کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1313526 1499312 2016 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Novel fluorinated benzimidazole-based scaffolds and their anticancer activity in vitro
ترجمه فارسی عنوان
ریل داربست های مبتنی بر بنزیمیدازول فلوراید و فعالیت ضد سرطانی آنها در آزمایشگاهی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی معدنی
چکیده انگلیسی


• A library of twelve fluoroaryl benzimidazoles prepared.
• SNAr strategy allows rapid assembly of linked and macrocyclic heterocyclic structures.
• X-ray crystal structures of fluorinated 21- and 24-membered macrocycles.
• Three compounds exhibit micromolar inhibition of K-562 and MCF-7 cell lines.
• Two compounds activate caspases leading to apoptosis.

A small library of twelve, structurally diverse, fluoroaryl benzimidazoles was prepared using a simple synthetic strategy employing SNAr reactions. This allowed rapid assembly of heterocyclic structures containing linked and tethered fluoroaryl benzimidazoles. X-ray crystal structures of seven compounds were obtained including those of two macrocyclic compounds containing 21- and 24-membered rings. Three tethered fluoroaryl benzimidazole derivatives demonstrated micromolar inhibition against K-562 and MCF-7 cell lines. These compounds, in addition to 1-tetrafluoropyrid-4-yl-2-tetrafluoropyrid-4-ylsulfanyl-1H-benzimidazole, also demonstrated micromolar inhibition against G361 and HOS cell lines. Two of the compounds were found to activate caspases leading to apoptosis.

Figure optionsDownload as PowerPoint slideLinked and macrocyclic fluoropyridylbenzimidazoles exhibit anti-cancer activity against breast carcinoma MCF-7 and leukemia K562 cell lines.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Fluorine Chemistry - Volume 188, August 2016, Pages 99–109
نویسندگان
, , , , , , , , , , ,