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المؤلفParker, James P.
المؤلفNimir, Hassan
المؤلفGriffith, Darren M.
المؤلفDuff, Brian
المؤلفChubb, Anthony J.
المؤلفBrennan, Marian P.
المؤلفMorgan, Maria P.
المؤلفEgan, Denise A.
المؤلفMarmion, Celine J.
تاريخ الإتاحة2015-11-15T10:42:59Z
تاريخ النشر2013-03
اسم المنشورJournal of Inorganic Biochemistry
المعرّفhttp://dx.doi.org/10.1016/j.jinorgbio.2013.03.011
الاقتباسParker, 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
الرقم المعياري الدولي للكتاب0162-0134
معرّف المصادر الموحدhttp://hdl.handle.net/10576/3818
الملخصThe 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.
راعي المشروعScience 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).
اللغةen
الناشرElsevier Inc.
الموضوعPlatinum
Histone deacetylases
Histone deacetylase inhibitors
Belinostat
Anti-cancer Cytotoxicity
العنوانA novel platinum complex of the histone deacetylase inhibitor belinostat: Rational design, development and in vitro cytotoxicity
النوعArticle
الصفحات70-77
رقم المجلد124
dc.accessType Abstract Only


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