scholarly journals Synthesis, Structure of Nitrogen-Containing Phosphinogold(I) Ferrocenes. In vitro Activity against Bladder and Colon Carcinoma Cell Lines

1995 ◽  
Vol 2 (6) ◽  
pp. 311-326 ◽  
Author(s):  
Manuella Viotte ◽  
Bernard Gautheron ◽  
Marek M. Kubicki ◽  
Ilya E. Nifant'ev ◽  
Simon P. Fricker
Keyword(s):  
Carcinoma Cell ◽  
In Vitro Activity ◽  
X Ray ◽  
Carcinoma Cell Lines ◽  
Anti Tumour Activity ◽  
Tetramethylammonium Bromide ◽  
Tumour Activity ◽  
Nitrogen Phosphorus ◽  
Good Agreement

The gold salt [(tht)AuCl] was reacted with [1-N,N-dimethylaminométhyl-2-diphenylphosphino]ferrocene (1) forming the bimetallic derivative 4. The reaction of methyl iodide and tetramethylammonium bromide on the chloride 4 produced the ammonium salt 5 and the bromide 6 respectively. New aminophosphines 2 and 3, which represent two of the rare phosphorylated metallocenes containing P(III)-N bond have also been coordinated to gold(I) to form 7 and 8. The presence of the ethoxy group in 7 provides evidence for the lability of one nitrogen-phosphorus bond. The X-ray structure of compounds 4 and 7 have been established. Both crystallize in space group P21/c, monoclinic, with a = 11.095(2) Å, b = 12.030(3) Å, c = 17.763(4) Å, β= 94.02(2)∘, Z = 4 for 4 and a = 14.863(3) Å, b = 8.036(5)Å, c = 18.062(5)Å, β =101.64(1)°, Z = 4 for 7. A197u Mössbauer data are in good agreement with those for other linear P-Au-Cl containing complexes. The compounds were evaluated for in vitro anti-tumour activity against two human tumours. Differential cytotoxicity was observed with activity comparable to cisplatin, with the exception of one compound which was significantly more cytotoxic.

scholarly journals Preparation and Anti-Tumour Activity of Some Arylbismuth(III) Oxine Complexes

1998 ◽  
Vol 5 (5) ◽  
pp. 295-304 ◽  
Author(s):  
Katharine A. Smith ◽  
Glen B. Deacon ◽  
W. Roy Jackson ◽  
Edward R. T. Tiekink ◽  
Silvina Rainone ◽  
...  
Keyword(s):  
Phenyl Group ◽  
Significant Activity ◽  
X Ray ◽  
Crystallographic Study ◽  
Anti Tumour Activity ◽  
In Vivo Testing ◽  
Tumour Activity ◽  
Better Than

New arylbismuth(lll) oxinates, PhBi(MeOx)2, (p-MeC6H4)Bi(Ox)2, (p-MeC6H4)Bi(MeOx)2, (p-ClC6H4)Bi(Ox)2, and (p-ClC6H4)Bi(MeOx)2 (Ox− = quinolin-8-olate and MeOx−=2-methylquinolin-8-olate) have been prepared by reaction of the appropriate diarylbismuth chlorides with Na(Ox) or Na(MeOx) in the presence of 15-crown-5. An X-ray crystallographic study has shown PhBi(MeOx)2 to be a five coordinate monomer with distorted square pyramidal stereochemistry. Chelating MeOx ligands have a cisoid arrangement in the square plane and the phenyl group is apical. The lattice is stabilised by significant π-π interactions between centrosymmetric molecules. A range of these complexes has been shown to have high in vitro biological activity (comparable with or better than cisplatin) against L1210 leukaemia, the corresponding cisplatin resistant line, and a human ovarian cell line, SKOV-3. However, initial in vivo testing against a solid mouse plasmacytoma (PC6) and P388 leukaemia has not revealed significant activity.

In vitro activity of novel antifolates against human squamous carcinoma cell lines of the head and neck with inherent resistance to methotrexate

1992 ◽  
Vol 51 (6) ◽  
pp. 909-914 ◽  
Author(s):  
B. F. A. M. van der Laan ◽  
G. Jansen ◽  
G. A. M. Kathmann ◽  
G. R. Westerhof ◽  
J. H. Schornagel ◽  
...  
Keyword(s):  
Head And Neck ◽  
Cell Lines ◽  
Carcinoma Cell ◽  
Squamous Carcinoma ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Carcinoma Cell Lines ◽  
Squamous Carcinoma Cell

scholarly journals X-Ray Structure and In Vitro Anti-Tumoural Activity of the Dimeric Bis[(2-Phenyl-1,2-Dicarba-Closo-Dodecaborane-1-Carboxylato)-Di-n-Butyltin] Oxide

1997 ◽  
Vol 4 (2) ◽  
pp. 75-80 ◽  
Author(s):  
Edward R. T. Tiekink ◽  
Marcel Gielen ◽  
Abdeslam Bouhdid ◽  
Rudolph Willem ◽  
Vladimir I. Bregadze ◽  
...  
Keyword(s):  
Cell Lines ◽  
Carboxylate Ligand ◽  
X Ray Diffraction ◽  
X Ray ◽  
Anti Tumour Activity ◽  
Common Motif ◽  
The Common ◽  
Tumour Activity ◽  
Oxygen Atoms

X-ray diffraction studies reveal the structure of {[(2-C6H5-1,2-C2B10H10-1-COO)Bu2Sn]2O}2, 1, to conform to the common motif found for {[(R′COO)R2Sn]2O}2 compounds. The dimer features a central Bu4Sn2O2 unit (two-fold symmetry) with the two Bu2Sn groups being linked via bridging oxygen atoms, each of which also carries an exocyclic Bu2Sn moiety. The two pairs of exo- and endo-cyclic tin atoms are each linked via an almost symmetrically bridging carboxylate ligand and the two remaining ligands coordinate an exocyclic tin atom only, in the monodentate mode. The in vitro anti-tumour activity of 1, determined against a variety of cell lines, is compared with those of the corresponding 2-methylcarboranylacetate, derivative 2, and with clinically used compounds.

A New Purine Derivative from the Roots of Phyllanthus flexuosus

2018 ◽  
Vol 13 (1) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Guanlin Zhu ◽  
Hongying Wang ◽  
Kunrong Gan ◽  
Heng Gao ◽  
Wei Li
Keyword(s):  
Spectroscopic Analysis ◽  
Carcinoma Cell ◽  
Inhibitory Effect ◽  
X Ray Diffraction ◽  
Purine Derivative ◽  
X Ray ◽  
Carcinoma Cell Lines ◽  
Human Hepatocellular Carcinoma Cell ◽  
Different Levels

A new purine derivative, 1-methyl-3-isopentenylisoguanine (1), together with six known compounds (2-7), was isolated from the roots of Phyllanthus flexuosus. The newly isolated structure was established by means of extensive spectroscopic analysis and single-crystal X-ray diffraction experiment. All isolates were evaluated for their in vitro cytotoxicities against two human hepatocellular carcinoma cell lines (HepG2 and SMMC-7721) by CCK-8 assays. Among them, three cleistanthane diterpenes (2–4) exhibited different levels of cytotoxicities against these cells with IC50 values ranging from 27.34 to 53.28 μM. Furthermore, acetylcholinesterase inhibitory effect for the new purine derivative was also assessed.

Synthesis and Anti-Tumor Activity Evaluation of Novel 7-Fluoro-4-(1- Piperazinyl) Quinolines

2019 ◽  
Vol 16 (6) ◽  
pp. 663-669
Author(s):  
Dan Liu ◽  
Aiqi Xue ◽  
Zhixin Liu ◽  
Yi Zhang ◽  
Penghui Peng ◽  
...  
Keyword(s):  
Spectral Analysis ◽  
Cancer Therapy ◽  
Carcinoma Cell ◽  
A549 Cells ◽  
Quinoline Derivatives ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Human Carcinoma Cell ◽  
Anti Tumor Activity

Background: Three series of new 7-fluoro-4-(1-piperazinyl) quinolines (I1~I6, II1~II2 and IV1~IV4) were synthesized. Their anti-tumor activity was evaluated in vitro against three human carcinoma cell lines, namely SGC-7901 cells, BEL-7402 cells and A549 cells expressing high levels of EGFR by Methyl Thiazolyl Terazolium (MTT) assay. Methods: Three series of quinoline derivatives were synthesized, characterized and evaluated for their in vitro anti-tumor activities. Results and Discussion: Structures of the newly synthesized compounds were confirmed by spectral analysis. The preliminary bioassay indicated that compounds I1, I10 and II1 exhibited better anti-tumor activity than the rest of the target compounds and gefitinib against A549 cell based assay, which demonstrated that compounds I1, I10 and II1 are potential agents for cancer therapy. Results suggested that the substitutes on piperazinyl influenced anti-tumor activities remarkably. Conclusion: These results are useful for discovering more potent novel anti-tumor compounds and further studies are ongoing.

Suppression of growth in vitro and tumorigenicity in vivo of human carcinoma cell lines by transfectedp16INK4

1996 ◽  
Vol 16 (1) ◽  
pp. 53-60 ◽  
Author(s):  
Elisa A. Spillare ◽  
Aikou Okamoto ◽  
Koichi Hagiwara ◽  
Douglas J. Demetrick ◽  
Manuel Serrano ◽  
...  
Keyword(s):  
Cell Lines ◽  
Carcinoma Cell ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Human Carcinoma Cell
Sign in / Sign up

Export Citation Format

Share Document