何国学

个人信息：

何国学 博士

助理研究员，国科大杭州高等研究院

浙江省杭州市西湖区象山支路1号310012

Phone: 0571-86080329

E-mail: heguoxue@ucas.ac.cn

教育及工作经历：

2014-2017年，广西师范大学有机化学硕士

2017-2020年，北京师范大学药物化学与分子工程博士

2020-2022年，中国科学院上海药物研究所药学博士后

2022年至今，国科大杭州高等研究院，助理研究员

2023年欧洲玛丽·居里学者（联合伦敦大学学院申请）

研究方向：

何国学博士专注于神经系统类疾病的先导化合物开发研究。

主要研究包括发现钠通道Nav1.1激动剂、Nav1.2抑制剂的抗癫痫先导化合物，以及mGluR2 PAM抗焦虑和癫痫活性的研究。同时开展一系列新的绿色有机合成方法学研究，致力于构建具有复杂多样性的类药性杂环骨架库。

代表性研究成果：

1.Guoxue He, Yueming Zheng, Shunzhen Chang, Long Wang, Xiaohao Yang, Haishuang Hao, Jiyuan Li, Xian Zhang, Fuyun Tian, Xuewu Liang, Haiyan Xu, Pei Wang, Xueqin Chen, Zeyu Cao, Sui Fang, Zhaobing Gao,* and Hong Liu. Discovery of Novel Pyrimidine-Based Derivatives as Nav1.2 Inhibitors with Efficacy in Mouse Models of Epilepsy. J. Med. Chem. 2024, 67, 12912−12931.

2.Yutian Li, Li Wang, Shengbin Zhou, Guoxue He*, Yu Zhou*. Electrochemical oxidative cyclization of N-allylamides for the synthesis of CF₃-containing benzoxazines and oxazolines, RSC Advances, 2024, 14(1): 154-159.

3.Xiaohao Yang, Hairu Ren, Shengbin Zhou, Chunpu Li, Chaoyi Liu, Yu Zhou, Guoxue He*, Hong Liu*. Rh(III)-Catalyzed Synthesis of Substituted Isoindoles through a Direct C–H Activation/[4 + 1] Annulation and Acyl Migration Cascade of Oxadiazolones with Diazo Compounds. Org. Lett. 2023, 25, 3195-3199.

4.Guoxue He, Yutian Li, Shengbin Zhou, Xiaohao Yang, Aolong Shang, Yunbo Wang, Hong Liu*, Yu Zhou*. A Facile Electrochemical Strategy for the Azidation of Benzylic C(sp3)−H Bonds. Eur. J. Org. Chem. 2022, 2022, e202201041.

5.Guoxue He; Jinyu, Ma; Jianhui, Zhou; Chunpu, Li; Hong, Liu*; Yu, Zhou*. A metal-free method for the facile synthesis of indanones via the intramolecular hydroacylation of 2-vinylbenzaldehyde, Green Chem., 2021, 23, 1036-1040.

6.Guoxue He, Chenglin Wu, Jianhui Zhou, Qiaolan Yang, Chunmei Zhang, Yu Zhou, Huabei Zhang* and Hong Liu*. A Method for Synthesis of 3-Hydroxy-1-indanones via Cu-Catalyzed Intramolecular Annulation Reactions. J. Org. Chem. 2018, 83, 13356-13362.

7.Lin-Su Wei, Guo-Xue He , Xiang-Fei Kong, Cheng-Xue Pan, Dong-Liang Mo^*, Gui-Fa Su^*, Gold(III)-Catalyzed Selective Cyclization of Alkynyl Quinazolinone-Tethered Pyrroles: Synthesis of Fused Quinazolinone Scaffolds, J. Org. Chem. 2018, 83, 6719−6727.

8.Guo-Xue He, Jing-Mei Yuan, Hai-Miao Zhu, Kai Wei, Ling-Yun Wang, Shi-Lin Kong, Dong-Liang Mo, Cheng-Xue Pan^*, Gui-Fa Su^*, Synthesis and antitumor evaluation of 2,3-diarylbenzofuran derivatives on HeLa cells, Bioorg. Med. Chem. Lett. 2017, 27, 1660–1664.

9.Chenglin Wu, Jianhui Zhou, Guoxue He, Huihui Li, Qiaolan Yang, Run Wang, Yu Zhou* and Hong Liu*. Ruthenium(II)-catalyzed selective C-H bond activation of imidamides and coupling with sulfoxonium ylides: an efficient approach for the synthesis of highly functional 3-ketoindoles. Org. Chem. Front. 2019, 6, 1183-1188.

10.Xiang-Fei Kong, Feng Zhan, Guo-Xue He, Cheng-Xue Pan, Chen-Xi Gu, Ke Lu, Dong-Liang Mo^*, Gui-Fa Su^*, Gold-Catalyzed Selective 6-exo-dig and 7-endo-dig Cyclizations of Alkyne-Tethered Indoles To Prepare Rutaecarpine Derivatives, J. Org. Chem. 2018, 83, 2006-2017.

科研项目：

1.浙江省青年科学基金项目，QN25H300020，新型选择性Nav1.1激动剂先导化合物的发现及其抗癫痫活性评价，主持

2.浙江省尖兵项目，人工智能与颠覆性技术辅助药物成药性评价研究，参与

3.国科大杭州高等研究院专项资金资助，自主交叉项目，2022ZZ01015，肺脏损伤再生中支气管上皮向肺泡上皮转分化的分子调控机制及靶向药物开发，2023-01至2024-12，100万元，结题，联合主持

4.国家自然科学基金委员会，面上项目，81973164，组蛋白修饰介导的抑郁症表观遗传调控机制及化学干预，2020-01-01至2023-12-31，55万元，参与