کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369758 | 981787 | 2016 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of novel 5-fluorine-benzimidazole-4-carboxamide analogs were designed and synthesized. All target compounds were evaluated for their PARP-1 inhibitory activity. Compounds possessed high intrinsic PARP-1 inhibitory potency have been evaluated in vitro cellular assays to measure the potentiation effect of cytotoxic agents against cancer cell line. These efforts led to the identification of compound 10f, which displayed strong inhibition against the PARP-1 enzyme with an IC50 of 43.7 nM, excellent cell inhibitory activity in HCT116 cells (IC50 = 7.4 μM) and potentiation of temozolomide cytotoxicity in cancer cell line A549 (PF50 = 1.6).
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 16, 15 August 2016, Pages 4127–4132
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 16, 15 August 2016, Pages 4127–4132
نویسندگان
Junwei Wang, Xuyan Wang, Hui Li, Dezhong Ji, Yuyan Li, Yungen Xu, Qihua Zhu,