共查询到20条相似文献,搜索用时 46 毫秒
1.
Ping Wang Stacy Ownby Zhizhen Zhang Wei Yuan Wanli Zhang R. Scott Beasley 《Phytochemistry》2009,70(3):430-436
Phytoecdysteroid glycosides (1-5) and a phenylpropanoid ester of sucrose (6) were isolated from the whole plant of Froelichia floridana, along with eight known compounds including three ecdysteroids (7-9), four flavonoids (10-13), and one phenolic compound (14). Structures were determined using a combination of spectroscopic techniques. Compounds 1, 2 and 6-14 were tested in vitro for their activity against human DNA topoisomerase I. Compound 13 (diosmetin) showed marginal inhibition against topoisomerase I with IC50 of 130 μM in conjunction with low intercalation ability. 相似文献
2.
In order to find potential anticancer drug candidate targeting topoisomerases enzyme, we have designed and synthesized oxiranylmethoxy- and thiiranylmethoxy-retrochalcone derivatives and evaluated their pharmacological activity including topoisomerases inhibitory and cytotoxic activity. Of the compounds prepared compound 25 showed comparable or better cytotoxic activity against cancer cell lines tested. Compound 25 inhibited MCF7 (IC50: 0.49 ± 0.21 μM) and HCT15 (IC50: 0.23 ± 0.02 μM) carcinoma cell growth more efficiently than references. In the topoisomerases inhibition test, all the compounds were inactive to topoisomerase I but moderate inhibitors to topoisomerase II enzyme. Especially, compound 25 inhibited topoisomerase II activity with comparable extent to etoposide at 100 μM concentrations. Correlation between cytotoxicity and topoisomerase II inhibitory activity implies that compound 25 can be a possible lead compound for anticancer drug impeding the topoisomerase II function. 相似文献
3.
Hai-Yan Tian Xiao-Qi Zhang Dong-Mei Zhang Ying Wang Jun-Shan Liu Wen-Cai Ye 《Steroids》2010,75(12):884-890
Six new bufadienolides (1-6) and two new C23 steroids (7 and 8), together with three known compounds (9-11) were isolated from the venom of Bufo bufo gargarizans. Their structures were elucidated by spectroscopic analysis and single-crystal X-ray diffraction. In vitro cytotoxicities of all compounds were evaluated in A549 cancer cell line. Compounds 2, 3 and 10 showed significant cytotoxic activities. 相似文献
4.
Marta Sobiesiak Agnieszka Mrozek Ingo-Peter Lorenz Urszula Krajewska 《Inorganica chimica acta》2010,363(10):2171-3244
1-Benzothiazol-2-yl-3,5-dimethyl-1H-pyrazole (1a) and 1-benzothiazol-2-yl-5-(2-hydroxyphenyl)-3-methyl-1H-pyrazole-4-carboxylic acid methyl ester (1b) were reacted with the hexahydrates of cobalt(II) chloride, cobalt(II) nitrate and cobalt(II) perchlorate to give the corresponding complexes 2a-4a and 2b-5b, respectively. Obtained compounds differ in coordination spheres of central atoms. The complex 2a includes a fivefold coordinated cobalt(II) ion, whereas 3a shows a distorted octahedral configuration around the cobalt(II) ion. All complexes were characterised by FTIR spectroscopy, MS and elemental analysis. The X-ray structures of 2a, 3a and 5b complexes were also solved. The cytotoxic properties of the ligand 1a and both series of Co(II) complexes were examined on human leukemia NALM-6 and HL-60 cells and melanoma WM-115 cells. The ligands, were found to have very low cytotoxicity. Complex 3b exhibited the highest cytotoxic activity with IC50 values in the range of 6.9-17.1 μM for three examined cell lines. 相似文献
5.
Peiju Yang Cui Zhang Xiao-Juan Yang Huai-Ming Hu Biao Wu 《Inorganica chimica acta》2009,362(1):89-3592
A series of nickel(II) and cobalt(II) complexes, NiX2L (X = Cl, Br; 1-6) and CoCl2L (7-9), with 2,9-diaryl-1,10-phenanthroline ligands (L1-L3) have been synthesized and characterized by elemental analysis, UV-Vis, IR spectroscopy, and X-ray crystal structural study (for 1, 4-7, 9). The solid-state structures of 1, 5-7 and 9 show four-coordinate, slightly flattened tetrahedral geometry at the Ni(II) or Co(II) center, while 4 is five-coordinated (square-pyramidal), containing a THF molecule as an auxiliary ligand. The title complexes (1-9) display good catalytic activities in ethylene oligomerization when activated with methylaluminoxane (MAO). While the Co(II) precatalysts produce primarily C4 isomers, the Ni(II) complexes give ethylene dimers and trimers at normal pressure. The activities and yields of linear α-olefins increase with increasing ethylene pressure for the Ni(II) complexes, leading to more high-molar-mass products (C8-C18). Complex 6 displays the best catalytic activity among the complexes studied (up to 1518 kg/mol[Ni] h at 10 atm). 相似文献
6.
The lithium β-diketiminate (1c, [Li{N(2,6-iPr2C6H3)C(Ph)CHC(tBu)NH}]2 represented as (LiL)2) reacted with 3d-metal (II) chlorides to afford the corresponding compounds (2-7). All metal compounds were fully characterized by elemental, spectroscopic analyses and the single-crystal X-ray diffraction. The coordination geometries around the metals are shown to be tetrahedral within the trinuclear Co2Li compound (2), planar in ML2 (M = Co, 3), pseudo-tetrahedral conformation in the ML2 with M as Mn (4), Fe (5) or Zn (6), and square planar in the dinickel compound (7). Indicated by the trimetallic Co2Li compound 2, a six-membered ring is constructed of three metal atoms and three bridged chlorides as a twisted conformation. An inversion center is present in the centroid of the Ni2Cl2 four-membered ring within compound 7. The plausible mechanism of forming ML2 was proposed through the chloro-bridged multinuclear compounds on the basis of isolated intermediates of trinuclear (2) and dinuclearic (7) compounds. Upon treatment with methylaluminoxane (MAO), the nickel compound 7 possessed good activity towards ethylene oligomerization, whereas the other metal compounds showed moderate activities towards ethylene polymerization. 相似文献
7.
Extraction of the leaves of Zanthoxylum ailanthoides Sieb. & Zucc. affords extracts and four isolated compounds which exhibit activities against leukemia cells. The chloroform-soluble fraction (ZAC) of the crude extract of this plant showed cytotoxic activity against human promyelocytic leukemia (HL-60) and myelomonocytic leukemia (WEHI-3) cells with IC50 values of 73.06 and 42.22 μg/mL, respectively. The active ZAC was further separated to yield pheophorbide-a methyl ester (1), pheophorbide-b methyl ester (2), 132-hydroxyl (132-S) pheophorbide-a methyl ester (3) and 132-hydroxyl (132-R) pheophorbide-b methyl ester (4) whose structures were confirmed by spectroscopic methods. Compounds 2-4 showed cytotoxic activities against both leukemia cells with IC50 value in the range of 46.76-79.43 nM, whereas compound 1 exhibited only weak cytotoxic activity. The extracts and compounds 1-4 also induced apoptosis and DNA damage in leukemia cells after treatment. The results suggested that the Z. ailanthoides is biologically active against leukemia cells. 相似文献
8.
Wing-Sze Lee Leung-Shi Cheng Chi-Sing Lee Wing-Tak Wong 《Inorganica chimica acta》2004,357(15):4389-4395
Chiral N,O pyridine alcohols HL1-HL6 were used to form complexes with copper(II) ions. Ligands HL1 and HL2 formed complexes with copper(II) ions when Cu(OAc)2 and HL were refluxed in methanol/ethanol mixture. Ligand HL3 formed a complex with copper(II) when deprotonated with NaH and stirred in a Cu(II) acetate THF solution. Ligands HL4-HL6 did not form complexes with copper(II) under similar conditions. Two complexes, [Cu(L1)2] and [Cu(L2)2], were isolated as single crystals and characterized by X-ray crystallography. These complexes showed low catalytic activities in asymmetric reactions. However, they became active when reacted with triflic acid. Copper complexes, [Cu(L)] or [Cu(L)]+, formed in situ by reacting ligands HL with copper(I) or (II) ions, respectively, were also found to be active copper catalysts for asymmetric cyclopropanation of styrene with ethyl diazoacetate and allylic oxidation of cyclohexene with t-butylperoxybenzoate. Enantioselectivities up to 56% and 38% were obtained in asymmetric cyclopropanation of styrene and asymmetric allylic oxidation of cyclohexene, respectively. 相似文献
9.
Daniel Pinheiro Maia Jair Mafezoli Manoel Odorico de Moraes Letícia Veras Costa-Lotufo 《Chemico-biological interactions》2009,180(2):220-1276
2-Azetidinones and 2H-azirines show antibacterial and cytotoxic activities, however the biological properties of molecules containing both 2H-azirine and 2-azetidinone functions in the same structure had never been evaluated before. In the present study, two 2H-azirine-2-azetidinones (1 and 2) and three 2H-azirines (3-5) were synthesized from 2-formyl-3-phenyl-2H-azirine-N-arylimines with diphenylketene. The compounds were assayed for antibacterial and cytotoxic activities. None of them showed antibacterial activity on the tested strains, but both 2H-azirine-2-azetidinones showed cytotoxicity against four tumor cell lines (HL-60, leukemia; HCT-8, colon cancer; MDA-MB-435, melanoma; and SF-295, CNS). The IC50 values of 1 ranged from 1.1 to 10.5 μM and from 3.8 to 26.6 μM for 2. The mechanism of cell growth inhibition of 1 and 2 towards HL-60 cell line was also investigated. Membrane damage, cell viability, DNA synthesis inhibition and morphological changes were evaluated. The preliminary findings suggested that 1 and 2 induce apoptosis. 相似文献
10.
A new easily synthetic route with a 96% yield of ligand 2-(3,5-diphenyl-1H-pyrazol-1-yl)ethanol (L) is obtained. The reactivity of L against Pd(II), Zn(II) and Cu(II) leads to [PdCl2(L)2] (1), [ZnCl2(L)] (2) and [CuCl(L′)]2 (3) (L′ is the ligand L without alcoholic proton), respectively. According to the different geometries imposed by the metallic centre and the capability of L to present various coordination links, it has been obtained complexes with square planar (1 and 3) or tetrahedral (2) geometry and different nuclearity: monomeric (1 and 2) or dimeric (3). Complete characterisation by analytical and spectroscopic methods, resolution of L and 1-3 by single-crystal X-ray diffraction and magnetic studies for complex 3 are presented. 相似文献
11.
A series of pyrazolyl palladium(II), platinum(II) and gold(III) complexes, [PdCl2(3,5-R2bpza)] {R = H (1), R = Me (2), bpza = bis-pyrazolyl acetic acid}, [PtCl2(3,5-R2bpza)] {R = H (3a), R = Me (4)}, [AuCl2(3,5-R2bpza)]Cl {R = H (5a), R = Me (6a)} and [PdCl2(3,5-R2bpzate)] {R = Me (7)} have been synthesised and structurally characterised. Single crystal X-ray crystallography showed that the pyrazolyl ligands exhibit N^N-coordination with the metals. Anticancer activities of six complexes 1-6a were investigated against CHO cells and were found to have low activities. Substitution reactions of selected complexes 1, 2, 3a and 5a with l-cysteine show that the low anticancer activities compounds and that the rate of substitution with sulfur-containing compounds is not the cause of the low anticancer activities. 相似文献
12.
Sumanta Kumar Padhi 《Inorganica chimica acta》2011,372(1):383-388
Compounds of the molecular formulae, [LH3](NO3)3 (1), [Fe(LH)2](PF6)4·5H2O (2), [Fe(L)2][Fe(L)(LH)](PF6)5·H2O (3), [Fe(L)2][Fe(L)(LH)](BF4)5·2H2O (4) and [Fe(L)2](Cr2O7)·6H2O (5) have been synthesized using 4′-(2-pyridyl)-2,2′:6′,2″-terpyridine (L). The molecular structures of all the compounds were determined. The Fe(II) complexes are high spin in nature at room temperature and upon cooling a gradual spin-transition is observed. Among 1-5, hydrogen-bonding, π···π, and anion···π interactions as well as water tetramer and pentamer are present in the molecular packing. 相似文献
13.
Takumi Higa Yuichi Shimazaki Tatsuo Yajima Satoru Karasawa Yoshinori Naruta 《Inorganica chimica acta》2007,360(10):3304-3313
Copper(II) complexes of N4-donor ligands containing imidazole moieties, 4-[bis(1-methylimidazole-2-yl-methyl)aminomethyl]imidazole (Him-im2) and 4-[bis(1-methylimidazole-2-yl-methyl)aminoethyl]imidazole (Hhis-im2), were prepared, and [Cu(Him-im2)Cl]ClO4 (1) and [Cu(Hhis-im2)Cl]ClO4 (2) were structurally characterized by the X-ray diffraction method. Complexes 1 and 2 have a mononuclear structure with a coordinated chloride ion. The geometry of the Cu(II) center in 1 was found to be 5-coordinate trigonal-bipyramidal, whereas that of 2 was square-pyramidal. Complexes 1 and 2 showed different absorption and EPR spectra in MeOH, indicating that these compounds in solution maintain the structures revealed in the solid state. On the other hand, the reaction of Him-im2 with Cu(ClO4)2 · 6H2O under basic conditions gave a tetranuclear Cu(II) complex, [Cu4(im-im2)4](ClO4)4 (3), whereas using the ligand Hhis-im2 gave two kinds of polynuclear complexes [Cu4(his-im2)4](ClO4)4 (4) and [Cu6(his-im2)6](ClO4)6 (5) exhibiting discretely different structures. X-ray crystal structure analysis of the polynuclear complexes revealed their cyclic structures bridged by the imidazolate moiety. The geometry difference of the Cu(II) centers between 1 and 2 is thus concluded to determine the structures of tetranuclear complexes 3 and 4, respectively. Temperature dependent magnetic susceptibility measurements of complexes 3, 4, and 5 have shown an antiferromagnetic exchange interaction with a coupling constant of J = −32.5, −27.1 and −22.8 cm−1, respectively. 相似文献
14.
The novel triphenyltin(IV) esters of flufenamic acid (1), Hflu, [Ph3Sn(flu)] (2), and of [2-(2,3-dichlorophenylamino)benzoic acid] (3), Hdcpa, [Ph3Sn(dcpa)] (4) have been structurally characterized by means of vibrational and 1H, 13C NMR spectroscopic studies. The crystal and molecular structures of [SnPh3(dcpa)(DMSO)] 4a are described. The molecular structure of 4a reveals that the Sn atom has a distorted trigonal bipyramidal coordination geometry with equatorial phenyl groups and the carboxylate and dimethylsulfoxide oxygen atoms occupying axial positions. The crystal structure of 4a is self-assembled by C-H---π and π-π stacking interactions. The in vitro cytotoxic activity of 1-4 and of the related non-steroidal anti-inflammatory drugs, NSAIDs, [2-(2,6-dimethylphenylamino)benzoic acid], Hdmpa (5), [Ph3Sn(dmpa)] (6), [2-(2,3-dimethylphenylamino)benzoic acid], mefenamic acid, Hmef (7) and [Ph3Sn(mef)] (8) has been evaluated against the cancer cell lines MCF-7, T-24, A-549 and L-929. The ligands exhibited very poor cytotoxic activity against the four cancer cell lines. Complex 6 exhibits the highest activity and selectivity against A-549 and MCF-7 cancer cell lines and complex 8 the highest activity and selectivity against T-24 cancer cell line. The cytotoxic results indicate that coupling of Hdmpa and Hmef with R3Sn(IV) metal center results in complexes with important biological properties and remarkable cytotoxic activity, since they display IC50 values in a μΜ range better to that of the antitumor drug cis-platin. Complexes 6 and 8 are considered as excellent antitumor compounds and the results of this study represent the discovery of triphenyltin(IV)esters as a potential novel class of anticancer agents. 相似文献
15.
Mauro Ghedini Massimo La Deda Iolinda Aiello Annarita Grisolia 《Inorganica chimica acta》2004,357(1):33-40
New series of 5-substituted-8-hydroxyquinolines HLn (1-6) bearing aliphatic or aromatic amido groups were synthesised. The chelating ability of these ligands toward the zinc(II) ion was tested and the photophysical characterisation of the resulting complexes (ZnLn)2 · 2H2O (7-12) is reported and compared to those of the uncomplexed ligands. The photophysical data of 1-6 revealed interesting differences between aliphatic (1-3) and aromatic (4-6) amido-substituted species which, however, are no longer evident upon metal complexation. In fact while the ligands 1-3 showed a very high quantum yield (2, λem=470 nm; Φ=0.22) higher than that of the unsubstituted HQ compound, the ligands 4-6 displayed low quantum yield, similar to that of the complexes 7-12, which was in turn lower than that of ZnQ2·2H2O. The behaviour of these compounds is discussed with particular reference to the possibility of controlling the photophysical properties of such compounds through selective modification of the amido substituents. 相似文献
16.
Zhao JM Li N Zhang H Wu CF Piao HR Zhao YQ 《Bioorganic & medicinal chemistry letters》2011,21(3):1027-1031
Three new dammarane-type sapogenins (1, 3, and 5) together with two known ones (2 and 4) were isolated from the total hydrolyzed saponins extracted from Panax ginseng berry. Their structures were elucidated using a combination of 1D and 2D 1H and 13C NMR spectra and mass spectroscopy as 20(R)-25-methoxyl-dammarane-3β,12β,20-triol (1), 20(R)-25-methoxyl-dammarane-3β,6α,12β,20-tetrol (2), 20(R)-20-methoxyl-dammarane-3β,12β,25-triol (3), 20(R)-20,25-dimethoxyl-dammarane-3β,12β-diol (4), and (12R,20S,24S)-20,24-; 12,24-diepoxy-dammarane-3β-ol (5). Their antitumor activities were evaluated in six human cancer cell lines. The novel compounds 1 and 3 showed significant cytotoxic activity against the six cell lines. The IC50 values of 3 against HepG2, Colon205, and HL-60 were the lowest (8.78, 8.64, and 3.98 μM, respectively). Compounds 1 and 20(S)-25-OCH3-PPD, which are a pair of configuration isomers, showed a 10- to 100-fold greater growth inhibition than ginsenoside-Rg3 (an anti-cancer clinical agent in China). The data presented here may be useful for the development of novel anti-cancer agents. 相似文献
17.
Xian-He Bu He LiuMiao Du Keith Man-Chung WongVivian Wing-Wah Yam 《Inorganica chimica acta》2002,333(1):32-40
The complexes of Cu(I), Cu(II), Ni(II), Zn(II) and Co(II) with a new polypyridyl ligand, 2,3-bis(2-pyridyl)-5,8-dimethoxyquinoxaline (L), have been synthesized and characterized. The crystal structures of these complexes have been elucidated by X-ray diffraction analyses and three types of coordination modes for L were found to exist in them. In the dinuclear complex [Cu(I)L(CH3CN)]2·(ClO4)2 (1), L acts as a tridentate ligand with two Cu(I) centers bridged by two L ligands to form a box-like dimeric structure, in which each Cu(I) ion is penta-coordinated with three nitrogen atoms and a methoxyl oxygen atom of two L ligands, and an acetonitrile. In [Cu(II)L(NO3)2]·CH3CN 2, the Cu(II) center is coordinated to the two nitrogen atoms of the two pyridine rings of L which acts as a bidentate ligand. The structures of [Ni(II)L(NO3)(H2O)2]·2CH3CN·NO3 (3), [Zn(II)L(NO3)2 (H2O)]·2CH3CN (4) and [Co(II)LCl2(H2O)] (5) are similar to each other in which L acts as a tridentate ligand by using its half side, and the metal centers are coordinated to a methoxyl oxygen atom and two bipyridine nitrogen atoms of L in the same side. The formation of infinite quasi-one-dimensional chains (1, 4 and 5) or a quasi-two-dimensional sheet (2) assisted by the intra- or intermolecular face-to-face aryl stacking interactions and hydrogen bonds may have stabilized the crystals of these complexes. Luminescence studies showed that 1 exhibits broad, structureless emissions at 420 nm in the solid state and at 450 nm in frozen alcohol frozen glasses at 77 K. Cyclic voltammetric studies of 1 show the presence of an irreversible metal-centered reduction wave at approximately −0.973 V versus Fc+/0 and a quasi-reversible ligand-centered reduction couple at approximately −1.996 V versus Fc+/0. The solution behaviors of these complexes have been further studied by UV-Vis and ESR techniques. 相似文献
18.
19.
Two new spirostanoides, filiasparosides E (1) and F (2), one new furostanoside, filiasparoside G (3), and one new ecdysterone, stachysterone A-20, 22-acetonide (4), together with six known steroidal saponins, asparagusin A (5), filiasparoside A (6), filiasparoside B (7), aspafilioside A (8), aspafilioside B (9), and filiasparoside C (10) were isolated from the roots of Asparagus filicinus Buch.-Ham. Their structures were elucidated on the basis of spectroscopic and chemical evidence. Compounds 1-10 were investigated for their cytotoxicities against human breast adenocarcinoma MDA-MB-231 cell line and compounds 8-10 exhibited cytotoxic activities with IC50 values ranging from 3.4 to 6.6 μM. 相似文献
20.
Sun YJ Li ZL Chen H Liu XQ Zhou W Hua HM 《Bioorganic & medicinal chemistry letters》2011,21(12):3794-3797
Three new aryltetralin lignans, 4-acetyl-4-demethyl-podophyllotoxin (1) and sinolignans A, B (2-3), and two new natural products (4-5), were isolated from the roots and rhizomes of Sinopodophyllum emodi together with twelve known lignans (6-17). Their structures and stereochemistry were elucidated on the basis of spectroscopic evidence, and circular dichroism (CD) method. The cytotoxic activities of all isolated compounds were evaluated against HeLa and KB cell lines. Compared with etoposide, compounds 1, 6-9, and 13 showed more potent cytotoxicities against two tumor cell lines. On the basis of IC50 values, deoxypodophyllotoxin (7) was about 579 and 1123 times more toxic than etoposide in HeLa and KB cell lines, respectively. The preliminary SAR study indicated that an oxygenated group at C-7′ might decrease cytotoxicity against two cell lines, which was different from most previous studies. However, this needs to be systematically verified by extensive pharmacological experiments. 相似文献