李志裕

李志裕,男,药物化学博士,教授,博士生导师,药学院副院长,先后在中国药科大学药物化学(本科、硕士以及博士),University della Carabulia(博士后)学习工作。

主要研究方向为天然产物的全合成与结构优化、及新药分子的设计与合成研究。近年来主要从事新型抗肿瘤药物的研发,在活性天然产物的结构改造、靶向抗肿瘤药物的设计与合成等方面取得显著成绩。

现主持两项国家自然基金面上项目,一项江苏省自然基金面上项目,主持完成了两项江苏省自然基金项目,参加了三项国家重大新药创制重大科技专项项目,主持横向课题15项,在国家1.1类药物注射用汉黄芩素的研究中,负责合成工艺研究,该项目现获得III期临床研究批件。以第一发明人申请专利20余项,获得授权15项。近三年来以第一通讯作者发表SCI等学术论文30余篇。

联系方式zhiyuli@cpu.edu.cn

近年来主要研究课题方向:

1.新型雄激素受体拮抗剂的设计与合成及活性研究;国家自然科学基金面上项目,批准号:21372260

2.天然多肽AAP做为先导物的GPIIb/IIIa受体拮抗剂研究;国家自然科学基金面上项目,批准号:81273375

3.靶向色氨酸-犬尿氨酸通路中关键双加氧酶的全新骨架抑制剂的研究;江苏省面上项目(2017年)

4.吲哚胺2,3-双加氧酶1IDO1)抑制剂的设计与合成以及生物活性研究

5.新型选择性CDK9抑制剂的设计、合成及生物学研究

代表性论文及著作:

1.Zhouling Xie, Benimana Oscar, Yi Kong**,Zhiyu Li*, Design, synthesis and evaluation of novel 2-amino-3-(naphth-2-yl)propanoic acid derivatives as potent inhibitors of platelet aggregation,European Journal of Medicinal Chemistry, 125 (2017) 197-209.

2.Tinghan Li, Tianwei Weng, Jubo Wang, Zhihui Wei, Lu Zhao,Zhiyu Li*. A practical and efficient approach to the preparation of bioactive natural product Wogonin.Org. Process Res. Dev.21 (2017) 171-176.

3.Oscar Benimana, Lulu Zhao, Yi Kong,Zhiyu Li*, Zhouling Xie*,The progress in the research of antiplatelet agents (1995-2017).Future Medicinal Chemistry, 9 (2017) 1087-1110.

4.Fei Ji, Yun Fan, Run Yang, Yueyan Yang, Dianwen Yu, Minyu Wang,Zhiyu Li*. Regioselective Synthesis of Thiocyanate-Containing Isoxazolines via FeIII/K2S2O8-Mediated Radical Thiocyanation/Cyclization Cascade Reaction of β,γ-Unsaturated Oximes.Asian Journal of Organic Chemistry. 2017.

5.Mingping Wang, Wei Tian, Chongqing Wang, Shihai Lu, Chao Yang, Juan Wang, Yunlong Song,

Youjun Zhou, Ju Zhu,Zhiyu Li*, Canhui Zheng*. Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites.Bioorganic & Medicinal Chemistry Letters26 (2016) 5207–5211

6.Minzan Zuo, Xi Xu, Zhouling Xie, Raoling Ge, Ziyu Zhang,Zhiyu Li*, Jinlei Bian*. Design and synthesis of indoline thiohydantoin derivatives based on enzalutamide as antiproliferative agents against prostate cancer.Eur. J. Med. Chem.125(2017) 1002-1022.

7.Tinghan Li, Tianwei Weng, Minzan Zuo, Zhihui Wei, Ming Chen,Zhiyu Li*, Recent progress of cyclin-dependent kinase inhibitors as potential anticancer agents,Future Medicinal Chemistry, 2016.

8.Bian J, Li T, Weng T, Wang J, Chen Y, Li Z. Synthesis, evaluation and quantitative structure-activity relationship (QSAR) analysis of Wogonin derivatives as cytotoxic agents.Bioorganic & Medicinal Chemistry Letters,27 (2017) 1012-1016.

9.Raoling Ge, Qian Zhao, Zhouling Xie, Lu Lu, Qinglong Guo,Zhiyu Li*, Li Zhao*, Synthesis and Biological Evaluation of 6-fluoro-3-phenyl-7-piperazinyl Quinolone Derivatives as Potential Topoisomerase I Inhibitors,European Journal of Medicinal Chemistry, 122 (2016) 465-474.

10.Zhouling Xie, Yu Chen, Pengfei Xu, Youli Zhou, Qian Zhao, He Jiao,Zhiyu Li*, Design, synthesis and bioevaluation of 1H-indole-4-carboxamide derivatives as potent Poly (ADP-ribose) polymerase-1 inhibitors,RSC Advance84 (2016) 80784-80796.

11.Zhouling Xie, Sen Feng, Ying Wang, Chen Cao, Jing Huang, Yahui Chen,Yi Kong **,Zhiyu Li*,Design, synthesis of novel tryptophan derivatives for antiplateletaggregation activity based on tripeptide pENW (pGlu-Asn-Trp)European Journal of Medicinal Chemistry102 (2015) 363-374

12.Qian Zhao, Xi Xu, Zhouling Xie, Xiao Liu, Qidong You, Qinglong Guo, Yi Zhong,Zhiyu Li*Design, synthesis and biological evaluation of 3-substituted indenoisoquinoline derivatives as topoisomerase I inhibitorsBioorganic & Medicinal Chemistry Letters26 (2016) 1068–1072.