陈益华

1997-2001年，南昌大学，化学系，学士

2001-2006年，中国科学院上海药物研究所，药物化学，博士，导师：南发俊 研究员

2006-2009年，University of Illinois at Chicago，药物化学，博士后，合作导师：Alan P. Kozikowski 教授

2022.12-至今，华东师范大学，上海市调控生物学重点实验室，教授，博士生导师

2015.12-2022.12，华东师范大学，上海市调控生物学重点实验室，研究员，博士生导师。

 2009.12 -2015.12，华东师范大学，上海市调控生物学重点实验室，副教授

中国药学会老年药学专业委员会委员

中国药理学会化疗药理专业委员会委员

中国抗癌协会肿瘤微环境专委会青年委员会委员

中国药学会《药学学报》中英两刊（药学学报、Acta Pharmaceutica Sinica B）青年编委

中国化学会《Chinese Chemical Letters》青年编委

Anti-cancer Agents in Medicinal Chemistry, Editorial Board Member

化学生物学、药物化学。

靶向关键转录因子的抗肿瘤药学

现代药学概论（本科生）

有机药物波谱分析（研究生）

主持：

1) 国家自然科学基金面上项目：81973160,Myoferlin蛋白小分子抑制剂的发现与活性评价,2020/01-2023/12，在研。

2）国家自然科学基金面上项目：81673304，USP15选择性抑制剂的设计、合成与优化及其抗肿瘤活性研究，2017/01-2020/12，已结题。

3）国家自然科学基金青年基金： 81202407，具有TGFbeta受体激酶抑制活性的咔啉类化合物结构优化及抗肿瘤转移功能研究，2013/01-2015/12，已结题。

4）上海市“科技创新行动计划”生物医药领域科技支撑项目：21S11907800，靶向STAT3的抗胰腺癌候选药物YY002的临床前研究，2021/08-2024/07，在研。

5）上海市“科技创新行动计划”生物医药领域科技支撑项目：15431902200，泛素特异性蛋白酶特异性抑制剂的发现、结构优化及其抗肿瘤作用研究，2015/07月-2018/06，已结题。

6）教育部博士点基金（新教师类）：20120076120029，一类新型HDAC抑制剂的构效关系及抗肿瘤作用评价，2013/01-2015/12，已结题。

7）横向合作课题：靶向KRAS药物发现，2021/07-2023/06，在研。

科研论文（近五年）与专利：

2023年：

1)    Peng He, Juanjuan Feng, Xinting Xia, Yue Sun, Jia He, Tian Guan, Yangrui Peng, Xueli Zhang, Mingyao Liu, Xiufeng Pang*, and Yihua Chen*. Discovery of a Potent and Oral Complex I OXPHOS Inhibitor that Abrogates Tumor Growth and Circumvents MEKi Resistance. J. Med. Chem. 2023, 66, 6047-6069.

2)    Jia He, Luzhen Wang, DaZhao Mi, Tian Guan, Wenjing Liu, Peng He, Haijun Gu, Yuzhan Li, Yangrui Peng, Ai-Qun Jia, Ceshi Chen*, and Yihua Chen*. Discovery of Pyrimidinediamine Derivatives as Potent Methuosis Inducers for the Treatment of Triple-Negative Breast Cancer. J Med. Chem. 2023, 66, 7421-7437.

3)   Haijun Gu, Ting Zhang, Tian Guan, Min Wu, Shen Li, Yunqi Li, Mengmeng Guo, Lin Zhang, Yangrui Peng, Dazhao Mi, Mingyao Liu, Zhengfang Yi,* and Yihua Chen*. Discovery of a Highly Potent and Selective MYOF Inhibitor with Improved Water Solubility for the Treatment of Gastric Cancer. J. Med. Chem. 2023,  doi: 10.1021/acs.jmedchem.3c01639.

4)    Dazhao Mi, Yuzhan Li, Haijun Gu, Yan Li, and Yihua Chen*. Current Advances of Small Molecule E3 Ligands for Proteolysis-Targeting Chimeras Design. Eur. J.  Med. Chem. 2023, 256, 115444. (Cover Story)

5)   Luzheng Wang, Dazhao Mi, Jinhui Hu, Wenjing Liu, Yi Zhang, Chunyan Wang*, Yihua Chen*, Ceshi Chen*. A novel methuosis inducer DZ-514 possesses antitumor activity via activation of ROS-MKK4-p38 axis in triple negative breast cancer. Cancer Lett.2023,555, 216049.

6)    Huang Chen, Wenbo Zhou, Aiwu Bian, Qiansen Zhang, Ying Miao, Xuan Yin, Jiangnan Ye, Shifen Xu, Chaowen Ti, Zhenliang Sun, Jianghua Zheng, Yihua Chen*, Mingyao Liu*, Zhengfang Yi*. Selectively targeting STAT3 using a small molecule inhibitor is a potential therapeutic strategy for pancreatic cancer. Clin. Cancer Res. 2023, 29, 815-830.

7)   Yuzhu Zhang, Jing Chen, Dazhao Mi, Jun Ling, Huachao Li, Peng He, Ning Liu3, Qianjun Chen*, Yihua Chen*, Luqi Huang*. Discovery of YH677 as a cancer stemness inhibitor for suppressing triple-negative breast cancer growth and metastasis by regulating the TGFβ signaling pathway. Cancer Lett., 2023, 560, 216142.

8)   Dazhao Mi, Yuzhan Li and Yihua Chen*. Small-Molecule Modulators Targeting SHP2 for Cancer Therapy. Anti-Cancer Agents Med. Chem.2023, 23, 498-504.

9)   Weikai Guo, Manjie Wang, Zhengfan Yang, Danyang Liu, Borui Ma, Yanqun Zhao, Yihua Chen*, and Yanzhong Hu*. Recent advances in small molecule and peptide inhibitors of glucose-regulated protein 78 for cancer therapy. Eur. J.  Med. Chem. 2023, 261, 115792.

10)  Lin Zhang, Min Wu, Weikai Guo, Shuangshuang Zhu, Shen Li, Shiyi Lv, Yan Li, Layang Liu, Yajing Xing, Huang Chen, Mingyao Liu, Shihong Peng*, Yihua Chen*, Zhengfang Yi*. A small molecule BCL6 inhibitor as chemosensitizers in acute myeloid leukemia. Biomedicine & Pharmacotherapy, 2023, 166, 115358.

11)  Yali Wang, Wenbo Zhou, Jianfeng Chen, Jinghong Chen, Peng Deng, Huang Chen, Yichen Sun, Zhaoliang Yu, Diwen Pang, Lizhen Liu, Peili Wang, Jing Han Hong, Bin Tean Teh, Huiqiang Huang, Wenyu Li, Zhengfang Yi, Soon Thye Lim, Yihua Chen, Choon Kiat Ong, Mingyao Liu*, and Jing Tan*. Preclinical characterization of WB737, a potent and selective STAT3 inhibitor, in natural killer/T-cell lymphoma. MedComm,2023, 4, e284. (Cover Story)

2022年：

12) Haixiang Pei, Weikai Guo, Yangrui Peng, Hai Xiong, Yihua Chen*. Targeting Key Proteins involved in Transcriptional Regulation for Cancer Therapy: Current Strategies and Future Prospective. Med. Res. Rev.2022,42, 1607-1660.

13)  Wangrui Jin, Tao Zhang, Wenbo Zhou, Peng He, Yue Sun, Shijia Hu, Huang Chen, Xinglong Ma, Yangrui Peng, Zhengfang Yi, Mingyao Liu, Yihua Chen*. Discovery of 2-Amino-3-cyanothiophene Derivatives as Potent STAT3 Inhibitors for the Treatment of Osteosarcoma Growth and Metastasis. J. Med. Chem.2022, 65, 6710-6728.

14)  Peng He, Ying Miao, Yue Sun, Aiwu Bian, Wangrui Jin, Huang Chen, Jiangnan Ye, Jia He, Yangrui Peng, Haijun Gu, Mingyao Liu, Zhengfang Yi*, and Yihua Chen*. Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr⁷⁰⁵/Ser⁷²⁷ Inhibitory Activity for Gastric Cancer Treatment. J. Med. Chem.2022, 65, 12650-12674.

15)  Peng He, Aiwu Bian, Ying Miao, Wangrui Jin, Huang Chen, Jia He, Liting Li, Yue Sun, Jiangnan Ye, Mingyao Liu, Zhengfang Yi*, Wenbo Zhou*, and Yihua Chen*. Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer treatment. J. Med. Chem.2022, 65, 15487-15511.

16)   Haijun Gu, Jia He, Yuzhan Li, Dazhao Mi, Tian Guan, Weikai Guo, Bo Liu* and Yihua Chen*. B‑cell lymphoma 6 inhibitors: current advances and prospects of drug development for diffuse large B-cell lymphomas. J. Med. Chem.2022, 65, 15559-15583.

17)  Yuzhu Zhang, Dazhao Mi and Yihua Chen*.An instructive attempt on developing aptamer-constructed PROTAC for potential breast cancer treatment. Molecular Therapy - Nucleic Acids. 2022, 30, 351-352.

18)  Haijun Gu, Ting Zhang, Yunqi Li, Yuan He, Tian Guan, Weiqiong Kan, Peng He, Zhengfang Yi, Yihua Chen*. Discovery of 1,5-diaryl-1,2,4-triazole derivatives as MYOF inhibitors and its antitumor effects in pancreatic cancer. Future Med. Chem.2022, 14,1425-1440.

19)  Shijia Hu, Yunqi Li, Weiqiong Kan, Tingting Ding, Haijun Gu, Ting Zhang Zhengfang Yi, Yihua Chen*.Novel ortho-diphenyl-five-member N-hetero- aromatics compounds as potent anti-cancer cell agents. Med. Chem. Res., 2022, 31, 936-948.

20) Haixiang Pei, Yihua Chen*. The promising combination therapy strategy for overcoming resistance to histone deacetylase inhibitors in diffuse large B-cell lymphoma. Clin. Trans. Discovery, 2022, 2, e56.

21)  Yajing Xing, Weikai Guo, Min Wu, Jiuqing Xie, Dongxia Huang, Pan Hu, Miaoran Zhou, Lin Zhang, Qiansen Zhang, Peili Wang, Xin Wang, Guixue Wang, Huangan Wu, Cili Zhou, Yihua Chen, Mingyao Liu, Zhengfang Yi, Zhenliang Sun. An orally available small molecule BCL6 inhibitor effectively suppresses diffuse large B cell lymphoma cells growth in vitro and in vivo. Cancer Lett.2022, 529, 100-111.

2021年：

22)  Yuan He, Weiqiong Kan, Yunqi Li, Yun Hao, Anling Huang, Haijun Gu, Minna Wang, Qingqing Wang, Jinlian Chen, Zhenliang Sun, Mingyao Liu*, Yihua Chen*, Zhengfang Yi*. A potent and selective small molecule inhibitor of myoferlin attenuates colorectal cancer progression. Clin. Trans. Med.2021, 11, e289.

2020年：

23) Qingxiang Lin, Yuan He, Xue Wang, Yong Zhang, Meichun Hu, Weikai Guo, Yundong He, Tao Zhang, Li Lai, Zhenliang Sun, Zhengfang Yi,* Mingyao Liu* andYihua Chen*. Targeting Pyruvate Carboxylase by a Small Molecule Suppresses Cancer Progression. Adv. Sci. 2020, 7, 1903483.

24)  Liang Li, Dazhao Mi, Haixiang Pei, Qiuhui Duan, Xinyue Wang, Wenbo Zhou, Jianping Jin, Dali Li, Mingyao Liu* and Yihua Chen*. In vivo target protein degradation induced by PROTACs based on E3 ligase DCAF15. Signal Trans. Targeted Therapy.2020, 5, 129.

25)  Weikai Guo, Yajing Xing, Qiansen Zhang, Jiuqing Xie, Dongxia Huang, Haijun Gu, Peng He, Miaoran Zhou, Shifen Xu, Xiufeng Pang, Mingyao Liu,* Zhengfang Yi,* Yihua Chen*. Synthesis and Biological Evaluation of B‑Cell Lymphoma 6 Inhibitors of N-phenyl-4-pyrimidinamine Derivatives Bearing Potent Activities against Tumor Growth. J. Med. Chem. 2020, 63, 676-695.

26)  Kewen Hu, Kun Li, Jing Lv, Jie Feng, Jing Chen, Haigang Wu, Feixiong Cheng, Wenhao Jiang, Jieqiong Wang, Haixiang Pei, Paul J. Chiao, Zhenyu Cai, Yihua Chen*, Mingyao Liu*, Xiufeng Pang*. Suppression of the SLC7A11/glutathione axis causes synthetic lethality in KRAS-mutant lung adenocarcinoma. J. Clin. Invest. 2020, 130, 1752-1766.

27) Tingting Fan, Weikai Guo, Ting Shao, Wenbo Zhou, Pan Hu, Mingyao Liu, Yihua Chen* and Zhengfang Yi*. Design, synthesis and evaluation of phenylthiazole and phenylthiophene pyrimidindiamine derivatives targeting the bacterial membrane. Eur. J. Med. Chem. 2020, 190, 112141.

28)  Feifei Yang, Na Zhao, Lina Han, Yang Yang, Di Ge*, Hua Zhang*, Yihua Chen* Synthesis and Biological Evaluation of Novel Thiophene-based N-bis-substituted Aromatic Amide Hydroxamic Acid Derivatives as Histone Deacetylase Inhibitors with Antitumor Activities. Future Med. Chem. 2020, 12, 655-672.

29)    Haijun Gu, Yangrui Peng and Yihua Chen*, An Emerging Therapeutic Approach by Targeting Myoferlin (MYOF) for Malignant Tumors. Curr. Topics Med. Chem.2020, 20, 1509-1515.

30)  Ting Shao, Wenshu Tang, Yunqi Li, Dan Gao, Kaiyang Lv, Peng He, Yajuan Song, Song Gao, Mingyao Liu*, Yihua Chen*, Zhengfang Yi*. Research on Function and Mechanisms of a Novel Small Molecule WG449E for Hypertrophic Scar. J. Eur. Acad. Dermatol., 2020, 34, 608-618.

2019年：

31) Yunqi Li, Yuan He, Ting Shao, Haixiang Pei, Weikai Guo, Dazhao Mi, Isabelle Krimm, Yuanjin Zhang, Peili Wang, Xin Wang, Mingyao Liu,* Zhengfang Yi,* Yihua Chen*. Modification and Biological Evaluation of a Series of 1,5-Diaryl-1,2,4-triazole Compounds as Novel Agents against Pancreatic Cancer Metastasis through Targeting Myoferlin. J. Med. Chem. 2019, 62, 4949-4966.

32) Liqiang Su, Jiahui Li, Zhen Zhou, Dongxia Huang, Yuanjin Zhang, Haixiang Pei, Weikai Guo, Haigang Wu, Xin Wang, Mingyao Liu, Cai-Guang Yang*, Yihua Chen*. Design, synthesis and evaluation of hybrid of tetrahydrocarbazole with 2,4-diaminopyrimidine scaffold as antibacterial agents. Eur. J. Med. Chem. 2019, 162, 203-211.

33) Haixiang Pei, Juliang Qin, Fengmian Wang, Binghe Tan, Zeda Zhao, Yangrui Peng, Fangfei Yu, Ennian Li, Mingyao Liu, Rong Zhang, Bo Liu*, Bing Du*, Yihua Chen*.Discovery of Potent Ureido Tetrahydrocarbazole Derivatives for Cancer Treatments through targeting Tumor-associated Macrophages. Eur. J. Med. Chem. 2019,183, 111741.

34) Haixiang Pei, Yangrui Peng, Qiuhua Zhao*, Yihua Chen*. Small Molecule PROTACs: An Emerging Technology for Targeted Therapy in Drug Discovery. RSC Advances, 2019, 9, 16967-16976.

35) Peng He, Wenbo Zhou, Mingyao Liu, and Yihua Chen*. Recent Advances of Small Molecular Regulators Targeting G Protein-Coupled Receptors Family for Oncology Immunotherapy. Curr. Topics Med. Chem.2019, 19, 1464-1483.

36) Feifei Yang, Na Zhao, Di Ge, Yihua Chen*, Next-Generation of Selective Histone Deacetylase Inhibitors. RSC Advances, 2019, 19571-19583.

37) Di Ge, Lina Han, Feifei Yang*, Na Zhao, Yang Yang, Hua Zhang* and Yihua Chen* Development of Hydroxamate-Based Histone Deacetylase Inhibitors of Bis-substituted Aromatic Amides with Antitumor Activities. MedChemComm, 2019, 10, 1828-1837.

38) Yang-jiong Xiao, Yang Yu, Dan Gao, Wangrui Jin, Pengcheng Jiang, Yuhong Li, Chao Wang, Yuning Song, Peng Zhan, Fei Gu, Cancan Zhang, Bin Wang, Yihua Chen*, Bing Du*, Rong Zhang*. Inhibition of CDC25B with WG-391D impedes the tumorigenesis of ovarian cancer. Frontiers in Oncology. 2019, 9, 236.

2018年：

39) Tao Zhang, Jingjie Li, Yuan He, Feifei Yang, Yun Hao, Wangrui Jin, Jing Wu, Zhenliang Sun, Yunqi Li, Yihua Chen*, Zhengfang Yi* and Mingyao Liu*. A small molecule targeting myoferlin exerts promising anti-tumor effects on breast cancer. Nat. Commun., 2018, 9, 3726.

40) Tao Zhang*, Jingjie Li, Xiaojun Ma, Yang Yang, Yuan He, Wangrui Jin, Wei Sun, Lei Wang, Yingqi Hua, Zhengfang Yi, Mingyao Liu, Yihua Chen*, Zhengdong Cai*.Inhibition of HDACs-EphA2 signaling Axis with WW437 demonstrates promising preclinical antitumor activity in breast cancer. EBioMedicine, 2018, 31, 276-286. 

第一发明人专利列表：

A.授权专利：

1)      陈益华、刘明耀、杨飞飞、张涛、易正芳、李静婕。氮原子多取代的芳香酰胺类小分子有机化合物及其衍生物、用途及其制备方法。中国发明专利，专利号：ZL201210174929.7。（已转让）

2)      陈益华、叶希韵、刘明耀、李国亮、何云东、周文波。一种芳香基噻唑类化合物及其类似物、用途及制备方法。中国发明专利号：ZL201110415182.5. （已转让）

3)      陈益华、吴婧、郁林羲、翟东、易正芳、罗剑、刘明耀。2,3-二芳香基噻唑啉酮类化合物及其在制备治疗肿瘤药物中的用途。中国发明专利号：ZL201210139633.1。（已转让）

4)      陈益华、罗剑、张勇、郑春兵、童为光、刘明耀。芳香烷酰基四氢-beta-咔啉及其衍生物在治疗代谢性疾病中的应用。中国发明专利号：ZL201210439033.7。

5)      陈益华、刘明耀、郑春兵、周文波、覃莉雯、陈华青、罗剑。芳香杂环类小分子有机化合物及衍生物、制备方法及医药用途。中国发明专利号：ZL201310429958.8.

6)      陈益华、刘明耀、李静婕、杨飞飞、易正芳、彭世鸿。含有噻唑啉酮结构的异羟肟酸类小分子有机化合物及其衍生物、用途及制备方法。中国发明专利号：ZL201410628974.4。

7)      陈益华、刘明耀、易正芳、杨飞飞、代付军。酰基吡咯类小分子有机化合物及其衍生物、用途及其制备方法。中国发明专利号：ZL201410653320.7。

8)      陈益华、刘明耀、杨洋、张涛、杨飞飞、吕方、易正芳、逄秀凤。杂环取代异羟肟酸类芳香酰胺化合物或药学上可接受的盐、及其制备方法和应用。中国发明专利号：ZL201410164011.3。

9)      陈益华，逄秀凤，胡克文，吴海刚，王洁琼，刘明耀。苯并三氮唑类化合物、制备方法和其医药用途。中国发明专利号：ZL201510672684.4。

10)  陈益华、刘明耀、郭伟凯，易正芳，林庆祥，张勇。一种芳香基-杂环取代的嘧啶二胺类化合物及其衍生物及其医药用途。中国发明专利号：ZL201510112092.7。

11)  陈益华，易正芳，李云齐，贺源，李静婕，刘明耀。1,5-二芳香基-1,2,4-三氮唑类化合物及其制药用途。中国发明专利申请号：ZL201610898072.1。

12)  陈益华、杨财广、苏立强、李佳慧、赵秋华、吴海刚、刘明耀。一类四氢咔唑类小分子有机化合物及其在制备抗菌药物中的用途及其制备方法。中国发明专利号：ZL201710819964.2。

13)  陈益华、刘明耀、周珍、肖洋炯、陈煌、易正芳、杜冰。一类哌啶并噻吩类小分子有机化合物及其应用。中国发明专利号：ZL201810083970.0。

14）陈益华、刘明耀、郭伟凯、邢雅婧、黄懂霞、易正芳、杜冰、张乾森。一类4-嘧啶二胺类小分子有机化合物及其衍生物及其应用。中国发明专利号：ZL201710405225.9.

B. 申请专利：

1)        陈益华、周文波、陈煌、易正芳、逄秀凤、刘明耀。一类靶向STAT3双功能磷酸化位点的三芳香环类化合物及其应用。PCT专利国际申请号：PCT/CN2020/102461。

2)        陈益华、刘明耀、郭伟凯、邢雅婧、黄懂霞、易正芳、杜冰、张乾森。一类4-嘧啶二胺类小分子有机化合物及其衍生物及其应用。PCT专利国际申请号：PCT/CN2018/088932.

3)        陈益华，张玉柱，陈静，米大钊。一类靶向肿瘤干性的氟代苯乙酰基四氢-b-咔啉类小分子有机化合物及其医药用途。中国发明专利申请号：202210301004.8。申请日期：2022.03.25.

4)        陈益华，陈策实，何佳，王露珍，米大钊。一类诱导肿瘤细胞发生methuosis死亡的三芳香杂环哌嗪类化合物及其应用。中国发明专利申请号：202210270361.2。申请日期：2022.03.18.

5)        陈益华，何朋，缪颖，易正芳，刘明耀。一类靶向于STAT3的三联芳香杂环哌嗪类小分子有机化合物及其应用。中国发明专利申请号：202210082125.8。申请日期：2022.01.24.

6)        陈益华，罗剑，裴海翔，高竞铎，胡诗佳，刘明耀。一类用于诱导软骨形成的化合物及其应用。中国发明专利申请号：202110052995.3，申请日期：2021.01.15

7)        陈益华, 裴海翔，秦居亮，杜冰，刘明耀。一类脲基四氢咔唑类小分子有机化合物及用途。中国发明专利申请号：201910524751.6。申请日期：2019.06.18.

8)        陈益华、周文波、陈煌、易正芳、逄秀凤、刘明耀。一类靶向STAT3双功能磷酸化位点的三芳香环类化合物及其应用。中国发明专利申请号：201910698892.X。申请日：2019.07.31. （已转让）

9)        陈益华、米大钊、李亮、裴海翔、李大力、刘明耀。一种基于DCAF15的蛋白降解靶向嵌合体及其制备方法和应用。中国发明专利申请号：201910768749.3。申请日：2019.08.20.

10)    陈益华、郭伟凯、谢玖清、邢雅婧、易正芳、刘明耀。一类靶向BCL6的芳香环并五元芳杂环类小分子有机化合物及其衍生物及其应用。中国发明专利申请号：201910898850.0。申请日：2019.09.23.

11)    陈益华、刘明耀、周文波、陈煌、胡盼、易正芳。一种环烷烃并噻吩衍生物及其制备方法和医药用途。中国发明专利申请号：201810353541.0. 申请日：2018.04.19.

12)    陈益华、王平、裴海翔、陈云飞、高丹、刘明耀、罗剑。一类羟基取代的四氢-β-咔啉类小分子有机化合物及其衍生物和医药用途。中国发明专利申请号：201810515378.3. 申请日：2018.05.25.

13)    陈益华，逄秀凤，王鹏，胡克文，刘明耀。含有苯并[b]噻吩结构的化合物及衍生物、制备方法和应用。中国发明专利申请号：201610806223.6

第十八届中国药学会-施维雅青年药物化学奖（2015）

第六届中国国际“互联网⁺”大学生创新创业大赛上海赛区优秀指导教师（2020）。