Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369758 | Bioorganic & Medicinal Chemistry Letters | 2016 | 6 Pages |
Abstract
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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Junwei Wang, Xuyan Wang, Hui Li, Dezhong Ji, Yuyan Li, Yungen Xu, Qihua Zhu,