李晓康  博士/副教授/博导

Email：xkli@ecust.edu.cn

邮编：200237

通讯地址1：上海市徐汇区梅陇路130号实验十八楼431办公室

通讯地址2：上海市奉贤区海思路999号实验五楼309办公室

【个人简介】

      2018年6月毕业于华东理工大学药学院，获药学专业博士学位；随后进入华东理工大学药学博士后科研流动站从事博士后研究，合作导师为蒋华良院士；2020年10月出站留校工作，“长江学者”李剑教授团队核心成员。

研究方向围绕临床未满足重大疾病新药创制与精准诊断，聚焦团队老药新用与老药二次研发创新策略，形成完善的“老药先导物发现→老药新用研究→新结构二次研发→新靶标机制研究→临床前候选PCC确定”技术体系，用多学科交叉合作，聚焦肝损伤（肝脏衰老）、急慢性肾衰竭（肾脏衰老）、阿尔茨海默病（脑衰老）、耐药感染（耐药疟疾、耐药真菌）等疾病领域，形成经验丰富的临床前候选新药发现与评价体系；此外，结合荧光探针可视化技术，构建可视化药效评价新方法/新模型。

近年来，以第一/通讯作者发表SCI论文19篇，包括Acta Pharm. Sin. B（2020）、J. Med. Chem.（2016/2021/2022/2024）、Chem. Sci.（2020）、Eur. J. Med. Chem.（2022a/b）等药物化学领域一区期刊；申请发明专利20项（其中PCT专利3项），已授权专利5项。作为项目负责人主持国家基金2项，省部级基金2项；入选上海市青年科技英才扬帆计划（2019）、晨光计划（2018）和“超级博士后”激励计划（2018）。作为研究骨干参与多项国家新药创制重大专项、国家重点研发计划课题、基金委重点项目等研究项目。讲授课程包括本科专业核心课程《药物化学》、专业选修课《药物结构优化——设计策略和经验规则》，参与“十四五”规划制药工程专业《药物化学》章节编写。

【学术兼职】

1、《中国药物化学杂志》首届青年编委

2、中医药慢病防治工程委员会委员

3、华东理工大学新药研发青少年创新实验室（市级），主理人

【研究方向】

1、老药新用与老药二次研发

2、器官衰老相关疾病候选新药研发与新靶标机制解析（肝脏：ALD/NAFLD/MAFLD；肾脏：ARF/CRF；脑：AD）

3、基于中草药活性成分的新靶标机制解析与新药研发

4、基于病理标志物设计荧光探针分子并构建可视化药效评价新方法/新模型

【招生专业】

  药学专业：学术型博士/学硕

【代表性论文】(^#共同第一作者，*为通讯作者)

[1]     Yunyuan Huang^#, Xin Chen^#, Jin Yang^#, Yue Yao, Manjiong Wan, Taotao Lu, Xiao Li, Jiqun Wang, Sicong Qiao, Donglei Shi, Xiaoking Li*, Jian Li*, Yixiang Xu*. Methoxsalen Identified through Synergistic Network Virtual Screening and Experimental Validation. J. Chem. Inf. Model.2024, https://doi.org/10.1021/acs.jcim.4c00670.

[2]     Haolan You^#, Yihe Song^#, Yi Yang^#, Xicheng Wang, Shiqi Pan, Junyang Huang, Qiqi Shao, Donglei Shi, Baoli Li*, Jian Li*, Xiaokang Li*. Rational design of a high-affinity fluorescent probe for visualizing monitoring the amyloid β clearance effect of anti-Alzheimer's disease drug candidates. Eur. J. Med. Chem.2024, 278, 116800.

[3]     Xiangran Lu^#, Rongrong Wang^#, Yao Yu^#, Jinlian Wei, Yixiang Xu, Luoyifan Zhou, Fei Mao, Jian Li*, Xiaokang Li*, and Xinming Jia*. Drug Repurposing of ACT001 to Discover Novel Promising Sulfide Prodrugs with Improved Safety and Potent Activity for Neutrophil-Mediated Antifungal Immunotherapy. J. Med. Chem. 2024, 67, 5783−5799.

[4]     Chao Zhang^#, Lan Wang^#, Yixiang Xu^#, Yunyuan Huang, Junyang Huang, Jin Zhu, Wei Wang, Wangsheng Li, Annan Sun, Xiaokang Li*, Haiyan Zhang*, Jian Li*. Discovery of novel dual RAGE/SERT inhibitors for the potential treatment of the comorbidity of Alzheimer’s disease and depression. Eur. J. Med. Chem.2022, 236, 114347.

[5]     Manjiong Wang^#, Tongke Tang^#, Zhenghui Huang, Ruoxi Li, Dazheng Ling, Jin Zhu, Lubin Jiang*, Jian Li*, Xiaokang Li*. Design and synthesis of novel hydroxamic acid derivatives based on quisinostat as promising antimalarial agents with improved safety. Acta Materia Medica2022, 1, 212–223.

[6]     Manjiong Wang^#, Tongke Tang^#, Ruoxi Li, Zhenghui Huang, Dazheng Ling, Lulu Zheng, Yan Ding, Taiping Liu, Wenyue Xu, Feng Zhu, Hui Min, Rachasak Boonhok, Fei Mao, Jin Zhu, Xiaokang Li*, Lubin Jiang*, and Jian Li*. Drug Repurposing of Quisinostat to Discover Novel Plasmodium falciparum HDAC1 Inhibitors with Enhanced Triple-Stage Antimalarial Activity and Improved Safety. J. Med. Chem.2022. 65, 4156−4181.

[7]     Xiaokang Li^#, Jinwen Li^#, Yunyuan Huang^#, Qi Gong, Yan Fu, Yixiang Xu, Junyang Huang, Haolan You, Dong Zhang, Dan Zhang, Fei Mao, Jin Zhu, Huan Wang*, Haiyan Zhang*, Jian Li*. The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. Eur. J. Med. Chem.2022, 229, 114045.

[8]     Ruoxi Li^#, Dazheng Ling^#, Tongke Tang^#, Zhenghui Huang, Manjiong Wang, Yan Ding, Taiping Liu, Hanwen Wei, Wenyue Xu, Fei Mao, Jin Zhu, Xiaokang Li*, Lubin Jiang*, Jian Li*. Discovery of novel P. falciparum HDAC1 inhibitors with dual-stage anti-malarial potency and improved safety based on the clinical anticancer drug candidate quisinostat. J. Med. Chem. 2021, 64, 2254.

[9]     Ruoxi Li^#, Dazheng Ling^#, Tongke Tang^#, Zhenghui Huang, Manjiong Wang, Fei Mao, Jin Zhu, Lubin Jiang*, Jian Li*, Xiaokang Li*. Repurposing of antitumor drug candidate Quisinostat lead to novel spirocyclic antimalarial agents. Chin. Chem. Lett.2021, 32, 1660−1664.

[10]Xiaokang Li^#, Jian Lu^#, Yixiang Xu^#, Jiaying Wang, Xiaoxia Qiu, Lei Fan, Baoli Li, Wenwen Liu, Fei Mao, Jin Zhu, Xu Shen*, Jian Li*. Discovery of nitazoxanide-based derivatives as autophagy activators for the treatment of Alzheimer's disease. Acta Pharm. Sin. B2020, 10, 646–666.

[11]Xiaokang Li^#, Wenjing Qiu^#, Jinwen Li^#, Xi Chen^#, Yulu Hu, Ying Gao, Donglei Shi, Xinming Li, Huiling Lin, Zelan Hu, Guoqiang Dong, Chunquan Sheng, Bei Jiang, Conglong Xia, Chu-Young Kim, Yuan Guo*, Jian Li*. First-generation species-selective chemical probes for fluorescence imaging of human senescence-associated β-galactosidase. Chem. Sci.2020, 11, 7292.（封面文章）

[12]Wenjing Qiu^#, Xiaokang Li^#, Donglei Shi, Xinming Li, Ying Gao, Fei Mao, Yuan Guo, Jian Li*. A rapid-response near-infrared fluorescent probe with a large Stokes shift for senescence-associated -galactosidase activity detection and imaging of senescent cells. Dyes Pigm. 2020, 182, 108657.

[13]Yixiang Xu^#, Jian Zhang^#, Huan Wang^#, Fei Mao, Keting Bao, Wenwen Liu, Jin Zhu, Xiaokang Li*, Haiyan Zhang*, and Jian Li*. Rational Design of Novel Selective Dual-Target Inhibitors of Acetylcholinesterase and Monoamine Oxidase B as Potential Anti-Alzheimer's Disease Agents. ACS Chem. Neurosci. 2019, 10, 482−496.

[14]Jin Li^#, Xiaokang Li^#, Jianbo Jia^#, Xi Chen, Yinjuan Lv, Yuan Guo*, and Jian Li*. A ratiometric near-infrared fluorescence strategy based on spiropyran in situ switching for tracking dynamic changes of live-cell lysosomal pH. Dyes Pigm.2019, 66, 433–442.

[15]Wenwen Liu^#, Huan Wang^#, Xiaokang Li^#, Yixiang Xu, Jian Zhang, Wei Wang, Qi Gong, Xiaoxia Qiu, Jin Zhu, Fei Mao*, Haiyan Zhang*, Jian Li*. Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. Bioorg. Med. Chem.2018, 26, 3117–3125.

[16]Wei Ni^#, Huan Wang^#, Xiaokang Li^#, Xinyu Zheng, Manjiong Wang, Jian Zhang, Qi Gong, Dazheng Ling, Fei Mao*, Haiyan Zhang*, and Jian Li*. Novel Tadalafil Derivatives Ameliorates Scopolamine-Induced Cognitive Impairment in Mice via Inhibition of Acetylcholinesterase (AChE) and Phosphodiesterase 5 (PDE5). ACS Chem. Neurosci.2018, 9, 1625−1636.

[17]Xiaokang Li^#, Yahui Huang^#, Junfei Cheng^#, Lingling Zhang, Fei Mao, Jin Zhu, Chunquan Sheng*, Jian Li*. Discovery of novel Syk/PDGFR-α/c-Kit inhibitors as multi-targeting drugs to treat rheumatoid arthritis. Bioorg. Med. Chem.2018, 26, 4375–4381.

[18]Xiaokang Li^#, Huan Wang^#, Yixiang Xu, Wenwen Liu, Qi Gong, Wei Wang, Xiaoxia Qiu, Jin Zhu, Fei Mao, Haiyan Zhang *, and Jian Li *. Novel Vilazodone–Tacrine Hybrids as Potential Multitarget-Directed Ligands for the Treatment of Alzheimer’s Disease Accompanied with Depression: Design, Synthesis, and Biological Evaluation. ACS Chem. Neurosci.2017, 8, 2708−2721.

[19]Xiaokang Li^#, Huan Wang^#, Zhengyu Lu, Xinyu Zheng, Wei Ni, Jin Zhu, Yan Fu, Fulin Lian, Naixia Zhang, Jian Li*, Haiyan Zhang*, and Fei Mao*. Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. J. Med. Chem.2016, 59, 8326–8344.

[20]Xiaokang Li, Wei Ni, Fei Mao, Wei Wang*, Jian Li*. A Metal-free Approach to 3-Aryl-3-hydroxy-2-oxindoles by Treatment of 3-Acyloxy-2-oxindoles with Diaryliodonium Salts. Chem. Asian J.2016, 11, 226–230.