职称:研究员 E-mail:liwaii@126.com 主要研究方向:靶向药物的设计、合成与构效关系研究。
个人简介
博导,毕业于南京大学化学系,5163银河主站线路检测药物化学与分析系主任,药学专业负责人,江苏省中医药学会药学专业委员会委员,国家卫生部保健品评审专家。从事药物化学教学和科研工作多年。系统讲授药学类专业导论、药物化学等课程,主编本科生《药物化学》、研究生《药物化学选论》等教材四部。兼任多个学术期刊审稿编辑。近年来指导研究生在Journal of Medicinal Chemistry, Organic Letters, Advanced Synthesis & Catalysis, Bioorganic Chemistry, J Org Chem等药学高水平期刊上发表SCI论文34篇;指导研究生获得研究生创新计划6项。
承担的主要科研项目
1. 科技部“十一五”科技重大专项(2009ZX09103-081),Liguzinediol先导物的候选药物研究,2009/01-2010/12,主持,150万,结题
2. 国家自然科学基金面上项目(81573304),基于SERCA2a靶点的正性肌力活性化合物设计,2016/01-2019/12,主持,60万,结题
3. 国家自然科学基金面上项目(81072542),Liguzinediol的结构修饰及正性肌力构效关系研究,2011/01-2013/12,主持,36万,结题
4. 教育部高等学校博士学科点专项科研基金(20123237110010),具有良好药代特性的川芎嗪衍生物设计、合成及构效关系研究,2013/01-2015/12,主持,12万,结题
5. 江苏省自然科学基金(BK2011077),H168的临床前基础研究,2012/01-2014/12,主持,20万,结题
6. 江苏省自然科学基金(BK2008454),H168的作用机理及新药基础研究,2008/01-2010/12,主持,8万,结题
7. 江苏省中药资源产业化过程协同创新中心重点项目(ZDXM-2-1),创新药物H168注射液的临床前研究,2015/01-2016/12,主持,50万,结题
8. 企业委托项目(012009210059),OL8102的合成工艺验证,2021/07-2025/12,主持,30万,在研
9. 企业委托项目(012009210023),OL2186的合成路径验证,2021/01-2022/12,主持,20万,在研
10. 企业委托项目(012009026031),TTX原料药及软胶囊一类新药研制,2010/01-2015/12,主持,200万,结题
代表性论文
1. Xiaomeng Zhang,# Yazhou Wang,# Jianfeng Ji,# Dongjuan Si, Xueting Bao, Zhuangzhuang Yu,Yueyue Zhu, Liwen Zhao,* Wei Li,* and Jian Liu*. Discovery of 1,6-Naphthyridin-2(1H)‑one Derivatives as Novel,Potent, and Selective FGFR4 Inhibitors for the Treatment of Hepatocellular Carcinoma. Journal of Medicinal Chemistry, 2022, doi.org/10.1021/acs.jmedchem.1c01977(共同通讯)
2. Yueyue Zhu #; Rupeng Dai # ; Chaoqun Huang#; Wang Zhou; Xiaoyuan Zhang; Kundi Yang; Hongmei Wen*; Wei Li*; and Jian Liu*. Synthesis of Isoquinolone, 1,2-Benzothiazine, and Naphtho[1',2':4,5]imidazo[1,2‑a]pyridine Derivatives via Rhodium(III)-Catalyzed (4+2) Annulation. Journal of Organic Chemistry, 2022, https://doi.org/10.1021/acs.joc.2c01376(共同通讯)
3. Xiaomeng Zhang#, Yazhou Wang#, Xue Li, Jie Wu, Liwen Zhao*, Wei Li*, & Jian Liu*. Dynamics-Based Discovery of Novel, Potent Benzoic Acid Derivatives as Orally Bioavailable Selective Estrogen Receptor Degraders for ERα+ Breast Cancer, Journal of Medicinal Chemistry, 2021, 64(11): 7575-7595(共同通讯)
4. Chao Wang#, Xiyan Rui#, Dongjuan Si, Rupeng Dai, Yueyue Zhu, Hongmei Wen, Wei Li*, and Jian Liu*. Copper‐Catalyzed Three‐Component Cascade Reaction of Benzaldehyde with Benzylamine and Hydroxylamine or Aniline: Synthesis of 1,2,4‐Oxadiazoles and Quinazolines, Advanced Synthesis & Catalysis, 2021, 363(11): 2825-2833(共同通讯)
5. Dongjuan Si, Huijuan Luo, Xiaomeng Zhang, Kundi Yang, Hongmei Wen, Wei Li*, and Jian Liu*. Design, synthesis and biological evaluation of novel pyrrolidone-based derivatives as potent p53-MDM2 inhibitors, Bioorganic Chemistry, 2021, 115: 105268(共同通讯)
6. Xiyan Rui, Chao Wang, Dongjuan Si, X. Hui, K. Li, Hongmei Wen, Wei Li*, and Jian Liu*. One-Pot Tandem Access to Phenothiazine Derivatives from Acetanilide and 2-Bromothiophenol via Rhodium-Catalyzed C-H Thiolation and Copper-Catalyzed C-N Amination, Journal of Organic Chemistry, 2021, 86(9): 6622-6632(共同通讯)
7. Yinyu Yan, Chaoqun Huang, Yi Shu, Hongmei Wen*, Chenxiao Shan,Xinzhi Wang, Jian Liu and Wei Li*. An HDAC8-selective fluorescent probe for imaging in living tumor cell lines and tissue slices. Organic & Biomolecular Chemistry, 2021,19(38): 8352-8366(共同通讯)
8. Jian Liu#, Yi Gao#, Yehua Zhu#, Junru Zhu, Chao Wang, Xiyan Rui, Kundi Yang, Dongjuan Si, Jiamin Lin, Dandan Yuan, Hongmei Wen, and Wei Li*. Rhodium(III)-Catalyzed Oxidative Annulation of 4-Aminoquinolines and Acrylate through Two Consecutive C(sp2)–H Activations, Organic Letters, 2020, 22(7): 2657-2662(通讯)
9. Yehua Zhu#, Yi Gao#, Xinjie Sun, Chao Wang, Xiyan Rui, Dongjuan Si, Junru Zhu, Wei Li*, and Jian Liu*. Discovery of Novel Serine/Threonine Protein Phosphatase 1 Inhibitors from Traditional Chinese Medicine through Virtual Screening and Biological Assays. Journal of Biomolecular Structure and Dynamics, 2020, 38(18): 5464-5473(共同通讯)
10. Jiyun Zhang, Hongmei Wen*, Fei Shen, Xinzhi Wang, Chenxiao Shan, Chuan Chai, Jian Liu, and Wei Li*. Synthesis and biological evaluation of a novel series of curcumin-peptide derivatives as PepT1-mediated transport drugs. Bioorganic Chemistry, 2019, 92: 103163(共同通讯)
获得奖项与荣誉
1. 基于系统性血管生成评价技术探索血瘀证的科学内涵及其创新药物评价研究,江苏药理科学技术二等奖,2017,第四完成人
2. 利用血管新生评价体系探究活血化瘀科学内涵及其中药新药创制,中华中医药学会科学技术奖三等奖,2017,第四完成人
3. 用于抗急性痛风的二妙类方配伍机理及效应物质基础研究,江苏中医药科学技术三等奖,2014,第六完成人
4. 白术质量标准化研究,省中医药科技进步一等奖,2000,第二完成人
其他成果
1. 2,5-二羟甲基-3,6-二甲基吡嗪的合成与精制方法。中国专利授权,ZL201310169578.5,2016
2. Application of 2,5-Dihydroxymethyl-3,6-dimethylpyrazine and its Derivates in Pharmacy. 美国专利授权,US8,158,630B2,2012;澳大利亚专利授权AU2010200453,2014
3. 2,5-二羟甲基-3,6-二甲基吡嗪及其衍生物在制药中的应用。中国专利授权,ZL200810157140.4,2010