scholarly journals Synthesis andin vitroAntitumor Potency of (Cyclohexane-1,2-Diamine)Platinum(II) Complexes with Aminotris(Methylenephosphonic Acid) as Bone-Seeking Ligand

2005 ◽  
Vol 3 (3-4) ◽  
pp. 179-190 ◽  
Author(s):  
Markus Galanski ◽  
Susanna Slaby ◽  
Michael A. Jakupec ◽  
Bernhard K. Keppler

In order to develop platinum complexes with selective activity in primary and secondary bone malignancies and with the aim to optimize antitumor activity, platinum(II) complexes with aminotris(methylenephosphonic acid) as bone-seeking (osteotropic) ligand have been synthesized, characterized and tested in the cisplatin-sensitive ovarian carcinoma cell line CH1. As non-leaving diamine ligands, which are decisive for the cellular processing of DNA adducts,cis-R,S-cyclohexane-1,2-diamine,trans-S,S-cyclohexane-1,2-diamine andtrans-R,R-cyclohexane-1,2-diamine have been used, resulting in complexes 1, 2, and 3, respectively. The cytotoxicity of the complexes under investigation decreases in the order 3>2>1 which is in accord with structure-activity relationships with other (cyclohexane-1,2- diamine)platinum(II) and platinum(IV) complexes: Bothtranscomplexes (2 and 3) display a higherin vitropotency than the correspondingcisisomer (I), with thetrans-R,Risomer (3) being the most active in this series. In comparison to the analogous (cyclohexane-1,2-diamine)platinum(II) complexes with bis(phosphonomethyl)aminoacetic acid as osteotropic carrier ligand, the cytotoxicity of 1-3 was found to be 1.5 – 2 fold higher, which is explainable by a different coordination mode of the phosphonic acid ligands (acetato versus phosphonato).


2013 ◽  
Vol 781-784 ◽  
pp. 1152-1155
Author(s):  
Tang Li ◽  
Li Yu

The invasion behavior of tumor cells is important in the metastasis process of ovarian cancer cells. In this study we investigated the effects of Genistein on invasion inhibition in ovarian carcinoma cell line SKOV3 in vivo and in vitro. The abilities of the Genistein-treated SKOV3 cells to invade through reconstitute matrigel in transwell chambers were investigated in vitro and the invasion effect in vivo was determined by using the xenograft models of SKOV3 in nude mice. The ability of the 20μmol/L Genistein-treated cells to invade the reconstitute basement membrane was decreased significantly at 72h. This inhibition was dose-dependent. 40μmol/L Genistein had the strongest effect. The in vivo result suggested that the grade of invasion in control SKOV3 cells was time-dependent and Genistein-treated group could apparently inhibit the progress of invasion, localizing the tumor in invasion Grade 0 or Grade I and decreasing the proportion of Grade II, III and IV. The results suggested that Genistein possessed inhibitory effect on invasion in human ovarian carcinoma cell lines SKOV3 in vivo and in vitro.





2018 ◽  
Vol 156 ◽  
pp. 214-223 ◽  
Author(s):  
Ricardo M. da Costa ◽  
Jairo K. Bastos ◽  
Maria C.A. Costa ◽  
Márcia M.C. Ferreira ◽  
Cássia S. Mizuno ◽  
...  




2004 ◽  
Vol 92 (2) ◽  
pp. 578-585 ◽  
Author(s):  
Xing Xie ◽  
Da-Feng Ye ◽  
Huai-Zeng Chen ◽  
Wei-Guo Lu ◽  
Yun-Feng Fu ◽  
...  






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