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Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-02-01 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00437 Biao Lu 1 , Xiaodong Shen 1 , Lei Zhang 1 , Dong Liu 2 , Caihua Zhang 1 , Jingsong Cao 2 , Ru Shen 2 , Jiayin Zhang 2 , Dan Wang 1 , Hong Wan 1 , Zhibin Xu 1 , Ming-Hsun Ho 1 , Minsheng Zhang 2 , Lianshan Zhang 1 , Feng He 1 , Weikang Tao 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-02-01 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00437 Biao Lu 1 , Xiaodong Shen 1 , Lei Zhang 1 , Dong Liu 2 , Caihua Zhang 1 , Jingsong Cao 2 , Ru Shen 2 , Jiayin Zhang 2 , Dan Wang 1 , Hong Wan 1 , Zhibin Xu 1 , Ming-Hsun Ho 1 , Minsheng Zhang 2 , Lianshan Zhang 1 , Feng He 1 , Weikang Tao 1
Affiliation
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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.
中文翻译：
EBI-2511的发现：一种用于治疗非霍奇金淋巴瘤的高效有效口服EZH2抑制剂
通过基于临床化合物EPZ-6438的脚手架跳跃方法发现了一系列新的苯并呋喃衍生的EZH2抑制剂。进一步的合理的构效关系的探索和优化导致了在小鼠和大鼠中发现具有口服生物利用度的更有效的EZH2抑制剂。铅化合物EBI-2511（化合物34）在小鼠Pfeiffer肿瘤异种移植模型中显示出出色的体内功效，并且正在临床前开发中，用于治疗与EZH2突变相关的癌症。
更新日期：2018-02-01
中文翻译：
EBI-2511的发现：一种用于治疗非霍奇金淋巴瘤的高效有效口服EZH2抑制剂
通过基于临床化合物EPZ-6438的脚手架跳跃方法发现了一系列新的苯并呋喃衍生的EZH2抑制剂。进一步的合理的构效关系的探索和优化导致了在小鼠和大鼠中发现具有口服生物利用度的更有效的EZH2抑制剂。铅化合物EBI-2511（化合物34）在小鼠Pfeiffer肿瘤异种移植模型中显示出出色的体内功效，并且正在临床前开发中，用于治疗与EZH2突变相关的癌症。
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