李晓康-全讯国际

李晓康  副教授/特聘副研究员/硕士生导师

地址：上海市徐汇区梅陇路130号实验十八楼431室

email：

邮编：200237

个人简介

      2018年6月毕业于华东理工大学药学院，此后加入cj学者李剑教授团队从事教学科研工作。研究方向主要围绕重大疾病新药创制与精准诊断，立足团队老药（化药和中药）二次研发策略，形成完善的“先导老药的发现（多种策略）→老药新用研究→新结构二次研发→新靶标机制研究→临床前候选药物确定（药效、药代、毒理、成药性等评估）”研究体系，结合荧光探针可视化检测，形成经验丰富的临床前候选新药发现与评价体系，采用多学科交叉合作，聚焦酒精性肝损伤、肝老化、阿尔茨海默病、耐药疟疾等难治性疾病，通过分子机制创新，开发临床前候选药物与诊断工具。近年来，本人以第一/通讯作者在acta pharm. sin. b、j. med. chem.、 chem. sci.、eur. j. med. chem.、chin. chem. lett.、acs chem. neurosci.、dyes pigm.、bioorg. med. chem.等国内外知名学术期刊行发表多篇sci文章，申请发明专利17项（授权5项）。

      作为负责人主持国家自然科学基金面上项目1项（2021）、国家自然科学基金青年基金1项（2019）、上海市面上项目（2023）、中国博士后科学基金面上项目（2018）；入选上海市青年科技英才扬帆计划（2019）、上海市晨光计划（2018）、上海市“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“十四五”规划制药工程专业《药物化学》章节编写。

主要研究方向

1. 老药新用与老药二次研发

2. 基于中草药的新靶标机制研究与新药发现

3. 衰老相关疾病（衰老、肝老化、ad）精准诊断与创新药物研发

4. 靶向pfhdac1的新型多时期抗耐药疟疾候选药物研发

代表性论文(^#共同第一作者，*为通讯作者)

1. 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.

   
   

2. 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.

   
   

3. 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.

4. 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.

5. 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.

6. 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.

7. 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. b 2020, 10, 646–666.

8. 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）

9. 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.

10. 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.

11. 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.

12. 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.

13. 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.

14. 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.

15. 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.

16. 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.

17. 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.