Benner
دنيا لفته الدحيدحاوي ( أستاذ مساعد )
كلية الصيدلة - صيدلة عام
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Synthesis of New Benzimidazole and Benzothiazole Disulfide Metal Complexes as G-quadruplex Binding Ligands
تحميل
بحث النوع:
صيدلة التخصص العام:
Lafta D اسم الناشر:
Saour K اسماء المساعدين:
Anti-Cancer Agents in Medicinal Chemistry(Bentham sciences) الجهة الناشرة:
Formerly Current Medicinal Chemistry - Anti-Cancer Agents) Ranking and Category: 27th of 59 in Chemistry, Medicinal 118th of 213 in Oncology Current: 2.722 5 - Year: 2.849  
2016 سنة النشر:

الخلاصة

Compounds that can bind and stabilize non-canonical DNA structures are named quadruplex and are of interest in anticancer drug design due to their selective inhibitions of telomerase and consequent effects on cell proliferation. In this study, we report novel Co/Cu [II] complex compounds as G-quadruplex DNA binding ligands. The results from the preliminary assay indicated that the introduction of a positively charged 6-membered tail to the aromatic terminal group of benzimidazole significantly enhanced the binding affinity with the quadruplex and exhibited anti-telomerase activity. These derivatives showed significant selectivities for the telomeric quadruplex over duplex nucleic acids. The stabilization of non-canonical forms estimated with the FRET DNA technology using different sequences, such as F21T, c-kit1 and c-kit2, in cancer cell lines were assessed. Three members of this family showed to be very selective in stabilizing one particular G-quadruplex.