively.  相似文献   

18.
A series of aluminum and zinc complexes supported by functionalized phenolate ligands were synthesized and characterized. Reaction of 2-(3,5-R2C3N2)C6H4NH2 (R = Me, Ph) with salicylaldehyde or 3,5-di-tert-butylsalicylaldehyde afforded 2-((2-(1H-pyrazol-1-yl)phenylimino)methyl)phenol derivatives 2a-2d. Treatment of 2a-2d with an equiv. of AlR23 (R2 = Me, Et) gave corresponding aluminum aryloxides 3a-3e, while reaction with an equiv. of ZnEt2 afforded zinc aryloxides 4a-4d. Treatment of 2c with 0.5 equiv. of ZnEt2 formed diphenolato zinc complex 5. All new compounds were characterized by 1H and 13C NMR spectroscopy and elemental analyses. The structures of complexes 3a, 4a and 5 were further characterized by single crystal X-ray diffraction techniques. The catalytic activity of complexes 3-5 toward the ring-opening polymerization of ε-caprolactone was studied. The zinc complexes (4a-4d) exhibited higher catalytic activity than the aluminum complexes (3a-3e). The diphenolato zinc complex 5 showed lower catalytic activity than the ethylzinc complexes 4a-4d. The aluminum complex (3b) is inactive to initiate the ROP of rac-lactide, while the zinc complex (4d) is active initiator for the ROP of rac-lactide, giving atactic polylactide.  相似文献   

19.
The new ligands 2-(1-pyrazolil)-1,3-thiazine (PzTz), 2-(3,5-dimethyl-1-pyrazolil)-1,3-thiazine (DMPzTz) and 2-(3,5-diphenyl-1-pyrazolil)-1,3-thiazine (DPhPzTz) and the complexes [ZnCl2(H2O)(PzTz)] (1), [ZnCl2(DMPzTz)] (2) and [ZnCl2(DPhPzTz)] (3) have been isolated and then characterized by elemental analysis, IR spectra and UV-Vis spectroscopy. Besides, the crystal structure of ligands PzTz and DPhPzTz and complexes 1-3 have been determined by single-crystal X-ray diffraction. In 1, the geometry around the Zn(II) atom can be considered a highly distorted trigonal bipyramid, with the metallic atom bonded to two chlorine atoms, one water molecule and one bidentate PzTz ligand. In 2 and 3, the environment around the metal ion can be described as a distorted tetrahedron with the zinc atom coordinated to one bidentate organic ligand molecule and two chloro ligands. In addition, the phagocytic function of human neutrophils treated with complexes 1-3, their organic ligands and ZnCl2 has been evaluated. The activity of cells enhanced in samples treated with 1, 2 and 3 with respect to the ones to which the inorganic salt, PzTz, DMPzTz or DPhPzTz were added.  相似文献   

20.
Competitive oxidative chlorination of p-substituted triarylstibines 3 [(p-XC6H4)3Sb; a: X = OMe, c: Cl, d: CO2Et, e: CF3, f: CN, g: NO2] by sulfuryl chloride was carried out against 3b (X = H) and the electronic effect of these substituents on the chlorination of 3 was compared with that of homologous triarylbismuthanes 1. The relative ratios 4/4b (Ar3SbCl2/Ph3SbCl2) decreased with increasing electron-withdrawing ability of the substituents (a: 53/47, c: 49/51, d: 46/54, e: 44/56, f: 40/60, g: 37/63), but the tendency was not so pronounced as observed in the chlorination of 1. A Hammett plot of the 4/4b ratios against the σp constants exhibited a good linear relationship with a negative slope, the value of which was almost half of that deduced from the 2/2b (Ar3BiCl2/Ph3BiCl2) ratios. The difference in the reactivity between 1 and 3 may be explained by the effect of the electron-withdrawing substituents in the aromatic rings, which affects the p-character of the lone pair on the pnictogen atoms by increasing the positive metal charge and appears more remarkably in 1 than in 3. The 13C NMR study of 3 revealed that the chemical shifts of the ipso carbons (C1) attached to the antimony show a linear relationship against the σp constants with a positive slope (14.5). The value was smaller than that deduced from 1 (17.0), suggesting that the antimony center of 3 is less sensitive to the substituent effect. This is in accord with the tendency of the chlorination.  相似文献   

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