Get 20M+ Full-Text Papers For Less Than $1.50/day. Start a 14-Day Trial for You or Your Team.

Learn More →

Studies on cis-DDP, (Pt(Dach)(MePhSO)Cl)+ and (Pt(NH3)2(N-Py)Cl)+ Binding to Fumarase

Studies on cis-DDP, (Pt(Dach)(MePhSO)Cl)+ and (Pt(NH3)2(N-Py)Cl)+ Binding to Fumarase STUDIES ON cis-DDP, [Pt(Dach)(MePhSO)Cl]+ AND [Pt(NH 3 ) 2 (N-Py)Clf BINDING TO FUMARASE Güler Yalgin University of Marmara, Faculty of Pharmacy, Department of Analytical Chemistry, 81010 Haydarpa$a, Istanbul, Turkey SUMMARY Two platinum analogs which have suitable physical properties and show antineoplastic activities comparable or greater than that obtained with c/s-DDP were synthesized: [c/s-Pt A 2 (Am) CI] N 0 3 and [Pt (dach) (RR'SO) CI] NO3 (A: ammonia, Am: pyridine, dach: transdiaminocyclohexane, RR'SO: methylphenylsulphoxide). Their interactions with fumarase were studied. Tlie inhibition of fumarase activity by the platinum compounds was followed kinetically by a spectrophotometric method. These two platinum compounds generally inhibited fumarase less than cm-DDP at the concentrators and reaction media (phosphate buffer or NaCl-buffer) studied. KEY WORDS c/s-dichlorodiamineplatinum(II), [Pt(MePhSOXdiaminocyclohexane) CI] N 0 3 , cw-[Pt(NH 3 ) 2 (pyridine)Cl]N03, iumarase, inhibition INTRODUCTION The square planar complex c/s-dichlorodiammineplatinum (cisDDP) (I) is an antineoplastic drug with proven effectiveness against numerous animal and human tumors III. Despite significant antineoplastic activity, its clinical use is limited due to severe side effects /2,3/, especially nephrotoxicity. The mechanism underlying the nephrotoxicity and other side effects is unclear /3-5/. Recently two cationic classes of platinum compounds were described which showed activity in primary http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Drug Metabolism and Drug Interactions de Gruyter

Studies on cis-DDP, (Pt(Dach)(MePhSO)Cl)+ and (Pt(NH3)2(N-Py)Cl)+ Binding to Fumarase

Loading next page...
 
/lp/de-gruyter/studies-on-cis-ddp-pt-dach-mephso-cl-and-pt-nh3-2-n-py-cl-binding-to-Fn4mfdCuxL

References (6)

Publisher
de Gruyter
Copyright
Copyright © 1995 by the
ISSN
2191-0162
eISSN
2191-0162
DOI
10.1515/DMDI.1995.12.2.105
Publisher site
See Article on Publisher Site

Abstract

STUDIES ON cis-DDP, [Pt(Dach)(MePhSO)Cl]+ AND [Pt(NH 3 ) 2 (N-Py)Clf BINDING TO FUMARASE Güler Yalgin University of Marmara, Faculty of Pharmacy, Department of Analytical Chemistry, 81010 Haydarpa$a, Istanbul, Turkey SUMMARY Two platinum analogs which have suitable physical properties and show antineoplastic activities comparable or greater than that obtained with c/s-DDP were synthesized: [c/s-Pt A 2 (Am) CI] N 0 3 and [Pt (dach) (RR'SO) CI] NO3 (A: ammonia, Am: pyridine, dach: transdiaminocyclohexane, RR'SO: methylphenylsulphoxide). Their interactions with fumarase were studied. Tlie inhibition of fumarase activity by the platinum compounds was followed kinetically by a spectrophotometric method. These two platinum compounds generally inhibited fumarase less than cm-DDP at the concentrators and reaction media (phosphate buffer or NaCl-buffer) studied. KEY WORDS c/s-dichlorodiamineplatinum(II), [Pt(MePhSOXdiaminocyclohexane) CI] N 0 3 , cw-[Pt(NH 3 ) 2 (pyridine)Cl]N03, iumarase, inhibition INTRODUCTION The square planar complex c/s-dichlorodiammineplatinum (cisDDP) (I) is an antineoplastic drug with proven effectiveness against numerous animal and human tumors III. Despite significant antineoplastic activity, its clinical use is limited due to severe side effects /2,3/, especially nephrotoxicity. The mechanism underlying the nephrotoxicity and other side effects is unclear /3-5/. Recently two cationic classes of platinum compounds were described which showed activity in primary

Journal

Drug Metabolism and Drug Interactionsde Gruyter

Published: Jun 1, 1995

There are no references for this article.