李志裕教授
個人簡介:李志裕,博士,教授,博士生導師,中國藥科大學藥學院藥學實驗教學中心主任。
研究方向:新藥分子設計與合成研究
1991年畢業于中國藥科大學藥學院獲得碩士學位,2000年獲中國藥科大學博士學位,2001年-2002年 意大利University della Carabulia化學系進行博士后研究。一直工作在教學科研第一線,參加了本科藥物化學精品課程,研究生化學藥物工業技術精品課程建設,多次獲得教育部及江蘇省教學成果獎。主編教材兩部,研究領域主要包括:HMG還原酶抑制劑,拓撲異構酶抑制劑、新型黃酮類抗腫瘤藥物的設計與合成,雄激素受體拮抗劑的研究等。完成了長春瑞濱,氟伐他汀,匹伐他汀,莫西沙星等十幾種原料藥工藝研究開發。主持國家自然基金兩項,主持完成江蘇省自然基金兩項,參加重大醫藥專項三項,主持完成橫向課題20余項,近兩年來,在國內外學術刊物上已發表SCI論文30余篇,申請專利18項,其中16項獲得授權。三次得江蘇省科學進步獎。
正在承擔的科研項目:
1、主持國家自然科學基金面上項目:具有腫瘤多靶點作用特征的漢黃芩素衍生物的研究,項目批準號:21072232,
2、主持國家自然科學基金面上項目基于突變型雄激素受體結構的新型拮抗劑設計及構效關系研究項目批準號:21372260
3、參加參加科技部“重大新藥創制”科技重大專項(抗腫瘤一類新藥注射用千層紙素的臨床前研究,2012ZX09103-101-050);
4、加參加科技部“重大新藥創制”科技重大專項(抗腫瘤1類藥物候選化合物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