李志裕教授
个人简介:李志裕,博士,教授,博士生导师,中国药科大学药学院药学实验教学中心主任。
研究方向:新药分子设计与合成研究
1991年毕业于中国药科大学药学院获得硕士学位,2000年获中国药科大学博士学位,2001年-2002年 意大利University della Carabulia化学系进行博士后研究。一直工作在教学科研第一线,参加了本科药物化学精品课程,研究生化学药物工业技术精品课程建设,多次获得教育部及江苏省教学成果奖。主编教材两部,研究领域主要包括:HMG还原酶抑制剂,拓扑异构酶抑制剂、新型黄酮类抗肿瘤药物的设计与合成,雄激素受体拮抗剂的研究等。完成了长春瑞滨,氟伐他汀,匹伐他汀,莫西沙星等十几种原料药工艺研究开发。主持国家自然基金两项,主持完成江苏省自然基金两项,参加重大医药专项三项,主持完成横向课题20余项,近两年来,在国内外学术刊物上已发表SCI论文30余篇,申请专利18项,其中16项获得授权。三次得江苏省科学进步奖。
正在承担的科研项目:
1、主持国家自然科学基金面上项目:具有肿瘤多靶点作用特征的汉黄芩素衍生物的研究,项目批准号:21072232,
2、主持国家自然科学基金面上项目基于突变型雄激素受体结构的新型拮抗剂设计及构效关系研究项目批准号:21372260
3、参加参加科技部“重大新药创制”科技重大专项(抗肿瘤一类新药注射用千层纸素的临床前研究,2012ZX09103-101-050);
4、加参加科技部“重大新药创制”科技重大专项(抗肿瘤1类药物候选化合物GL-V9的研究,2013ZX09103-001-007);
代表性文章:
1. Zhouling Xie, Sen Feng , Ying Wang , Chen Caoa, Jing Huang , Yahui Chenb,Yi Kong b, **, Zhiyu Li , *Design, synthesis of novel tryptophan derivatives for antiplateletaggregation activity based on tripeptide pENW (pGlu-Asn-Trp) European Journal of Medicinal Chemistry 102 (2015) 363-374
2. Tianze Jiang, Yingying Sun,Zhichao Yin, Sen Feng, Liping Sun & Zhiyu Li*,Research progress of indoleamine 2,3-dioxygenase inhibitors Future Med. Chem. (2015) 7(2), 185–201
3. Yi Kong *, Ying Wang , Wei Yang, Zhouling Xie, Zhiyu Li* LX0702, a novel snake venom peptide derivative, inhibits thrombus formation via affecting the binding of fibrinogen with GPIIb/IIIa Journal of Pharmacological Sciences 127 (2015) 462-466 2.15
4. Yahui Chen , 1, Ying Wang a, 1, Zhouling Xie b, Xin Ming c, Zhiyu Li b, **, Yi Kong a, *A tryptophan derivative TD-26 attenuates thrombus formation by inhibiting both PI3K/Akt signaling and binding of fibrinogen to integrin aIIbb3 Biochemical and Biophysical Research Communications 465 (2015) 516-522 2.406
5. Zhouling Xie, Youli Zhou, Wei Zhao, He Jiao, Yu Chen, Yong Yang, Zhiyu Li a,Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation Bioorganic & Medicinal Chemistry Letters xxx (2015) xxx–xxx (in press) 2.55
6. Zhouling Xie, Chen Cao,Sen Feng, Jing Huang& Zhiyu Li*,Progress in the research of GPIIb/IIIa antagonists Future Med. Chem. (2015) 7(9), 1149–1171 3.74
7. Ji, H. X., Zou, Y. L., Duan, J. J., Jia, Z. R., Li, X. J., Wang, Z. Li L, Li Y.W., Liu,G.Y., Tong,M.Q., Li, X. Y,, Zhang,G.H, Dai,X.R., He,L., Li Z.Y*., Cao C*, Yang, Y*. (2013). The Synthetic Melanocortin (CKPV) 2 Exerts Anti-Fungal and Anti-Inflammatory Effects against Candida albicans Vaginitis via Inducing Macrophage M2 Polarization. PloS one, 8(2), e56004. 4.092
8. Yi Zhang · Li Zhao · Xin Li · Yajing Wang · Jing Yao ·Hu Wang · Fanni Li · Zhiyu Li*· Qinglong Guo* V8, a newly synthetic flavonoid, induces apoptosis through ROS mediated ER stress pathway in hepatocellular carcinoma Arch Toxicol (2014) 88:97–107 5.98
9. Jun-Peng Zhang Jie Huangd Chao Liu Xu-Fang Lu Bao-Xiang Wu Li Zhao Na Lu Qing-Long Guo Zhi-Yu Li* Cheng Jiang. Discovery of a series of pyridopyrimidine derivatives as potential topoisomerase I inhibitors[J]. Chinese Chemical Letters, 2014 (007): 1025-1028.
10. Lu, Xufang; Dun, Kang; Wang, Yang; Yang, Yong; You, Qidong; Li, Zhiyu*. Recent Androgen Receptor Antagonists in Prostate Cancer[J]. Mini reviews in medicinal chemistry, 2014, 14(8): 655-663. 3.18
11. Rong Luo a, Jubo Wanga, Li Zhao b, Na Lub, Qidong You a, Qinglong Guo b, Zhiyu Li* a,Synthesis and biological evaluation of baicalein derivatives as potent antitumor agents Bioorg. Med. Chem. Lett. 24 (2014) 1334–1338 2.33