Wang, Junwei; Wang, Xuyan; Li, Hui; Ji, Dezhong; Li, Yuyan; Xu, Yungen; Zhu, Qihua published the artcile< Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors>, Safety of 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is fluorobenzimidazolecarboxamide preparation PARP1 inhibitor anticancer potentiation; Antitumor; Benzimidazole; Fluorine atom; Inhibitors; PARP-1.
Novel 5-fluorobenzimidazole-4-carboxamides were designed and synthesized. All target compounds were evaluated for their PARP-1 inhibitory activity. Compounds possessed high intrinsic PARP-1 inhibitory potency and were evaluated by in vitro cellular assays to measure their growth inhibitory activity as single agents against human colon cancer cell line HCT116 and their potentiation effect toward cytotoxic agent temozolomide (TMZ) against cancer cell line A549. One compound 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).
Bioorganic & Medicinal Chemistry Letters published new progress about Alveolar carcinoma. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Safety of 1-Boc-4-(4-Formylphenyl)piperazine.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics