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徐进宜 教授 博士生导师    

        药学博士,中国药科大学药学院药物化学系教授,博导。1986年毕业于中国药科大学,留校任教30余年,一直工作在教学科研第一线,先后讲授了药物化学、药物合成反应、药物分子设计、药学英语、专业英语等课程。协助指导和独立指导过博士、硕士研究生80余名。在国内外期刊发表论文120多篇,其中SCI论文90余篇;申请国内外发明专利30多项,授权20项;参编著作12部。曾经获得“教书育人”优秀教师奖;教育部优秀青年教师;国家科技部优秀论文二等奖;广东省科学技术奖励一等奖;中国药科大学先进科技工作者等荣誉。

     曾经担任国家科技进步奖、国家863计划评审专家、国家自然科学基金评审专家、农业部兽药审评、江苏省新药审评专家;担任了Journal of Medicinal Chemistry, Current Medicinal ChemistryEuropean Journal of Medicinal Chemistry, Bioorganic & Medicinal Chemistry等国际杂志特约审稿人。


研究方向


1、活性天然产物的合成、结构优化与生物活性研究:基于具有生物活性天然产物的结构,研究其可能的作用机制及合成方法,发现具有活性的最简化学结构,并针对其成药性进行结构优化研究(硕士招生方向)。

2、针对重大疾病的创新药物研究:对严重危害人类健康的重大疾病,根据其相关的生理、生化知识,开展药物分子的创新设计、合成和成药性优化研究(博士招生方向)。

 

近期文章

2021

(1) Shaowen Xie, Yuan Sun, Yulin Liu, Xinnan Li, Xinuo Li, Wenyi Zhong, Feiyan Zhan, Jingjie Zhu, Hong Yao, Dong-Hua Yang, Zhe-Sheng Chen, Jinyi Xu*, and Shengtao Xu*. Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK). J. Med. Chem. https://doi.org/10.1021/acs.jmedchem.1c00270. (IF: 7.443)

(2) Hong Yao, Giuseppe Uras, Pengfei Zhang, Shengtao Xu, Ying Yin, Jie Liu, Shuai Qin, Xinuo Li, Stephanie Allen, Renren Bai, Qi Gong, Haiyan Zhang*, Zheying Zhu*, Jinyi Xu*. Discovery of novel tacrine-pyrimidone hybrids as potent dual AchE/GSK-3 inhibitors for the treatment of Alzheimer’s disease. J. Med. Chem. 2021, 64: 7483-7505. (IF: 7.443)

(3) Huajian Zhu, Wenlong Li, Wen Shuai, Yang Liu, Limei Yang, Yuchen Tan, Tiandong Zheng, Hong Yao, Jinyi Xu*, Zheying Zhu, Dong-Hua Yang, Zhe-Sheng Chen, Shengtao Xu*. Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities. Eur. J. Med. Chem. 2021, 216, 113316. (IF:6.513)

 

2020

(1) Wen Shuai, Xinnan Li, Wenlong Li, Feijie Xu, Lixue Lu, Hong Yao, Limei Yang, Huajian Zhu, Shengtao Xu*, Zheying Zhu, Jinyi Xu*. Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors. Eur. J. Med. Chem. 2020, 197: 112308. (IF: 5.572)

(2) Huajian Zhu, Honghao Sun, Yang Liu, Yiping Duan, Jie Liu, Xue Yang, Wenlong Li, Shuai Qin, Shengtao Xu*, Zheying Zhu, Jinyi Xu*. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur. J. Med. Chem. 2020, 207: 112716. (IF: 5.572)

(3) Hong Yao, Shaowen Xie, Xiaoqian Ma, Junkai Liu, Hongyu Wu, Aijun Lin, Hequan Yao, Dahong Li, Shengtao Xu*, Dong-Hua Yang, Zhe-Sheng Chen, Jinyi Xu*. Identification of a potent oridonin analogue for treatment of triple-negative breast cancer. J. Med. Chem. 2020, 63: 8157-8178. (IF:6.205)

(4) Junkai Liu, Hong Yao, Xinnan Li, Hongyu Wu, Aijun Lin, Hequan Yao, Jinyi Xu*, Shengtao Xu*. Organocatalytic 1,5-trifluoromethylthiosulfonylation of vinylcyclopropane mediated by visible light in the water phase. Org. Chem. Front. 2020, 7: 1314-1320. (IF:5.155)

(5) Tong Wang, Yanpeng Liu, Jinyi Xu*. Expansion of annulation of allenoates with trifluoroketones: Synthesis of trifluoromethylated dihydropyrans. Synth. Commun. 2020, 50: 315-321. (IF: 1.796)

 

 

2019

(1) Wen Shuai, Wenlong Li, Ying Yin, Limei Yang, Feijie Xu, Shengtao Xu*, Hequan Yao, Zheying Zhu, Jinyi Xu*. Desing, synthesis and molecular modeling of isothiochromanone derivatives as acetylcholinesterase inhibitors. Future Med. Chem. 2019, 11: 2687-2699. (IF: 3.617)

(2)Yanpeng Liu, Lixue Lu, Haipin Zhou, Feijie Xu, Cong Ma, Zhangjian Huang, Jinyi Xu*, Shengtao Xu. Chemodivergent synthesis of N-(pyridin-2-yl)amides and 3-bromoimidazo[1,2-a]pyridines from alpha-bromoketones and 2-aminopyridines. RSC Adv. 2019, 9: 34671-34676. (IF: 3.049)

(3) Lixue Lu, Hengyuan Zhang, Jie Liu*, Yang Liu, Yiwei Wang, Shengtao Xu, Zheying Zhu, Jinyi Xu*. Synthesis, biological evaluation and mechanism studies of C-23 modified 23-hydroxybetulinic acid derivatives as anticancer agents. Eur. J. Med. Chem. 2019, 182: 111659. (IF: 4.833)

(4) Pengfei Zhang, Shengtao Xu*, Zheying Zhu, Jinyi Xu*. Multi-target design strategies for the improved treatment of Alzheimer's disease. Eur. J. Med. Chem. 2019, 176: 228-247. (IF: 4.833)

(5) Shaowen Xie, Xinnan Li, Hao Yu, Pengfei Zhang, Jia Wang, Chaolei Wang, Shengtao Xu, Zheng Wu, Jie Liu*, Zheying Zhu, Jinyi Xu*. Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates. Bioorg. Med. Chem. 2019, 27: 2764-2770. (IF: 3.073)

(6) Feijie Xu, Wenlong Li, Wen Shuai, Limei Yang, Yi Bi, Cong Ma, Hequan Yao, Shengtao Xu*, Zheying Zhu, Jinyi Xu*. Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents. Eur. J. Med. Chem. 2019, 173: 1-14. (IF: 4.833)

(7) Hong Yao, Shanshan Luo, Junkai Liu, Shaowen Xie, Yanpeng Liu, Jinyi Xu*, Zheying Zhu, Shengtao Xu*. Controllable thioester-based hydrogen sulfide slow-releasing donors as cardioprotective agents. Chem. Commun. 2019, 55: 6193-6196. (IF: 6.164)

(8) Wenlong Li, Honghao Sun, Feijie Xu, Wen Shuai, Jie Liu, Shengtao Xu*, Hequan Yao, Cong Ma, Zheying Zhu*, Jinyi Xu*. Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site. Bioorg. Chem. 2019, 85: 49-59. (IF: 3.926)

(9) Hong Yao, Feijie Xu, Guangyu Wang, Shaowen Xie, Wenlong Li, Hequan Yao, Cong Ma, Zheying Zhu, Jinyi Xu*, Shengtao Xu*. Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors. Eur. J. Med. Chem. 2019, 167: 485-498. (IF: 4.833)

(10) Wenlong Li, Ying Yin, Wen Shuai, Feijie Xu, Hong Yao, Jie Liu, Keguang Cheng, Jinyi Xu*, Zheying Zhu*, Shengtao Xu*. Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain. Bioorg. Chem. 2019, 0-83: 38390. (IF: 3.926)

(11) Wenlong Li, Wen Shuai, Honghao Sun, Feijie Xu, Yi Bi, Jinyi Xu*, Cong Ma, Hequan Yao, Zheying Zhu, Shengtao Xu*. Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site. Eur. J. Med. Chem. 2019, 163: 428-442. (IF: 4.833)

(12) Wenlong Li, Feijie Xu, Wen Shuai, Honghao Sun, Hong Yao, Cong Ma, Shengtao Xu*, Hequan Yao, Zheying Zhu, Dong-Hua Yang, Zhe-Sheng Chen, Jinyi Xu*. Discovery of novel quinoline-chalcone derivatives as potent antitumor agents with microtubule polymerization inhibitory activity. J. Med. Chem. 2019, 62: 993-1013.(IF: 6.054)

(13) Shengtao Xu, Shanshan Luo, Zheying Zhu, Jinyi Xu*. Small molecules as inhibitors of PCSK9: Current status and future challenges. Eur. J. Med. Chem. 2019, 162: 212-233. (IF: 4.833)

 

2018

(1) Yanpeng Liu, Honghao Sun, Zhangjian Huang, Cong Ma, Aijun Lin, Hequan Yao, Jinyi Xu*, Shengtao Xu*. Metal-Free Synthesis of N-(Pyridine-2-yl)amides from Ketones via Selective Oxidative Cleavage of C(O)-C(Alkyl) Bond in Water. J. Org. Chem. 2018, 83: 14307-14313. (IF: 4.805)

(2) Wenlong Li, Wen Shuai, Feijie Xu, Honghao Sun, Shengtao Xu*, Hong Yao, Jie Liu*, Hequan Yao, Zheying Zhu, Jinyi Xu*. Discovery of novel 4-arylisochromenes as anticancer agents inhibiting tubulin polymerization. ACS Med. Chem. Lett. 2018, 9: 974-979. (IF: 3.794)

(3) Hong Yao, Guoxiang Wei, Yanpeng Liu, Hequan Yao, Zheying Zhu, Wencai Ye, Xiaoming Wu, Jinyi Xu*, Shengtao Xu*. Synthesis, biological evaluation of fluorescent 23-hydroxybetulinic acid probes and their cellular localization studies. ACS Med. Chem. Lett. 2018, 9: 1030-1034. (IF: 3.794)

(4) Wenlong Li, Ying Yin, Hong Yao, Wen Shuai, Honghao Sun, Shengtao Xu*, Jie Liu, Hequan Yao, Zheying Zhu, Jinyi Xu*. Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities. Eur. J. Med. Chem. 2018, 157: 1068-1080. (IF: 4.816)

(5) Pengfei Zhang, Yu Zhou, Xu Han, Jinyi Xu*, Hong Liu*. N-Heterocyclic Carbene Catalyzed Enantioselective [3+2] Dearomatizing Annulation of Saturated Carboxylic Esters with N-Iminoisoquinolinium Ylides. J. Org. Chem. 2018, 83: 3879-3888. (IF: 4.805)

(6) Tianyu Wang, Jichao Chen, Jia Wang, Shengtao Xu*, Aijun Lin, Hequan Yao, Sheng Jiang*, Jinyi Xu*. Cobalt-catalyzed carbon-sulfur/selenium bond formation: synthesis of benzo[b]thio/selenophene-fused imidazo[1,2-a]pyridines. Org. Biomol. Chem. 2018, 16: 3721-3725. (IF: 3.423)

(7) Shengtao Xu, Guangyu Wang, Feijie Xu, Wenlong Li, Aijun Lin, Hequan Yao, Jinyi Xu*. Concise total synthesis of (+/-)-deguelin and (+/-)-tephrosin using a vinyl iodide as a key building block. J. Nat. Prod. 2018, 81: 1055-1059. (IF: 3.885)

(8) Jia Wang, Chaolei Wang, Zheng Wu, Xinnan Li, Shengtao Xu*, Jie Liu*, Qinying Lan, Zheying Zhu, Jinyi Xu*. Design, synthesis, biological evaluation, and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II). Chem. Biol. Drug Des. 2018, 91: 756-762.(IF: 2.328)

 

2017

(1) Wenlong Li, Honghao Sun, Shengtao Xu, Zheying Zhu, Jinyi Xu*. Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures. Future Med. Chem. 2017, 9: 1765-1794. (IF: 3.556)

(2) Shengtao Xu, Hong Yao, Mei Hu, Dahong Li, Zheying Zhu, Weijia Xie, Hequan Yao, Liang Wu*, Zhe-Sheng Chen, Jinyi Xu*. 6,7-Seco-ent-kauranoids derived from oridonin as potential anticancer agents. J. Nat. Prod. 2017, 80: 2391-2398. (IF: 3.885)

(3) Jichao Chen, Tianyu Wang, Shengtao Xu, Pengfei Zhang, Aijun Lin, Liang Wu*, Hequan Yao, Weijia Xie, Zheying Zhu*, Jinyi Xu*. Discovery of novel antitumor nitric oxide-donating beta-elemene hybrids through inhibiting the PI3K/Akt pathway. Eur. J. Med. Chem. 2017, 135: 414-423. (IF: 4.519)

(3) Jichao Chen, Tianyu Wang, Shengtao Xu, Aijun Lin, Hequan Yao*, Weijia Xie, Zheying Zhu*, Jinyi Xu*. Novel hybrids of natural beta-elemene bearing isopropanolamine moieties: Synthesis, enhanced anticancer profile, and improved aqueous solubility. Fitoterapia. 2017, 120: 117-125. (IF: 2.698)

(4) Jichao Chen, Tianyu Wang, Shengtao Xu, Aijun Lin, Hequan Yao*, Weijia Xie, Zheying Zhu*, Jinyi Xu*. Design, synthesis and biological evaluation of novel nitric oxide-donating protoberberine derivatives as antitumor agents. Eur. J. Med. Chem. 2017, 132: 173-183. (IF: 4.519)

(5) Shengtao Xu, Hong Yao, Lingling Pei, Mei Hu, Dahong Li, Yangyi Qiu, Guangyu Wang, Liang Wu*, Hequan Yao, Zheying Zhu*, Jinyi Xu*. Design, synthesis, and biological evaluation of NAD(P)H: Quinone oxidoreductase (NQO1)-targeted oridonin prodrugs possessing indolequinone moiety for hypoxia-selective activation. Eur. J. Med. Chem. 2017, 132: 310-321. (IF: 4.519)

(6) Zhaoliang Li, Yanchun Meng, Shengtao Xu, Wang Shen, Zhaoqing Meng, Zhenzhong Wang, Gang Ding, Wenzhe Huang, Wei Xiao*, Jinyi Xu*. Discovery of acylguanidine oseltamivir carboxylate derivatives as potent neuraminidase inhibitors. Bioorg. Med. Chem. 2017, 25: 2772-2781. (IF: 2.331)

(7) Jichao Chen, Ruifan Wang, Tianyu Wang, Qilong Ding, Aliahmad Khalil, Shengtao Xu, Aijun Lin, Hequan Yao*, Weijia Xie, Zheying Zhu*, Jinyi Xu*. Antioxidant properties of novel dinners derived from natural beta-elemene through inhibiting H2O2-induced apoptosis. ACS Med. Chem. Lett. 2017, 8: 443-448. (IF: 3.746)

(8) Shengtao Xu, Hong Yao, Shanshan Luo, Yun-Kai Zhang, Dong-Hua Yang, Dahong Li, Guangyu Wang, Mei Hu, Yangyi Qiu, Xiaoming Wu, Hequan Yao*, Weijia Xie, Zhe-Sheng Chen*, Jinyi Xu*. A novel potent anticancer compound optimized from a natural oridonin scaffold induces apoptosis and cell cycle arrest through the mitochondrial pathway. J. Med. Chem. 2017, 60: 1449-1468. (IF: 6.259)

(9) Hong Yao, Junkai Liu, Shengtao Xu*, Zheying Zhu, Jinyi Xu*. The structural modification of natural products for novel drug discovery. Expert Opin. Drug Discov. 2017, 12: 121-140. (IF: 3.876)

(10) Dahong Li, Tong Han, Xu Hu, Kangtao Tian, Shengtao Xu, Tingting Zhou, Keguang Cheng, Zhanlin Li, Huiming Hua, Jinyi Xu*. Synthesis, cytotoxicity and antimicrobial activity of new enmein-type kauranoid diterpenoid derivatives. Anticancer Agents Med Chem. 2017, 17: 1679-1688. (IF: 2.598)

 

2016

(1) Dahong Li, Tong Han, Jie Liao, Xu Hu, Shengtao Xu, Kangtao Tian, Xiaoke Gu,  Keguang Cheng*, Zhanlin Li, Huiming Hua*, Jinyi Xu*. Oridonin, a promising ent-kaurane diterpenoid lead compound. Int. J. Mol. Sci. 2016, 17: E1395. (IF: 3.257)

(2) Dahong Li, Xu Hu, Tong Han, Jie Liao, Wei Xiao*, Shengtao Xu, Zhanlin Li, Zhenzhong Wang, Huiming Hua*, Jinyi Xu*. NO-Releasing Enmein-Type Diterpenoid Derivatives with Selective Antiproliferative Activity and Effects on Apoptosis-Related Proteins. Molecules. 2016, 21:1193. (IF: 2.465)

(3) Dahong Li, Tong Han, Kangtao Tian, Shuang Tang, Shengtao Xu, Xu Hu, Lei Wang, Zhanlin Li, Huiming Hua*, Jinyi Xu*. Novel nitric oxide-releasing spirolactone-type diterpenoid derivatives with in vitro synergistic anticancer activity as apoptosis inducer. Bioorg. Med. Chem. Lett. 2016, 26: 4191-4196. (IF: 2.486)

(4) Hong Yao, Yu Zhou, Xia Chen, Pengfei Zhang, Jinyi Xu*, Hong Liu*. N-Heterocyclic Carbene Catalytic [4+2] Cyclization of 3-Alkylenyloxindoles with Enals: gamma-Carbon Activation for Enantioselective Assembly of Spirocarbocyclic Oxindoles. J. Org. Chem. 2016, 81: 8888-8899. (IF: 4.785)

(5) Shengtao Xu, Guangyu Wang, Yan Lin, Yanju Zhang, Lingling Pei, Hong Yao, Mei Hu, Yangyi Qiu, Zhangjian Huang, Yihua Zhang*, Jinyi Xu*. Novel anticancer oridonin derivatives possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: Design, synthesis, biological evaluation and nitric oxide release studies. Bioorg. Med. Chem. Lett. 2016, 26: 2795-2800. (IF: 2.486)

(6) Dahong Li, Xu Hu, Tong Han, Shengtao Xu, Tingting Zhou, Zhenzhong Wang*, Keguang Cheng, Zhanlin Li, Huiming Hua*, Wei Xiao, Jinyi Xu*. Synthesis, biological activity, and apoptotic properties of NO-Donor/enmein-type ent-kauranoid hybrids. Int. J. Mol. Sci. 2016, 17: E747. (IF: 3.257)

(7) Shengtao Xu, Shanshan Luo, Hong Yao, Hao Cai, Xiaoming Miao, Fang Wu*, Dong-Hua Yang, Xiaoming Wu, Weijia Xie, Hequan Yao, Zhe-Sheng Chen, Jinyi Xu*. Probing the anticancer action of oridonin with fluorescent analogues: Visualizing subcellular localization to mitochondria. J. Med. Chem. 2016, 59: 5022-5034. (IF: 5.589)

(8) Dahong Li, Tong Han, Shengtao Xu, Tingting Zhou, Kangtao Tian, Xu Hu,  Keguang Cheng*, Zhanlin Li, Huiming Hua*, Jinyi Xu*. Antitumor and antibacterial derivatives of oridonin: A main composition of Dong-Ling-Cao. Molecules. 2016, 21: E575. (IF: 2.465)

(9) Hao Cai, Xiaojing Huang, Shengtao Xu, Hao Shen, Pengfei Zhang, Yue Huang, Jieyun Jiang, Yijun Sun, Bo Jiang, Xiaoming Wu*, Hequan Yao, Jinyi Xu*. Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy. Eur. J. Med. Chem. 2016, 108: 89-103. (IF: 3.902)


 

专利:

1)     具有胆碱酯酶抑制活性的异色满-4-酮类衍生物、其制备方法及医药用途。专利授权号:ZL201510615725.6

2)     A-环改造的冬凌草甲素衍生物、其制备方法及用途。专利授权号:ZL201611034438.7

3)     冬凌草甲素14-O-取代氮芥衍生物、制备方法及用途。专利授权号 ZL201410196592.9

4)     20S, 24R/S-环氧-12β25-羟基-达玛烷-3β-胺衍生物的制备方法和用途、专利授权号:ZL201510066711.3

5)     一氧化氮供体型β-榄香烯衍生物及其制备方法和应用。专利授权号:ZL201710066664.1

6)     冬凌草甲素荧光探针、制备及其在靶细胞定位中的用途。专利授权号:ZL201510066677.X

7)     23-羟基白桦酸荧光探针、制备及其在细胞定位与摄取中的用途。专利授权号:ZL201510943477.8

8)     具有α-葡萄糖苷酶抑制活性的锍糖类天然产物及其衍生物的制备方法及用途。专利授权号:ZL201210505804.8

 


 

联系方式

 

E-mailjinyixu@china.com;  jinyixu@cpu.edu.cn