HDAC

作品数：138被引量：297H指数：8
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相关机构：山东大学中国药科大学华中科技大学中南大学更多>>
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Design and synthesis of tri-substituted pyrimidine derivatives as bifunctional tumor immunotherapeutic agents targeting both A2A adenosine receptors and histone deacetylases
《Chinese Chemical Letters》2024年第1期295-299,共5页Ruiquan Liu Wenwen Duan Wenzhong Yan Jinfeng Zhang Jianjun Cheng 
Lingang Laboratory(No.LG-QS-202205-03);ShanghaiTech University and the Shanghai Municipal Government.
The A_(2A)adenosine receptor(A_(2A)AR)has attracted attention as an emerging immunotherapeutic target with several antagonists being evaluated in clinical trials.However,A_(2A)AR antagonists show limited efficacy as m...
关键词：BIFUNCTIONAL A_(2A)AR antagonism HDAC inhibition Cancer IMMUNOTHERAPY 
Design, synthesis and antitumor evaluations of nucleoside base hydroxamic acid derivatives as DNMT and HDAC dual inhibitors
《Chinese Chemical Letters》2021年第8期2479-2483,共5页Qinsheng Sun Qiuzi Dai Cunlong Zhang Yan Chen Lei Zhao Zigao Yuan Yuyang Jiang 
financial supports from China Postdoctoral Science Foundation (No.2018M631825);Shenzhen Development and Reform Committee (No.2019156);Shenzhen Science,Technology and Innovation Commission (No.JCYJ20180306174248782);Department of Science and Technology of Guangdong Province (No.2017B030314083);Shenzhen Bay Laboratory Open Funding (No.SZBL2019062801009)。
DNA methyl transferase(DNMT) and histone deacetylase(HDAC) are well recognized epigenetic targets for discovery of antitumor agents.In this study,we designed and synthesized a series of nucleoside base hydroxamic acid...
关键词：EPIGENETIC DNMT HDAC Multitarget Antitumor bioactivity 
Combined inhibition of HDAC and DNMT1 induces p85α/MEKmediated cell cycle arrest by dual target inhibitor 208 in U937 cells
《Chinese Chemical Letters》2019年第6期1233-1236,共4页Yue Ren Qinsheng Sun Zigao Yuan Yuyang Jiang 
financial supports from Shenzhen Development and Reform Committee(No. 20151961);China Postdoctoral Science Foundation(No. 2018M631825);Department of Science and Technology of Guangdong Province (No. 2017B030314083)
Multiple histone deacetylase inhibitors (HDACi) and DNA methyltransferase inhibitors (DNMTi) have been developed for cancer therapy. However, the research on their mechanisms of action is not sophisticated enough. In ...
关键词：Proteomics Epigenetic INHIBITOR HDAC DNMT1 Cell cycle ARREST 
Discovery of ErbB/HDAC inhibitors by combining the core pharmacophores of HDAC inhibitor vorinostat and kinase inhibitors vandetanib,BMS-690514,neratinib,and TAK-285
《Chinese Chemical Letters》2017年第6期1220-1227,共8页Chao Ding Dan Li Yan-Wei Wang Sai-Sai Han Chun-Mei Gao Chun-Yan Tan Yu-Yang Jiang 
supported by funding from the National Natural Science Foundation of China(No.21272134);Shenzhen Municipal Government(No.CXB201104210014A and20150113A0410006)
By combining the core pharmacophores of HDAC inhibitor vorinostat and kinase inhibitors vandetanib,BMS-690514,neratinib,and TAK-285 with 1,2,3-triazole as linker,eight novel 6-substituted-4-aminoquinazolin derivatives...
关键词：Anticancer Kinase HDAC Multitarget Selectivity 
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