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العنوان
N,S and N,O-donors complexes as anticancer agents /
المؤلف
Ismail, Amany Mahmoud Ismail.
هيئة الاعداد
باحث / امانى محمود اسماعيل اسماعيل
مشرف / سحر ابراهيم حامد مصطفى
مشرف / برتراند جون كلود
مشرف / وئام محمد ابوالمعاطي
مناقش / محمج عبدالجواد عبدالسلام زايد
مناقش / ليلى حمدان عبدالرحمن قناوي
الموضوع
Indoleacetic acid. Chemical equilibrium.
تاريخ النشر
2019.
عدد الصفحات
online resource (214 pages) :
اللغة
الإنجليزية
الدرجة
ماجستير
التخصص
Inorganic Chemistry
الناشر
تاريخ الإجازة
01/01/2019
مكان الإجازة
جامعة المنصورة - كلية العلوم - Department of Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 214

Abstract

New complexes of indole-3-acetic acid (HIAA) and 2-amino-4,6-dimercaptotriazine (HAT) as primary chelate with Zn(II), Pd(II), Pt(II) , Ag(I) and and MoO22+ in presence and absence of secondary ligands, 2,2,-bipyridyl (bpy) and triphenylphosphine (PPh3) . The stoichiometries and stability constants of these complexes in aqueous (saline) solutions were also calculated spectrophotometrically. UV-visible spectroscopy was applied to study interaction of selected complexes with CT-DNA. Based on the degree of binding ability of the complexes with CT-DNA, the anticancer activity of some complexes was tested against the human ovarian cancer (VC-8-BRCA and VC-8) cell lines.High to moderate binding ability of the complexes with CT-DNA are reported. The moderate binding ability may be due to steric hindrance around the metal ions, that comes from the HIAA or HAT primary and /or bulky secondary (bpy, PPh3) chelate, due to π-π interactions through the conjugated moieties. In addition, this feature may be due to either the different matching between the complex and DNA or the different binding sites of the donors, as DNA is a flexible double helix, and the complex can intercalate towards the DNA helix axis from any direction in an intercalative mode. The reported complexes show hyperchromic effect (an external contact or a partial uncoiling of the DNA structure, thus exposing more DNA bases to the possibility of electrostatic binding). Furthermore, hyperchromism may also signify the modifications (unwinding/opening) in the DNA double helical structure. Moreover, the molar Gibb’s free energy of binding (ΔGob) values were calculated and found in -30.01to-41.89 kJmol-1 region, indicating the spontaneity of the complexes-DNA adduct formation.The growth of the human ovarian cancer (VC-8-BRCA & VC-8) cell lines was measured using SRB assay the combination of HIAA or HAT with the metal ions in the complexes could inhibit the growth of VC-8-BRCA & VC-8 cells more than the free HIAA, suggesting that the anticancer activity is due to complexation. The complex, [Ag(bpy)(HIAA)]NO3, shows the highest efficacy with IC50 8.87±0.2 and 8.80±0.1 M against VC-8-BRCA and VC-8 cell lines, respectively. The moderate activity of [Zn(AT)2(H2O)2] and [Zn(bpy)(AT)Cl(H2O)], indicate that they are promising as anticancer agents due to their high selectivity towards cancer cells and low toxicity towards non-cancer cells; i.e., they are of great significance for the exploitation of the metal drugs with high selectivity and low toxicity.