Structure—Activity Relationships for Anti—Tumour Platinum Complexes

1983 ◽  
pp. 59-91 ◽  
Author(s):  
M. J. Cleare
Keyword(s):  
Platinum Complexes ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Characterization of platinum(II) complexes exhibiting inhibitory activity against the 20S proteasome

2020 ◽  
Vol 7 (8) ◽  
pp. 200545
Author(s):  
Tatsuto Kiwada ◽  
Hiromu Katakasu ◽  
Serina Okumura ◽  
Akira Odani
Keyword(s):  
Inhibitory Activity ◽  
Chemical Structure ◽  
Competitive Inhibition ◽  
Proteasome Inhibitors ◽  
Platinum Complex ◽  
Platinum Complexes ◽  
Binding Mode ◽  
Structure Activity Relationships ◽  
Structure Activity

Proteasome inhibitors are useful for biochemical research and clinical treatment. In our previous study, we reported that the 4N-coordinated platinum complexes with anthracenyl ring and heterocycle exhibited proteasome-inhibitory activity. In the present study, the structure–activity relationships and characterization of these complexes were determined for the elucidation of the role of aromatic ligands. Lineweaver–Burk analysis revealed that the chemical structure of heterocycles affects the binding mode of platinum complexes. Platinum complexes with anthracenyl ring and pyridine showed competitive inhibition, although platinum complexes with anthracenyl ring and phenanthroline showed non-competitive inhibition. The structure–activity relationships demonstrated that anthracenyl moiety plays a crucial role in proteasome-inhibitory activity. The platinum complexes with naphthyl or phenyl rings exhibited lower inhibitory activities than the platinum complex with anthracenyl ring. The reactivity with N-acetylcysteine varied according to the chemical structure of complexes.

ANTITUMOR PLATINUM COMPLEXES: STRUCTURE-ACTIVITY RELATIONSHIPS

Cisplatin ◽  
1980 ◽  
pp. 149-170 ◽  
Author(s):  
Michael J. Cleare ◽  
Paul C. Hydes ◽  
Deric R. Hepburn ◽  
Bernard W. Malerbi
Keyword(s):  
Platinum Complexes ◽  
Structure Activity Relationships ◽  
Structure Activity

Reversion of Structure-Activity Relationships of Antitumor Platinum Complexes by Acetoxime but Not Hydroxylamine Ligands

2006 ◽  
Vol 71 (1) ◽  
pp. 357-365 ◽  
Author(s):  
Stefanie Zorbas-Seifried ◽  
Michael A. Jakupec ◽  
Nikolay V. Kukushkin ◽  
Michael Groessl ◽  
Christian G. Hartinger ◽  
...  
Keyword(s):  
Platinum Complexes ◽  
Structure Activity Relationships ◽  
Structure Activity

Structure-activity relationships in the acronycine and benzo[b]acronycine series: Role of the pyran ring

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
Q Do ◽  
H Doan Thi Mai ◽  
T Gaslonde ◽  
B Pfeiffer ◽  
S Léonce ◽  
...  
Keyword(s):  
Pyran Ring ◽  
Structure Activity Relationships ◽  
Structure Activity

Structure activity-relationships of P-Glycoprotein modulation using a small library of macrocyclic lathyrane diterpenes

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
M Reis ◽  
RJ Ferreira ◽  
MMM Santos ◽  
DJVA dos Santos ◽  
J Molnár ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
Structure Activity ◽  
P Glycoprotein
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