کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10596180 | 981897 | 2013 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and inhibitory activities of naringenin derivatives on human colon cancer cells
ترجمه فارسی عنوان
طراحی، سنتز و فعالیت های مهار کننده مشتقات نیرینژین در سلول های سرطانی انسان کولون
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کلمات کلیدی
فلاونون، نایرینگینین، سرطان کولون، در اتصال سیلکو،
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
Based on the previous result, several naringenin derivatives modified at position 7 with bulky substituents were designed and synthesized, and their inhibitory effects on HCT116 human colon cancer cells were tested using a clonogenic assay. The half maximal inhibitory concentrations (IC50) of five naringenin derivatives ranged between 1.20 μM and 20.01 μM which are much better than naringenin used as a control. In addition, new structural modification at C-4 of flavanone results in improving both the anti-cancer effect and anti-oxidative effect. In vitro cyclin dependent kinase 2 (CDK2) binding assay was carried out based on the previous results. To elucidate the possible interaction between naringenin derivatives and CDK2, in silico docking study was performed. This result demonstrates the rationale for the different inhibitory activities of the naringenin derivatives. These findings could be used for designing cancer therapeutic or preventive flavanone-derived agents.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 1, 1 January 2013, Pages 232-238
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 1, 1 January 2013, Pages 232-238
نویسندگان
Hyuk Yoon, Tae Woo Kim, Soon Young Shin, Mi Joo Park, Yeonjoong Yong, Dong Woon Kim, Tasneem Islam, Young Han Lee, Kang-Yeoun Jung, Yoongho Lim,