7505-81-9Relevant articles and documents
Discovery of Novel Polycyclic Heterocyclic Derivatives from Evodiamine for the Potential Treatment of Triple-Negative Breast Cancer
Chen, Zhe-Sheng,Li, Dahong,Qiu, Yangyi,Wu, Liang,Xu, Jinyi,Xu, Shengtao,Yang, Dong-Hua,Yao, Hong,Zhou, Manzhen
, p. 17346 - 17365 (2021/12/09)
Evodiamine (Evo) is a quinazolinocarboline alkaloid found in Evodia rutaecarpa and exhibits moderate antiproliferative activity. Herein, we report using a scaffold-hopping approach to identify a series of novel polycyclic heterocyclic derivatives based on Evo as the topoisomerase I (Top1) inhibitor for the treatment of triple-negative breast cancer (TNBC), which is an aggressive subtype of breast cancer with limited treatment options. The most potent compound 7f inhibited cell growth in a human breast carcinoma cell line (MDA-MB-231) with an IC50 value of 0.36 μM. Further studies revealed that Top1 was the target of 7f, which directly induced irreversible Top1-DNA covalent complex formation or induced an oxidative DNA lesion through an indirect mechanism mediated by reactive oxygen species. More importantly, in vivo studies showed that 7f exhibited potent antitumor activity in a TNBC-patient-derived tumor xenograft model. These results suggest that compound 7f deserves further investigation as a promising candidate for the treatment of TNBC.
Synthesis and docking studies of a novel tetrahydroquinazoline derivative as promising scaffold for acetylcholine esterase inhibition
Alsuhaimat, Rawan A.,Abualassal, Qais,Abudayeh, Zead Helmi,Ebada, Sherif S.,Albohy, Amgad
, p. 4797 - 4804 (2020/12/25)
Alzheimer's disease (AD) is one of the most prevalent neurodegenerative disorders. While pathological hallmarks of this disorder are known, the exact cause of AD remains unclear. Quinazoline was found to be a promising scaffold for the design and developm
Metal-free oxidative synthesis of quinazolinones via dual amination of sp3 C-H bonds
Zhao, Dan,Wang, Teng,Li, Jian-Xin
, p. 6471 - 6474 (2014/06/09)
A novel metal-free synthesis of quinazolinones via dual amination of sp3 C-H bonds was developed. The sp3 carbon in methylarenes or adjacent to a heteroatom in DMSO, DMF or DMA was used as the one carbon synthon. This journal is the Partner Organisations 2014.