期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 124, 期 -, 页码 70-77出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2013.03.011
关键词
Platinum; Histone deacetylases; Histone deacetylase inhibitors; Belinostat; Anti-cancer; Cytotoxicity
资金
- Science Foundation Ireland [08/RFP/CHE1675, 11/RFP.1/CHS/3095]
- Programme for Research in Third Level Institutions (PRTLI)
- Technological Sector Research, Strand III
- Science Foundation Ireland (SFI) [11/RFP.1/CHS/3095, 08/RFP/CHE1675] Funding Source: Science Foundation Ireland (SFI)
The successful design and synthesis of a novel Pt complex of the histone deacteylase inhibitor belinostat are reported. Molecular modelling assisted in the identification of a suitable malonate derivative of belinostat (mal-p-Bel) for complexation to platinum. Reaction of [Pt(NH3)(2)(H2O)(2)](NO3)(2) with the disodium salt of mal-p-Bel gave cis-[Pt(NH3)(2)(mal-p-Bel(-2H))] (where -(2H) indicates that mal-p-Bel is doubly deprotonated) in excellent yield. An in vitro cytotoxicity study revealed that cis-[Pt(NH3)(2)(mal-p-Bel(-2H)] possesses (i) considerable cytotoxicity against reported ovarian cancer cell lines, (ii) enhanced cytotoxicity relative to the previously reported Pt histone deacetylase inhibitor conjugate, cis-[Pt-II(NH3)(2)(malSAHA(-2H))] and (iii) favourable cyto-selective properties as compared to cisplatin and belinostat. (C) 2013 Elsevier Inc. All rights reserved.
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