In vivo Anti-Tumour Activity of Ethyl Heptyloxyacetate against Ehrlich Ascites Cells

Nature ◽  
1963 ◽  
Vol 198 (4878) ◽  
pp. 384-385 ◽  
Author(s):  
GORDON F. TOWNSEND ◽  
WILLIAM H. BROWN ◽  
ETHEL E. FELAUER
2019 ◽  
Vol 30 ◽  
pp. v424
Author(s):  
K. Hasegawa ◽  
K. Taniguchi ◽  
S. Sato ◽  
A. Yoshinaga ◽  
M. Tsugane ◽  
...  

1985 ◽  
Vol 16 (3-4) ◽  
pp. 284-286 ◽  
Author(s):  
Antoinette Fray ◽  
Claude Burtin ◽  
Pierre Scheinmann ◽  
Geneviève Lespinats ◽  
Paulette Canu

2009 ◽  
Vol 16 (4) ◽  
pp. 1185-1195 ◽  
Author(s):  
Céline Van Themsche ◽  
Sophie Parent ◽  
Valérie Leblanc ◽  
Caroline Descôteaux ◽  
Anne-Marie Simard ◽  
...  

We have previously reported the synthesis of VP-128, a new 17β-oestradiol (E2)-linked platinum(II) hybrid with high affinity for oestrogen receptor α (ERα). In the present study, we have investigated the anti-tumour activity of VP-128 towards breast cancer cells in vitro and in vivo. We used human ERα-positive (MCF-7) and -negative (MDA-MB-468) cells as a model for treatment with increasing doses of VP-128, cisplatin or E2 in vitro and for xenograft experiments in nude mice in vivo. Compared with cisplatin, VP-128 showed markedly improved in vitro and in vivo anti-tumour activity towards ERα-positive MCF-7 breast cancer cells, without increased systemic toxicity. In these caspase-3-deficient cells, treatment with VP-128 overcame weak cellular sensitivity to cisplatin in vitro and in vivo. In these cells, only the hybrid induced apoptosis in an ERα-dependent manner, inactivated both X-linked inhibitor of apoptosis protein and Akt, and induced selective nuclear accumulation of ERα and the expression of ER-regulated genes c-myc and tff1, which was blocked by ERα-specific antagonist ICI 282 780. In the case of ERα-negative MDA-MB-468 cells, VP-128, but not cisplatin, induced nuclear accumulation of apoptosis-inducing factor and inhibited c-myc expression. However, VP-128 did not show enhanced in vivo anti-tumour activity compared with cisplatin. These results reveal two different modes of action for VP-128 in ERα-positive and -negative breast cancer cells, and highlight the promising therapeutic value of this unique E2-platinum hybrid for selective targeting of hormone-dependent cancers.


1999 ◽  
Vol 80 (8) ◽  
pp. 1252-1258 ◽  
Author(s):  
L Qiu ◽  
M J Kelso ◽  
C Hansen ◽  
M L West ◽  
D P Fairlie ◽  
...  

1998 ◽  
Vol 5 (5) ◽  
pp. 295-304 ◽  
Author(s):  
Katharine A. Smith ◽  
Glen B. Deacon ◽  
W. Roy Jackson ◽  
Edward R. T. Tiekink ◽  
Silvina Rainone ◽  
...  

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.


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