92944-77-9Relevant academic research and scientific papers
Copper-Catalyzed Oxidative Cyclization of 2-Aminobenzamide Derivatives: Efficient Syntheses of Quinazolinones and Indazolones
Duraisamy, Tamilselvan,Govindan, Karthick,Jayaram, Alageswaran,Lin, Wei-Yu,Senadi, Gopal Chandru
supporting information, (2021/12/02)
A simple copper-catalyzed assembly to formulate quinazolinone and indazolone derivatives in a single protocol manner is reported. These transformations are based on the fact that DMF can serve as a reaction solvent and one carbon synthon for the construct
N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation
Li, Junfang,Hu, Xiaoling,Luo, Tian,Lu, Yingmei,Feng, Yiyue,Zhang, Honghua,Liu, Dan,Fan, Xiaohong,Wang, Yuqing,Jiang, Liming,Wang, Yuying,Hao, Xiangyong,Shi, Tao,Wang, Zhen
, (2021/09/20)
Glioblastoma is one of the most lethal brain tumors. The crucial chemotherapy is mainly alkylating agents with modest clinical success. Given this desperate need and inspired by the encouraging results of a phase II trial via concomitant Topo I inhibitor plus COX-2 inhibitor, we designed a series of N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents based on structure modification on 1,5-naphthyridine derivatives (Topo I inhibitors). Notably, the target compounds I-1 (33.61 ± 1.15 μM) and I-8 (45.01 ± 2.37 μM) were confirmed to inhibit COX-2, while a previous reported compound (1,5-naphthyridine derivative) resulted nearly inactive towards COX-2 (IC50 > 150 μM). Besides, I-1 and I-8 exhibited higher anti-proliferation, anti-migration, anti-invasion effects than the parent compound 1,5-naphthyridine derivative, suggesting the success of modification based on the parent. Moreover, I-1 obviously repressed tumor growth in the C6 glioma orthotopic model (TGI = 66.7%) and U87MG xenograft model (TGI = 69.4%). Besides, I-1 downregulated PGE2, VEGF, MMP-9, and STAT3 activation, upregulated E-cadherin in the orthotopic model. More importantly, I-1 showed higher safety than temozolomide and different mechanism from temozolomide in the C6 glioma orthotopic model. All the evidence demonstrated that N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents could be promising for the glioma management.
The N-Aryl aminocarbonyl ortho-substituent effect in Cu-catalyzed aryl amination and its application in the synthesis of 5-substituted 11-Oxo-dibenzodiazepines
Diao, Xiaoqiong,Xu, Lanting,Zhu, Wei,Jiang, Yongwen,Wang, Haoyang,Guo, Yinlong,Ma, Dawei
supporting information; experimental part, p. 6422 - 6425 (2012/02/03)
Double amination of ortho-substituted aryl bromides proceeded under mild conditions to afford 5-substituted 11-oxo-dibenzodiazepines, which revealed that there is a strong ortho-substituent effect caused by N-aryl aminocarbonyl groups during copper-cataly
Novel alternative for the N-N bond formation through a PIFA-mediated oxidative cyclization and its application to the synthesis of indazol-3-ones
Correa, Arkaitz,Tellitu, Imanol,Dominguez, Esther,SanMartin, Raul
, p. 3501 - 3505 (2007/10/03)
The synthesis of a series of N,N′-disubstituted indazolone derivatives starting from methyl anthranilates is presented. This general approach features a novel and easy way for access to the target N-heterocycles by formation of a new N-N single bond. The
