Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors

Wang Junwei; Wang Xuyan; Li Hui; Ji Dezhong; Li Yuyan; Xu Yungen; Zhu Qihua

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Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors

机译：新型5-氟-1H-苯并咪唑-4-羧酰胺衍生物作为强效PARP-1抑制剂的设计，合成和生物学评价

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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 mu M) and potentiation of temozolomide cytotoxicity in cancer cell line A549 (PF50 = 1.6). (C) 2016 Elsevier Ltd. All rights reserved.

机译：设计并合成了一系列新颖的5-氟-苯并咪唑-4-羧酰胺类似物。评价所有目标化合物的PARP-1抑制活性。具有高固有PARP-1抑制能力的化合物已在体外细胞分析中进行了评估，以测量细胞毒剂对癌细胞系的增强作用。这些努力导致了化合物10f的鉴定，该化合物显示出对PARP-1酶的强抑制作用，IC50为43.7 nM，在HCT116细胞中具有出色的细胞抑制活性（IC50 = 7.4μM），并增强了癌细胞系中替莫唑胺的细胞毒性A549（PF50 = 1.6）。（C）2016 Elsevier Ltd.保留所有权利。

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《Bioorganic and Medicinal Chemistry Letters》 |2016年第16期|共6页
作者
Wang Junwei; Wang Xuyan; Li Hui; Ji Dezhong; Li Yuyan; Xu Yungen; Zhu Qihua;
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正文语种 eng
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关键词
PARP-1; Inhibitors; Fluorine atom; Benzimidazole; Antitumor;

机译：PARP-1;抑制剂;氟原子;苯并咪唑;抗肿瘤;

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1. Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors [J] . Wang Junwei, Wang Xuyan, Li Hui, Bioorganic and Medicinal Chemistry Letters . 2016,第16期

机译：新型5-氟-1H-苯并咪唑-4-羧酰胺衍生物作为强效PARP-1抑制剂的设计，合成和生物学评价
2. Synthesis and biological evaluation of piperidyl benzimidazole carboxamide derivatives as potent PARP-1 inhibitors andantitumor agents [J] . Xinwei Zhang, Cunlong Zhang, Lin Tang, 中国化学快报（英文版） . 2020,第001期

机译：哌啶基苯并咪唑羧酰胺衍生物作为强效PARP-1抑制剂和抗肿瘤剂的合成及生物学评价
3. Design, synthesis and biological evaluation of novel imidazo[4,5-c] pyridinecarboxamide derivatives as PARP-1 inhibitors [J] . ZhuQ., WangX., ChuZ., Bioorganic and Medicinal Chemistry Letters . 2013,第7期

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Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors

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