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陈悦,男,汉族, 南开大学化学学院教授、博士生导师,药物化学生物学国家重点实验室 PI。国家“千人计划”;海外高层次人才;国家杰出青年科学基金获得者;教育部新世纪优秀人才支持计划;霍英东教育基金会高等院校青年教师基金应用研究课题资助获得者;天津市“131” 创新型人才培养工程第一层次;天津市杰出人才; 天津市创新人才推进计划重点领域创新团队负责人;天津市技术发明奖一等奖;南开大学“百名青年学术带头人”。
1、 国家自然科学基金面上项目,82273794、基于天然产物cyclotheonellazole A药效团设计与合成急性肺损伤治疗药物的研究、51万、2023/01-2026/12、在研、主持。
2、 国家自然科学基金面(NSFC-广东联合基金),U1801288,靶向新型癌基因metadherin的抗肾纤维化新药研发、2019/01-2022/12、 245万、结题、主持。
3、 国家杰出青年科学基金, 81625021、癌症干细胞的药物化学、2017/01-2021/12、350万、结题、主持。
4、 国家自然科学基金面上项目,81573282、抗肺癌症干细胞天然产物葫芦素I的全合成及构效关系研究、2016/01-2019/12、81.2万元、结题、主持。
5、 国家自然科学基金面上项目,21372129、抗癌症干细胞天然产物RakicidinA的合成及构效关系研究、2014/01-2017/12、80万元、结题、主持。
6、 国家自然科学基金面上项目,21072106、抗癌症干细胞的小白菊内酯的全合成及其构-效关系初探、2011/01-2013/12、36万元、结题、主持。
近5年发表论文:
1. TieshunRen, Ke Lv, Fangzhong Hu and Yue Chen * . Total syntheses of Kavaratamide A and5-epi-Kavaratamide A†. Org. Biomol. Chem. 2025, 23, 1569–157381.
2.Xiuhe Zhao , Xiaonan Xi ,* Mingxiao Zhang, Mengxue Lv, Xiang Zhang, Yaxin Lu,Liang Wang,* and Yue Chen.* Structure-ActivityRelationship Study of Majusculamide D: Overcoming Metabolic Instability andSevere Toxicity with a Fluoro Analogue, Mar. Drugs 2024, 22, 537-550
3. Bolin Chen,Xijing Zhang,Yufen Yang,Dongdong Xu,Qianwei Wu,Shibo Wang,Shiqi Bao,Xuemei Zhang,Yahui Ding,*Liang Wang*Yue Chen.*Hypocretenolides: Collective TotalSyntheses and Activities toward Metastatic Colon Cancer, Chem. Sci. 2024, Mar28;15(17), 6397-6401.
4. Qing Meng, Jianshuang Guo, KeLv, Yang Liu, Jin Zhang, Mingyue Li, Xirui Cheng, Shenghua Chen, Xiaoguang Huo,Quan Zhang*, Yue Chen*, Jing Li*, 5S-Heudelotinonealleviates experimental colitis by shaping the immune system and enhancing theintestinal barrier in a gut microbiotadependent manner, ActaPharmaceutica Sinica B, 2024,14(5):2153-2176
5. Xiuhe Zhao, Mengxue Lv, XiaonanXi, Yaxin Lu, Liang Wang*, and Yue Chen*, Synthesis of Anti-PancreaticCancer Natural Product Majusculamide D and Analogues Reveals a reliminaryStructure–Activity Relationships, Chin. J. Chem. 2024, 42,605-610
6. BolinChen, Yufen Yang, Xijing Zhang, Dongdong Xu, Yuanjun Sun,* Yue Chen,*and Liang Wang* , Total Syntheses of Brassicicenes A, R, and T, Org Lett.2023, 25(48), 8570-8574.
7. SenZhang, Songming Zhang, Yunlong Fan, Xuhai Zhang, Jing Chen, Chaofan Jin, SisiChen, Liang Wang,* Quan Zhang,* and Yue Chen*, Total Synthesis of theProposed Structure of Neaumycin B, Angew Chem Int Ed. 2023, 62(51):e202313186.
8. Liang Li,Pengfei Li, Tianhao Li, Mingxiao Zhang, Wenjie Liu, Jing Li, Liang Wang*, YueChen*, Synthesis of the ABC Ring System of Kadlongilactones†, OrgBiomol Chem. 2023, 1(8),1704-1708
9. Jianshuang Guo, Kaihui Liu, Jiyan Wang, Hao Jiang,Mengyi Zhang, Yang Liu, Changliang Shan , Fangzhong Hu, Wenzheng Fu, ChunzeZhang , Jing Li ,*, Yue Chen ,* A rational foundation for micheliolide-basedcombination strategy by targeting redox and metabolic circuit in cancer cells,Biochem Pharmacol. 2022, 200:115037
10. Lei Wang, Xiu-Juan Zhao, Chuang Hua, Hai-Xiang Wu, Cui-Gai Bai*, YueChen*, Synthesis of ponatinib analogues as novel inhibitors of leukemiastem cells, Future. Med.Chem. 2022, 14(9):623-645
11. Bolin Chen, Qianwei Wu, Dongdong Xu, XijingZhang, Yahui Ding, Shiqi Bao, Xuemei Zhang,Liang Wang,* Yue Chen.* ATwo-phase Approach to Fusicoccane Synthesis To Uncover a Compound That ReducesTumourigenesis in Pancreatic Cancer Cells. Angew. Chem. Int. Ed. 2022,61, e202117476.
12. Can Liu, LiangWang,* Yuanjun Sun, Xiuhe Zhao, Tianyang Chen, Xiuwen Su, Hui Guo, Qin Wang,Xiaonan Xi, Yahui Ding,* Yue Chen.* Probe Synthesis Reveals EukaryoticTranslation Elongation Factor 1 Alpha 1as the Anti-Pancreatic Cancer Target of BE-43547A2. Angew. Chem. Int. Ed. 2022,61, e202206953.
13. Yingjun Cui,Mengyi Zhang, Honglei Xu, Tingrong Zhang, Songming Zhang, Xiuhe Zhao, Peng Jiang,Jing Li,* Baijun Ye, Yuanjun Sun, Mukuo Wang, Yangping Deng, Qing Meng, YangLiu, Qiang Fu, Liang Wang,* Yue Chen.* ElastaseInhibitor Cyclotheonellazole A: Total Synthesis and In Vivo 2 BiologicalEvaluation for Acute Lung Injury. J. Med. Chem. 2022, 65(4), 2971-2987.
14. Yahui Ding; Xiaoping Chen; Can Liu; Weizhi Ge; Qin Wang; Xin Hao;Mengmeng Wang; Yue Chen*; Quan Zhang*. Identifcation of a small moleculeas inducer of ferroptosis and apoptosis through ubiquitination of GPX4 intriple negative breast cancer cells. Journal of Hematology and Oncology,2021, 14: 19
15. Tingrong Zhang; Shaojie Miao; Mingxiao Zhang;Wenjie Liu; Liang Wang*; Yue Chen*. Optimization of Two Steps inScale-Up Synthesis of Nannocystin A. Marine Drugs, 2021, 19: 198.
16. Fangzhi Han; GuangjuLiu; Xuhai Zhang; Yahui Ding; Liang Wang; Yijing Wu; Yue Chen*; Zhang Quan*. Total Synthesis and Structure Revision ofBoholamide A. Organic Letters, 2021, 23: 4976-4980
17. Fangzhi Han; Guangju Liu; Chaofan Jin; Jinghan Wang; JianweiLiu; Liang Wang*; Yue Chen*.Total Synthesis and Determination of theAbsolute Configuration of Rakicidin C. Org. Lett.2021,23(18),7069-7073
18. Junhong Xiang, Xuemei Zhang, Dehong Wang,Jiaxin Li, Qiuying Li, Qin Wang, Yahui Ding,* Tianyang Chen, Yuanjun Sun, ShiqiBao, Jing Chen, Dongmei Li, Liang Wang* and Yue Chen * Chemicalmodification of ovatodiolide revealed a promising amino-prodrug with improved pharmacokineticprofile. Chem.Commun., 2020, 56,11018--11021
19.Yahui Ding, Qingqing Xue, Shuo Liu, Kai Hu, Da Wang, Tianpeng Wang, Ye Li, HongyuGuo, Xin Hao, Weizhi Ge, Yan Zhang, Ang Li, Jing Li, * Yue Chen, *Quan Zhang*.Identification ofParthenolide Dimers as Activators of Pyruvate Kinase M2 in Xenografts ofGlioblastoma Multiforme In Vivo. J. Med. Chem. 2020, 63, 1597-1611.
20. Xiaonan Xi, Yahui Chu, Ning Liu , Qianqian Wang, Zheng Yin, YaxinLu* and Yue Chen * . Jointbioinformatics analysis of underlying potential functionsof hsa-let-7b-5p and core genes in human glioma. J Transl Med, 2019, 17:129
21.Junhong Xiang, Yahui Ding,* Jiaxin Li, XiuheZhao, Yuanjun Sun, Da Wang, Liang Wang,* Yue Chen*. Ovatodiolides:Scalable Protection-free Syntheses, Configuration Determination and BiologicalEvaluation against Hepatic Cancer Stem Cells. Angew. Chem. Int. Ed. 2019,58, 10587-10590.
22. Yahui Ding, # ShengzuLi, # Weizhi Ge, Zhongquan Liu, Xuhai Zhang, Mengmeng Wang, TianyangChen, Yue Chen,* Quan Zhang*. Design and Synthesis of Parthenolide and 5-Fluorouracil Conjugatesas Potential Anticancer Agents against Drug Resistant Hepatocellular Carcinoma.Eur. J. Med. Chem. 2019, 183, 111706.
23. JunhongXiang, Xiuhe Zhao, Jiaxin Li, Yahui Ding,* Chao Wang, Liang Wang,* Yue Chen*. Rapid Construction of theScaffold of Quorumolide A Enabled by a Tandem ROM/RCM Strategyand a Tandem Oxidative Cyclization Strategy. Org. Lett. 2019, 211, 66485-6487.
24. YuanjunSun, Ruifei Zhou, Honglei Xu, Xiuwen Su, Dehong Wang, Chao Wang, Yahui Ding, LiangWang*, Yue Chen* Syntheses andbiological evaluation of BE-43547A2 analogues modified at O35 esterand C15-OH sites. Tetrahedron 2019,75, 1808-1818. (InvitedPaper, Special Issue, In Meomory of Weishan Zhou).
25. Weizhi Ge,Xin Hao, Fangzhi Han, Zhongquan Liu, Tianpeng Wang, Ning Chen, Yahui Ding*, YueChen*, Quan Zhang*. Synthesis and structure-activity relationship studiesof parthenolide derivatives as potential anti-triple negative breast canceragents. Eur. J. Med. Chem., 2019,166, 445-469.
新药研发:
陈悦教授作为第一发明人研发的候选药物ACT001具有抗多种癌症干细胞作用,核心品种ACT001用于恶性颅内肿瘤及自身免疫性疾病,曾获得国家十二五、十三五科技重大专项、各级政府科技人才项目; 目前ACT001在全球开展了十多项临床试验,包括1项2b/3期临床。到目前为止,获得了美国FDA在48小时内批准的单一患者临床试验,并收到中国香港及海外十多家医院的同情赠药申请。ACT001因此获得3项欧美孤儿药资格,并于2021年获得美国FDA批准的儿童罕见病资格,是我国获得该资质的首个品种,《参考消息》于同年11月报道了该事实,2023年12月又获得美国FDA批准的快速通道资格,创造了中国新药研发的里程碑。2025年1月ACT001被中国CDE纳入“突破性治疗品种”名单。
第一发明人研发的另一新药ACT004, 已在澳洲开展临床1期试验。
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