Convenient preparation of pinometostat and related 5′-deoxy-5′-amino adenosine derivatives as well as their activity against DOT1L |
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| Authors: | Tongchao Liu Huanming Ren Cong Li Guohua Chen Maosheng Cheng Dongmei Zhao Jingkang Shen Jia Li Yubo Zhou Bing Xiong Yue-Lei Chen |
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| Institution: | 1. Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Lu, Shenyang 110016, PR China;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China;3. The National Center for Drug Screening, 189 Guoshoujing Road, Shanghai 201203, PR China;4. School of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;5. University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing 100049, PR China |
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| Abstract: | From adenosine and 2′-C-Me adenosine, a 3-step route towards nucleoside DOT1L inhibitors, including pinometostat, EPZ5677, and FED1, was established. With useful structural-activity relationship information, the newly prepared 2′-C-Me adenosine derivatives contribute to the limited repertoire of ribose-modified nucleoside DOT1L inhibitors. In general, this new synthetic method will facilitate not only the study of nucleoside DOT1L inhibitors, but also the synthetic and medicinal chemistry research of 5′-deoxy-5′-amino adenosine derivatives. |
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| Keywords: | DOT1L inhibitor Pinometostat Amination 5′-Deoxy-5′-amino adenosine derivative Structure activity relationship |
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