Synthesis and cytotoxicity of new platinum(IV) complexes of mixed carboxylates

Rita Song, Sun Young Park, Yeong Sang Kim, Youngmee Kim, Sung Jin Kim, Byung Tae Ahn, Youn Soo Sohn

Research output: Contribution to journalArticlepeer-review

26 Scopus citations

Abstract

In order to develop new antitumor platinum(IV) complexes with highly tuned lipophilicity, a series of (diamine)Pt(IV) complexes of the formula [PtIV(dach)L3L′] or [PtIV(dach)L2L″2] (dach=trans-(±)-1,2-diaminocyclohexane; L=acetato, propionato; L′=acetato, propionato, valerato or pivalato; L″=trifluoroacetato) have been synthesized by electrophilic substitution of the tris(carboxylato)hydroxoplatinum(IV) complexes, [PtIV(dach)L3OH] (L=acetato, propionato), with various carboxylic anhydrides such as acetic, trifluoroacetic, pivalic and valeric anhydrides. The present platinum(IV) complexes were fully characterized by means of elemental analyses, 1H NMR, mass and IR spectroscopies. The complexes 8 and 10, satisfying the appropriate range of lipophilicity (logP=0.18-1.54), exhibited high activity (ED50, 5.1 and 1.3 μM, respectively) compared with other complexes, which implies that the lipophilicity is an important factor for the antitumor activity of this series of complexes.

Original languageEnglish
Pages (from-to)339-345
Number of pages7
JournalJournal of Inorganic Biochemistry
Volume96
Issue number2-3
DOIs
StatePublished - 1 Aug 2003

Bibliographical note

Funding Information:
This research was supported by the Basic Research Program of the Korea Science and Engineering Foundation (R03-2000-000-000080(2002)) and the Ministry of Science and Technology in Korea.

Keywords

  • Anticancer
  • Cytotoxicity
  • Lipophilicity
  • Platinum(IV)

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