研究生教育

药物化学

胡有洪

姓 名 胡有洪 性 别 职 称 研究员
学 历 博士 电 话 传 真
电子邮件 yhhu@simm.ac.cn 个人主页 主页链接 专家类别
职 务 课题组长、博导
通讯地址 烟台市牟平区滨海东路198号
研究方向

1.类天然产物和类药性骨架合成新方法的研究与高质量多样性小分子库的构建;

2.新型活性化合物的发现与成药性优化至先导或候选药物的开发;

3.小分子探针的设计合成及相关化学生物学方法探索生物机制研究;

科研项目

    2021.5-2023.4
    1. 中国科学院药物创新研究院自主部署科研项目,选择性抑制HDACI候选化合物Yhhu6974的抗肿瘤临床前研究,课题负责人。

    2021.1-2022.12
    2. 上海市市级科技重大专项,去唾液酸糖蛋白受体靶向的糖类抗肝癌候选新药发现,课题负责人。

    2019.1-2022.12
    3. 国家自然科学基金面上项目,新型抗乙肝病毒哒嗪酮类小分子的优化及降解相关蛋白小分子探针的发现,课题负责人。

    2018.1-2019.12
    4. 中国科学院战略性先导科技专项A类,哒嗪酮类选择性HDAC6抑制剂的个性化抗肿瘤先导化合物的发现,课题负责人。

    2016.1-2017.12
    5. 中国科学院战略性先导科技专项A类,抗糖尿病靶向GPR40个性化先导化合物的发现,课题负责人。

    2013.1-2016.12
    6. 国家杰出青年科学基金,药物化学,课题负责人。

    2012.1-2015.12
    7. 科技部重大专项,基于天然产物D8的抗糖尿病活性的候选新药研究,课题负责人。

    2012.1-2015.12

    8. 国家自然科学基金面上项目,基于含色酮环中间体的串联及多组分反应研究和多样性分子库的合成,课题负责人。

    2010.7-2013.9

    9. 上海市科学技术委员会:新型抗肿瘤微管蛋白抑制剂嘧啶类化合物的成药性研究,课题负责人。

科研成果

1.发展高效合成技术,快速构建结构多样性的类药杂环及类天然产物小分子库,是获得原创性活性化合物的基础;

2.基于发现的活性化合物,成药性优化发展候选药物,为我国1.1 类新药的开发奠定基础,两项新药研究转让与企业;

3.发展探针分子进行化学生物学研究,为生命科学的基础性研究和药物新靶点的发现提供有效的工具。

荣誉获奖

    2010年 中国药学会—赛诺菲安万特青年生物药物奖

    2011年 中国科学院朱李月华优秀教师奖

    2015年 上海药学会科技奖一等奖(集体奖)

    2016年 中国药学会科学技术奖二等奖(集体奖)

代表论著

    1.Zhicheng Xie#, Lin Li#, Yihao Guo, Mi Zhang, Taiwen Chen, Yongpeng Li, Xin Li, Xi Zhu, Yu Zhang, Liguang Lou*, Youhong Hu*, Discovery of novel heteroaryl alkynes for highly potent KITD816V cells inhibition to treat gastrointestinal stromal tumors, Acta Pharmaceutica Sinica B, 2022, 12, 4004-4007.

    2.Sheng Han#, Heng Li#, Weixiong Chen, Li Yang, Xiankun Tong*, Jianping Zuo*, Youhong Hu*, Discovery of potent ebola entry inhibitors with (3S,4aS,8aS)-2-(3-amino-2-hydroxypropyl) decahydroisoquinoline-3-carboxamide scaffold, European Journal of Medicinal Chemistry, 2022, 240, 114608.

    3.Jingjing Chen#, Huixin He #, Aihuan Wei, Yalei Li, Gang Cheng, Hui Qin, Hanyue Zhong, Hongchun Liu, Meiyu Geng, Aijun Shen*, Youhong Hu*, Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold, European Journal of Medicinal Chemistry, 2022,236, 114259.

    4.Jinxin Che, Zhilong Wang, Zheyuan Shen, Weihao Zhuang, Huazhou Ying, Yongzhou Hu, Youhong Hu*, Xin Xie*, and Xiaowu Dong*, Discovery of 1,5-Dihydro‑4H‑imidazol-4-one Derivatives as Potent, Selective Antagonists of CXC Chemokine Receptor 2, ACS Med. Chem. Lett. 2021, 12, 836−845. 

    5.Zhicheng Xie#, Caigui Xiang#, Xin Li, Chen Fan, Taiwen Chen, Moting Liu, Yanjie Ma, Fang Bai, Wei Tang,* and Youhong Hu*, Discovery of Potent Antiallergic Agents Based on ano‑Aminopyridinyl Alkynyl Scaffold, J. Med. Chem, 2021, 64 (18), 13588-13603. 

    6.Jingjing Chen#; Yalei Li#; Jie Zhang; Minmin Zhang ; Aihuan Wei ; Hongchun Liu ; Zhicheng Xie ; Wenming Ren ; Wenwen Duan ; Zhuo Zhang; Aijun Shen* ; Youhong Hu*; Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes, European Journal of Medicinal Chemistry, 2021, Vol209, 112868.

    7.Congcong Wang#, Yu-Fang Zhang#, Shimeng Gu#, Quan Zhao, Yanping Zeng, Zhicheng Xie, Xin Xie*, Boxun Lu*, and Youhong Hu* ,GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington’s Disease-Related Phenotypes, J. Med. Chem, 2021, 64, 941-957. 

    8.Wen-Di Duan, Yu-Fang Zhang, and Youhong Hu*,NaH Promoted One-Pot Tandem Reactions of 3‑(1-Alkynyl) Chromones to Form 2‑Nitrogen-Substituted Xanthones, ACS Omega, 2020, 5, 13454−13461. 

    9.Wuhong Chen,# Feifei Liu,# Qiliang Zhao,# Xinna Ma, Dong Lu, Heng Li, Yanping Zeng, Xiankun Tong, Limin Zeng, Jia Liu, Li Yang,* Jianping Zuo,* and Youhong Hu*, Discovery of Phthalazinone Derivatives as Novel Hepatitis B Virus Capsid Inhibitors, J. Med. Chem., 2020, 63(15): 8134-8145. 

    10.Zhicheng Xie#; Bing Wu #; Yingqiang Liu#; Wenming Ren; Linjiang Tong; Caigui Xiang; Aihuan Wei; Yuanzhuo Gao; Limin Zeng; Hua Xie*; Wei Tang*; Youhong Hu*; Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an o-Aminopyridyl Alkynyl Scaffold as Potential Treatment for Inflammatory Disorders, J. Med. Chem., 2020, 63 (3): 1397-1414. 

    11.Yu Lei#,Wenming Ren#, Cheng-Kun Wang, Rong-Rong Tao, Huai-Jiang Xiang, Li-Li Feng, Yin-Ping Gao, Quan Jiang, Xin Li*, Youhong Hu*, Feng Han*, Visualizing Autophagic Flux during Endothelial Injury with a Pathway-Inspired Tandem-Reaction Based Fluorogenic Probe, Theranostics 2019, Vol. 9, Issue 19, 5672-5680. 

    12.Yu-Fang Zhang, Wen-Di Duan, Jingjing Chen, and Youhong Hu*, Base-Promoted Cascade Reactions of 3‑(1-Alkynyl)chromones with Pyridinium Ylides to Chromeno[2,3-d]azepine Derivatives, J. Org. Chem., 2019, 84, 4467−4472.

    13.Wenming Ren#, Jingjing Zhang#, Cheng Peng#, Huaijiang Xiang, Jingjing Chen, Chengyuan Peng, Weiliang Zhu, Ruimin Huang,* Haiyan Zhang,* and Youhong Hu*, Fluorescent Imaging of β‑Amyloid Using BODIPY Based Near-Infrared Off−On Fluorescent Probe, Bioconjugate Chem. 2018, 29, 3459−3466. 

    14.Wenming Ren#, Huaijiang Xiang#, Chengyuan Peng, Zulipali Musha, Jingjing Chen, Xin Li, Ruimin Huang*, and Youhong Hu*, Direct C–H functionalization of difluoroboron dipyrromethenes (BODIPYs) at b-position by iodonium salts, RSC Advances, 2018, 8, 5542–5549. 

    15.Dong Lu#, Jianan Liu#, Yunzhe Zhang#, Feifei Liu, Limin Zeng, Runze Peng, Li Yang, Huazhou Ying, Wei Tang, Wuhong Chen, Jianping Zuo, Xiankun Tong*, Tao Liu*, Youhong Hu*, Discovery and optimization of phthalazinone derivatives as a new class of potent dengue virus inhibitors, European Journal of Medicinal Chemistry, 2018, 145, 328-337. 

    16.Dong Lu#, Juan Yan#, Lang Wang, Hongchun Liu, Limin Zeng, Minmin Zhang, Wenwen Duan, Yinchun Ji, Jingchen Cao, Meiyu Geng, Aijun Shen*, and Youhong Hu*, Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives, ACS Med. Chem. Lett., 2017, 8 (8), 830–834. 

    17.Jianwei Yan#, Gaihong Wang#, Xiangyu Dang, Binbin Guo, Wuhong Chen, Ting Wang, Limin Zeng, Heyao Wang*, Youhong Hu*, Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety, Bioorgan. Med. Chem., 2017, 25, 4701-4714.

    18.Shan Li, Penghui Wan, Jing Ai, Rong Sheng*, Yongzhou Hu*, and Youhong Hu*, Palladium-Catalyzed, Silver-Assisted Direct C-5–H Arylation of 3-Substituted 1,2,4-Oxadiazoles under Microwave Irradiation, Adv. Synth. Catal., 2017, 359, 772 –778. 

    19.Dong Lu#, Feifei Liu#, Weiqiang Xing, Xiankun Tong, Lang Wang, Yajuan Wang, Limin Zeng, Chunlan Feng, Li Yang*, Jianping Zuo*, and Youhong Hu*, Optimization and Synthesis of Pyridazinone Derivatives as Novel Inhibitors of Hepatitis B Virus by Inducing Genome-free Capsid Formation, ACS Infect. Dis., 2017, 3 (3), 199–205. 

    20.Yang Liu#, Xia Peng#, Xiaocong Guan#, Dong Lu, Yong Xi, Shiyu Jin, Hui Chen, Limin Zeng, Jing Ai*, Meiyu Geng*, Youhong Hu*, Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors, Eur. J. Med. Chem., 2017, 126, 122-132. 

社会任职

上海市药学会第十二届理事会药物化学专业委员会委员。

胡有洪

姓 名 胡有洪 性 别 职 称 研究员
学 历 博士 电 话 传 真
电子邮件 yhhu@simm.ac.cn 个人主页 主页链接 专家类别
职 务 课题组长、博导
通讯地址 烟台市牟平区滨海东路198号