2098546-05-3Relevant academic research and scientific papers
BENZOFURAN DERIVATIVE, PREPARATION METHOD THEREOF AND USE THEREOF IN MEDICINE
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, (2018/10/11)
The present invention relates to a benzofuran derivative, a preparation method thereof and a use thereof in medicine. In particular, the present invention relates to the benzofuran derivative as shown by general formula (I), the preparation method thereof, a pharmaceutical composition containing the derivative, and uses thereof as an EZH2 inhibitor and in the prevention and/or treatment of diseases such as tumours and cancers, etc., and in particular uses thereof in the prevention and/or treatment of non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, follicular lymphoma and synovial sarcoma, wherein the definitions of the substituents in the general formula (I) are the same as those defined in the description.
Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma
Lu, Biao,Shen, Xiaodong,Zhang, Lei,Liu, Dong,Zhang, Caihua,Cao, Jingsong,Shen, Ru,Zhang, Jiayin,Wang, Dan,Wan, Hong,Xu, Zhibin,Ho, Ming-Hsun,Zhang, Minsheng,Zhang, Lianshan,He, Feng,Tao, Weikang
, p. 98 - 102 (2018/02/19)
A novel series of benzofuran derived EZH2 inhibitors were discovered through a scaffold hopping approach based on the clinical compound of EPZ-6438. Further rational structure-activity relationship exploration and optimization led to the discovery of more potent EZH2 inhibitors with oral bioavailability in mice and rats. A lead compound EBI-2511 (compound 34) demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations.
