Novel Achiral Aryl-Substituted Vanadocenes: Synthesisand Preliminary Cytotoxicity Studies

2010 ◽  
Vol 63 (11) ◽  
pp. 1514 ◽  
Author(s):  
Brendan Gleeson ◽  
Anthony Deally ◽  
Helge Müller-Bunz ◽  
Siddappa Patil ◽  
Matthias Tacke
Keyword(s):  
Single Crystal ◽  
Renal Cell ◽  
In Vitro Testing ◽  
X Ray Diffraction ◽  
X Ray ◽  
Cytotoxicity Studies ◽  
Ic50 Values ◽  
Renal Cell Line ◽  
Vanadocene Dichloride

From the reaction of 6‐(4‐methoxymethyl‐phenyl) fulvene (1a), 6‐(N‐methyl‐pyrrole) fulvene (1b), and 6‐(4‐dimethylamino‐phenyl) fulvene (1c) with LiBEt3H, the corresponding lithium cyclopentadienide intermediates (2a–c) were synthesized. These intermediates were then transmetallated to vanadium with VCl4 to yield the substituted vanadocene dichlorides bis‐[(4‐methoxymethyl‐benzyl)cyclopentadienyl] vanadium(iv) dichloride (3a), bis‐[(N‐methylpyrrole)2‐methylcyclopentadienyl] vanadium(iv) dichloride (3b), and bis‐[(p‐dimethylaminobenzyl)cyclopentadienyl] vanadium(iv) dichloride (3c). The vanadocene dichloride 3a was characterized by single crystal X‐ray diffraction. All three vanadocenes had their cytotoxicity investigated through MTT based preliminary in vitro testing on the human renal cell line Caki‐1 in order to determine their IC50 values. Vanadocenes 3a–b were found to have IC50 values of 6.5 and 5.2 µM, respectively, while 3c displayed a superior value of 1.7 µM.

scholarly journals Secondary Metabolites with α-Glucosidase Inhibitory Activity from the Mangrove Fungus Mycosphaerella sp. SYSU-DZG01

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 483 ◽  
Author(s):  
Pei Qiu ◽  
Zhaoming Liu ◽  
Yan Chen ◽  
Runlin Cai ◽  
Guangying Chen ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Secondary Metabolites ◽  
Single Crystal ◽  
Absolute Configuration ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
X Ray Diffraction ◽  
X Ray ◽  
Ic50 Values ◽  
New Metabolites

Four new metabolites, asperchalasine I (1), dibefurin B (2) and two epicoccine derivatives (3 and 4), together with seven known compounds (5–11) were isolated from a mangrove fungus Mycosphaerella sp. SYSU-DZG01. The structures of compounds 1–4 were established from extensive spectroscopic data and HRESIMS analysis. The absolute configuration of 1 was deduced by comparison of ECD data with that of a known structure. The stereostructures of 2–4 were further confirmed by single-crystal X-ray diffraction. Compounds 1, 8 and 9 exhibited significant α-glucosidase inhibitory activity with IC50 values of 17.1, 26.7 and 15.7 μM, respectively. Compounds 1, 4, 6 and 8 showed antioxidant activity by scavenging DPPH· with EC50 values ranging from 16.3 to 85.8 μM.

scholarly journals Anti-inflammatory Anthraquinones from the Crinoid Himerometra magnipinna

2015 ◽  
Vol 10 (2) ◽  
pp. 1934578X1501000
Author(s):  
Yen-You Lin ◽  
Su-June Tsai ◽  
Michael Y. Chiang ◽  
Zhi-Hong Wen ◽  
Jui-Hsin Su
Keyword(s):  
Single Crystal ◽  
Diffraction Analysis ◽  
Absolute Configuration ◽  
Spectroscopic Data ◽  
Test Compound ◽  
X Ray Diffraction ◽  
X Ray ◽  
Anti Inflammatory ◽  
Raw264.7 Macrophage

Chemical investigation of a crinoid Himerometra magnipinna has afforded three anthraquinones (1–3), including one new metabolite, (+)-rhodoptilometrin (1). The structures of these compounds were elucidated on the basis of their spectroscopic data and the absolute configuration of 1 was further confirmed by single-crystal X-ray diffraction analysis. In the in vitro anti-inflammatory effects test, compound 2 was found to significantly inhibit the accumulation of the pro-inflammatory iNOS protein of the LPS-stimulated RAW264.7 macrophage cells.

Synthesis, characterization, X-ray diffraction, antimicrobial and in vitro cytotoxicity studies of 7a-Aza-B-homostigmast-5-eno [7a,7-d] tetrazole

2013 ◽  
Vol 16 (3) ◽  
pp. 201-206 ◽  
Author(s):  
Mahboob Alam ◽  
Shahab A.A. Nami ◽  
Ahmad Husain ◽  
Dong-Ung Lee ◽  
Soonheum Park
Keyword(s):  
In Vitro Cytotoxicity ◽  
X Ray Diffraction ◽  
X Ray ◽  
Cytotoxicity Studies

scholarly journals X-ray Crystal Structure, Geometric Isomerism, and Antimicrobial Activity of New Copper(II) Carboxylate Complexes with Imidazole Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3253 ◽  
Author(s):  
Ioana Vlaicu ◽  
Gheorghe Borodi ◽  
Gina Scăețeanu ◽  
Mariana Chifiriuc ◽  
Luminița Măruțescu ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Single Crystal ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Infrared Spectrometry ◽  
X Ray Diffraction ◽  
X Ray ◽  
Imidazole Derivatives ◽  
Potential Applications

Five new copper(II) acrylate complexes (acr is the acrylate anion: C3H3O2) with imidazole derivatives (2-methylimidazole/2-MeIm, 5-methylimidazole/5-MeIm, 2-ethylimidazole/2-EtIm) of type: cis-[Cu(2-RIm)2(acr)2]·xH2O ((1): R = –CH3, x = 2; (4): R = –CH2–CH3, x = 0), trans-[Cu(2-RIm)2(acr)2] ((2): R = –CH3; (5): R = –CH2–CH3) and trans-[Cu(5-RIm)2(acr)2] ((3): R = –CH3) have been prepared and characterized by elemental analysis, Fourier Transform Infrared spectrometry (FTIR), Electron Paramagnetic Resonance (EPR), electronic reflectance spectroscopy, scanning electron microscopy, and mass spectrometry. The single crystal X-ray diffraction study of complexes (2) and (5) reveals that the copper(II) ion is located on an inversion center and show elongated octahedral geometry completed by two coplanar bidentate acrylates and two unidentate imidazole derivatives displayed in trans positions. For complex (4) the single crystal X-ray diffraction shows that the copper(II) ion is in a distorted octahedral environment which can be easily confused with a trigonal prism completed by two bidentate acrylates and two unidentate imidazole derivatives displayed in cis positions. These results indicate the fact that complexes (4) and (5) are the geometric isomers of the same compound bis(acrylate)-bis(2-ethylimidazole)-copper(II). Complexes (1) and (2), as well as (4) and (5), were produced simultaneously in the reaction of the corresponding copper(II) acrylate with imidazole derivatives in methanol solution. Furthermore, in order to be able to formulate potential applications of the obtained compounds, our next goal was to investigate the in vitro antimicrobial activity of the synthesized complexes against Gram-positive and Gram-negative bacteria, as well as fungal strains, of both clinical and ecological importance (biodeterioration of historical buildings). The trans isomers (2) and (5), followed by (4) have shown the broadest range of antimicrobial activity. In case of (1) and (2) isomers, the trans isomer (2) was significantly more active than cis (1), while the cis isomer (4) proved to be more active than trans (5). Taken together, the biological evaluation results indicate that the trans (2) was the most active complex, demonstrating its potential for the development of novel antimicrobial agents, with potential applications in the biomedical and restoration of architectural monuments fields.

scholarly journals Tersone A-G, New Pyridone Alkaloids from the Deep-Sea Fungus Phomopsis tersa

Marine Drugs ◽  
2019 ◽  
Vol 17 (7) ◽  
pp. 394 ◽  
Author(s):  
Shan-Chong Chen ◽  
Zhao-Ming Liu ◽  
Hai-Bo Tan ◽  
Yu-Chan Chen ◽  
Sai-Ni Li ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
A549 Cell ◽  
Deep Sea ◽  
X Ray Diffraction ◽  
X Ray ◽  
Spectroscopic Analyses ◽  
Ic50 Values ◽  
Mic Value ◽  
Mcf 7

Four phenylfuropyridone racemates, (±)-tersones A-C and E (1–3, 5), one phenylpyridone racemate, (±)-tersone D (4), one new pyridine alkaloid, tersone F (6), single new phenylfuropyridone, tersone G (7) and two known analogs 8 and 9 were isolated from the deep-sea fungus Phomopsis tersa. Their structures and absolute configurations were characterized on the basis of comprehensive spectroscopic analyses, single-crystal X-ray diffraction experiments, and electronic circular dichroism (ECD) calculations. Moreover, compounds 1–9 were evaluated for in vitro antimicrobial and cytotoxic activity. Compounds 5b and 8b exhibited antibacterial activity against S. aureus with the MIC value of 31.5 μg/mL, while compound 5b showed cytoxic activities against SF-268, MCF-7, HepG-2 and A549 cell lines with IC50 values of 32.0, 29.5, 39.5 and 33.2 μM, respectively.

Novel organotin(iv) complexes derived from 4-fluorophenyl-selenoacetic acid: synthesis, characterization and in vitro cytostatic activity evaluation

2017 ◽  
Vol 41 (13) ◽  
pp. 5639-5650 ◽  
Author(s):  
Ya-Ru Qiu ◽  
Ru-Fen Zhang ◽  
Shao-Liang Zhang ◽  
Shuang Cheng ◽  
Qian-Li Li ◽  
...  
Keyword(s):  
Single Crystal ◽  
Elemental Analysis ◽  
Acid Synthesis ◽  
Cytostatic Activity ◽  
X Ray Diffraction ◽  
X Ray ◽  
Activity Evaluation ◽  
Ft Ir

A cluster of novel organotin(iv) complexes were designed, synthesized, and characterized by elemental analysis, FT-IR, and NMR (1H, 13C, and 119Sn) spectroscopy as well as single-crystal X-ray diffraction.

Design and in vitro biological evaluation of substituted chalcones synthesized from nitrogen mustards as potent microtubule targeted anticancer agents

2017 ◽  
Vol 41 (10) ◽  
pp. 4096-4109 ◽  
Author(s):  
X. Janet Sabina ◽  
J. Karthikeyan ◽  
Gunasekaran Velmurugan ◽  
M. Muthu Tamizh ◽  
A. Nityananda Shetty
Keyword(s):  
Single Crystal ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
X Ray Diffraction ◽  
Nitrogen Mustards ◽  
X Ray

Six chalcones were synthesized and their structures determined by single crystal X-ray diffraction studies. They exhibited enhanced anticancer activity and tubulin inhibition.

scholarly journals Mixed natural arylolefin–quinoline platinum(II) complexes: synthesis, structural characterization and in vitro cytotoxicity studies

2018 ◽  
Vol 74 (12) ◽  
pp. 1732-1743
Author(s):  
Nguyen Thi Thanh Chi ◽  
Pham Van Thong ◽  
Truong Thi Cam Mai ◽  
Luc Van Meervelt
Keyword(s):  
Double Bond ◽  
Cytotoxic Effect ◽  
In Vitro Cytotoxicity ◽  
Quinoline Derivative ◽  
X Ray Diffraction ◽  
Hep G2 ◽  
X Ray ◽  
Cytotoxicity Studies ◽  
Mcf 7

Five new platinum(II) complexes bearing a eugenol and a quinoline derivative, namely [η2-4-allyl-2-methoxy-1-(propoxycarbonylmethoxy)benzene]-trans-dichlorido(quinoline-κN)platinum(II), [PtCl2(C15H20O4)(C9H7N)], (2), {η2-4-allyl-2-methoxy-1-[(propan-2-yloxy)carbonylmethoxy]benzene}-trans-dichlorido(quinoline-κN)platinum(II), [PtCl2(C15H19O4)(C9H7N)], (3), [η2-4-allyl-2-methoxy-1-(propoxycarbonylmethoxy)benzene]chlorido(quinolin-8-olato-κ2 N,O)platinum(II), [Pt(C9H6NO)Cl(C15H20O4)], (4), {η2-4-allyl-2-methoxy-1-[(propan-2-yloxy)carbonylmethoxy]benzene}chlorido(quinolin-8-olato-κ2 N,O)platinum(II), [Pt(C9H6NO)Cl(C15H20O4)], (5), and [η2-4-allyl-2-methoxy-1-(propoxycarbonylmethoxy)benzene]chlorido(quinolin-2-carboxylato-κ2 N,O)platinum(II), [Pt(C10H6NO2)Cl(C15H20O4)], (6), have been synthesized and fully characterized spectroscopically. A single-crystal X-ray diffraction study was carried out for complexes (2) and (4)–(6). PrEug [or 4-allyl-2-methoxy-1-(propoxycarbonylmethoxy)benzene] in (2), (4) and (6), and iPrEug (the propan-2-yloxy analogue of PrEug) in (3) and (5) coordinate with PtII at the ethylenic double bond of the allyl group. In (2)–(6), the donor N atom of the amine group occupies a trans position with respect to the double bond. A comparison of the IC50 values of 0.38–29.23 µM for (2)–(6) with cisplatin, as well as other platinum(II) complexes, indicates an excellent in vitro cytotoxicity against the KB, LU, Hep-G2 and MCF-7 cancer cell lines, with the highest cytotoxic effect (IC50 = 0.38–1.99 µM) being for complexes (4) and (5) bearing a quinolin-8-olate ligand.

Electron Microscopy of Shock Loaded Polycrystalline Beryllium

1974 ◽  
Vol 32 ◽  
pp. 506-507 ◽  
Author(s):  
J. M. Galbraith ◽  
L. E. Murr ◽  
A. L. Stevens
Keyword(s):  
Electron Microscopy ◽  
Wave Propagation ◽  
Structural Change ◽  
Single Crystal ◽  
Diffraction Pattern ◽  
Shock Loading ◽  
Slip Systems ◽  
Compression Tests ◽  
X Ray Diffraction ◽  
X Ray

Uniaxial compression tests and hydrostatic tests at pressures up to 27 kbars have been performed to determine operating slip systems in single crystal and polycrystal1ine beryllium. A recent study has been made of wave propagation in single crystal beryllium by shock loading to selectively activate various slip systems, and this has been followed by a study of wave propagation and spallation in textured, polycrystal1ine beryllium. An alteration in the X-ray diffraction pattern has been noted after shock loading, but this alteration has not yet been correlated with any structural change occurring during shock loading of polycrystal1ine beryllium.This study is being conducted in an effort to characterize the effects of shock loading on textured, polycrystal1ine beryllium. Samples were fabricated from a billet of Kawecki-Berylco hot pressed HP-10 beryllium.

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