李广哲，教授、博士生导师；

中国化学会、日本化学会、日本药学会、日本癌分子靶向治疗学会会员；

邮箱：liguangzhe@dlut.edu.cn

【个人经历】

• 2002.09－2006.07  大连理工大学制药工程，工学学士

• 2006.09－2009.07  大连理工大学药物工程，理学硕士

• 2009.10－2013.03  日本东北大学药学研究科，药学博士

• 2013.04－2014.04  日本东北大学药学研究科，助教

• 2014.05－2015.09  东京工业大学化学生命科学研究所，助教

• 2015.12－2021.12　大连理工大学化工学院药学系，副教授

• 2022.01－至今　　大连理工大学化工学院药学系，教授

• 2016.10－至今　　大连理工大学化工学院药学系教工党支部书记兼副系主任

【研究内容】

面向人民生命健康，围绕恶性肿瘤等重大疾病治疗的新靶点、新药物和新方法开展应用基础研究：

1. 分子靶向抗肿瘤药物的研究：HIF-1 抑制剂、热休克蛋白HSP90、HSP60 抑制剂等；

2. 用于光动力、声动力治疗的光敏剂、声敏剂的设计与开发；

3. BNCT 治疗中含硼药物的设计与开发；

4.药物活性分子导向的绿色有机合成新方法的开发。

【代表性研究成果】

18. Wang, L.; Li, G.*; Cao, L.; Shao, K.; Li, Y.; Zhang, X.; Zhao, J.; Zhao, W.* A novel water-soluble chlorin-based photosensitizer for low-fluence photodynamic therapy. ACS Pharmacol. Transl. Sci., 2022, 2, 110-117.

17. Li, G.*; Yu, G.; Wang, C.; Morita,T.; Zhang, X.; Nakamura, H.* Copper(i)-catalysed intramolecular hydroarylation-redox cross-dehydrogenative coupling of N-propargylanilines with phosphites. Org. Biomol. Chem., 2022, 20, 113-116.

16. Wang, L.; Li, G.*; Cao, L.; Dong, Y.; Wang, Y.; Wang, S.; Li, Y.; Guo, X.; Zhang, Y.; Sun, F.; Du, X.; Su, J.; Li, Q.; Peng X.; Shao, K.*; Zhao, W.* An Ultrasound-Driven Immune Boosting Molecular Machine for Systemic Tumor Suppression. Sci. Adv., 2021, 7, eabj4796.

15. Li, G.*; Shao, Y.; Pan Y.; Li, Y.; Wang, Y.; Wang, L.; Wang, X.; Shao, K.; Wang, S.; Liu, N.; Zhang, J.; Zhao, W.; Nakamura, H. Total synthesis and biological evaluation of 7-Hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy. Bioorg. Med. Chem. Lett., 2021, 50, 128338.

14. Wang, S.; Wang, X.; Shao, Y.; Shao, K.; Wang, Y.; Guo, X.; Dong, H.; Zhao, W.; Li, Y.; Li, G.* Synthesis and evaluation of 3-(phenylethynyl)-1,1′-biphenyl-2-carboxylate derivatives as new HIF-1 inhibitors. Bioorg. Chem., 2021, 116, 105298.

13. Li, G.*; Wang, C.; Li, Y.; Shao, K.; Yu, G.; Wang, S.; Guo, X.; Zhao, W.; Nakamura, H. Zinc(ii)-catalyzed intramolecular hydroarylation-redox cross-dehydrogenative coupling of N-propargylanilines with diverse carbon pronucleophiles: facile access to functionalized tetrahydroquinolines. Chem. Commun., 2020, 7333-7336.

12. Dong, Y.; Li, G.*; Wang, L.; Cao, L.; Li, Y.; Zhao, W.* Anti-tumor evaluation of a novel methoxyphenyl substituted chlorin photosensitizer for photodynamic therapy. J. Photoch. Photobio. B, 2020, 211, 112015.

11. Li, G.*; Dong, H.; Ma, Y.; Shao, K.; Li, Y.; Wu, X.; Wang, S.; Shao, Y.; Zhao, W. Structure-activity relationships study of neolamellarin A and its analogues as hypoxia inducible factor-1 (HIF-1) inhibitors. Bioorg. Med. Chem. Lett., 2019, 29, 2327-2331.

10. Wang, S.; Liu, L.; Guo, X.; Li, G.*; Wang, X.; Dong, H.; Li, Y.; Zhao, W. Synthesis of novel natural product-like diaryl acetylenes as hypoxia inducible factor-1 inhibitors and antiproliferative agents. RSC Adv., 2019, 9, 13878-13886.

9. Li, Y.; Li, G.*; Dong, Y.; Ma, X.; Dong, H.; Wu, Q.; Zhao, W.* Orobanone analogues from acid-promoted aromatization rearrangement of curcumol inhibit hypoxia-inducible factor-1 (HIF-1) in cell-based reporter assays. Bioorg. Chem., 2019, 85, 357-363.

8. Li, G.; Shao, K.; SokkeUmeshappa C. Recent progress in blood-brain barrier transportation research. In : Gao H, Gao X(Eds.), Brain Targeted Drug Delivery System, Elsevier, 2019, 33-51.

7. Li, G.; Ban, H.; Nakamura, H. Design of Carborane‐Based Hypoxia‐Inducible Factor Inhibitors. In: Evamarie H, Clara V T (Eds.), Boron‐Based Compounds: Potential and Emerging Applications in Medicine, Wiley, 2018, 35-59. 

6. Li, G.; Nakamura, H.* Synthesis of 2-Indolyltetrahydroquinolines by Zinc(II)-Catalyzed Intramolecular Hydroarylation-Redox Cross-Dehydrogenative Coupling of N-Propargylanilines with Indoles. Angew. Chem. Int. Ed., 2016, 55, 6758-6761.

5. Li, G.; Azuma, S.; Sato, S.; Minegishi, H.; Nakamura, H.* ortho-Carboranylphenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity and heat shock protein (HSP) 60 chaperon activity. Bioorg. Med. Chem. Lett., 2015, 25, 2624-2628.

4. Li, G.; Azuma, S.; Minegishi, H.; Nakamura, H. Synthesis and biological evaluation of meta-carborane-containing phenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity. J. Organomet. Chem., 2015, 798, 189-195.

3. Li, G.; Arisawa, M.; Yamaguchi, M.* Rhodium-catalyzed synthesis of unsymmetrical di(aryl/heteroaryl) methanes using aryl/heteroarylmethyl ketones via CO-C bond cleavage. Chem. Commun., 2014, 50, 4328-4330.

2. Li, G.; Arisawa, M.; Yamaguchi, M.* Rhodium-Catalyzed Synthesis and Reactions of N-Acylphthalimides. Asian J. Org. Chem., 2013, 2, 983-988.

1. Arisawa, M.*; Li, G.; Yamaguchi, M.* Rhodium-catalyzed synthesis of 2,3-diaryl-1,4-diketones via oxidative coupling of benzyl ketones using α-thioketone oxidizing reagent. Tetrahedron Lett., 2013, 54, 1298-1301.

 

【个人奖励】

• 2016 年，入选大连理工大学“星海学者”人才培育计划“星海骨干”

• 2018 年，入选大连理工大学“星海学者”人才培育计划“星海优青”

• 2016 年，大连理工大学青年教师讲课竞赛二等奖

• 2019 年，全国高等学校药学类专业青年教师教学能力大赛 一等奖

• 2019 年，全国高等学校药学类专业青年教师微课教学大赛 特等奖

2022 年招收药学（学硕），药物工程（学硕），生物与医药（专硕）硕士研究生，

欢迎制药工程、药学、化学、化工、生物工程、生物学等相关专业的考生报考！

2022.8 -- 2027.8

常务理事(辽宁省细胞生物学学会淋巴细胞肿瘤及头颈部肿瘤医工融合专业委员会)

2022.6 -- 2027.6

理事(大连市药学会)

2020.1 -- 2020.12

青年编委(《中国化学快报》编辑部)