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AuthorParker, James P.
AuthorNimir, Hassan
AuthorGriffith, Darren M.
AuthorDuff, Brian
AuthorChubb, Anthony J.
AuthorBrennan, Marian P.
AuthorMorgan, Maria P.
AuthorEgan, Denise A.
AuthorMarmion, Celine J.
Available date2015-11-15T10:42:59Z
Publication Date2013-03
Publication NameJournal of Inorganic Biochemistry
Identifierhttp://dx.doi.org/10.1016/j.jinorgbio.2013.03.011
CitationParker, J., Nimir, H., Griffith, D. , et. al. (2013) ,"A novel platinum complex of the histone deacetylase inhibitor belinostat: Rational design, development and in vitro cytotoxicity", 124:70-77
ISSN0162-0134
URIhttp://hdl.handle.net/10576/3818
AbstractThe 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-[PtII(NH3)2(malSAHA-2H)] and (iii) favourable cyto-selective properties as compared to cisplatin and belinostat.
SponsorScience Foundation Ireland Grant Nos. [08/RFP/CHE1675] and [11/RFP.1/CHS/3095]. Programme for Research in Third Level Institutions (PRTLI), administered by the HEA for funding and the Technological Sector Research, Strand III (2006–2010).
Languageen
PublisherElsevier Inc.
SubjectPlatinum
SubjectHistone deacetylases
SubjectHistone deacetylase inhibitors
SubjectBelinostat
SubjectAnti-cancer Cytotoxicity
TitleA novel platinum complex of the histone deacetylase inhibitor belinostat: Rational design, development and in vitro cytotoxicity
TypeArticle
Pagination70-77
Volume Number124


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