刘刚

教授 博士生导师 教育部长江学者特聘教授 清华大学“百人”计划教授

课题组研究兴趣

主要开展与发现和优化药物分子相关的药物化学与化学生物学的研究工作，重点是利用小分子化合物为探针分子，力图解决在寻找和优化药物先导化合物的过程中一些与药物化学和化学生物学相关的方法、技术、理论等前沿性科学问题，包括合成“骨架导向”的小分子杂环化合物、合成多肽及多肽模拟物、合成以天然产物为骨架分子的化学库，并利用这些合成分子研究与肿瘤的发生、发展相关的信号通路、微环境等新药物靶标。课题组的研究目标是寻找、发现和优化抗肿瘤、抗感染性疾病药物以及疫苗。

2007年来发表的主要研究性论文

1. Xiaofan Lu, Li Liu, Xu Zhang, Terrence Lau, Stephen Kwok-Wing Tsui,   Yuanxi Kang,  Purong Zheng, Gang Liu^* and Zhiwei Chen^*, F18, a novel small molecule NNRTI, inhibits HIV-1 replication using distinct binding motifs, Antimicrobial Agents and Chemotherapy, 2011, accepted.
2. Yu Yan, Qifei Zhong, Nan Zhao, Gang Liu*, Cascade Mitsunobu reaction for the preparation of substituted 2-benzoxazole-N-phenyl and 2-benzimidazole-N-phenyl derivatives, Molecule Diversity, 2011, accepted.
3. Rui Liu, Zhuhui Huang, Michael G. Murray, Xiaoyong Guo, Gang Liu*, Quinoxalin-2(1H)-One Derivatives As Inhibitors Against Hepatitis C Virus, Journal of Medicinal Chemistry, 2011, 54, 5747–5768.
4. Purong Zheng, Shichao Lu, Gang Liu^*, An Unexpected C-C Cleavage Reaction: Mild and Oxidation Free Access to o-OH and o-NH-Ts Benzoic Acids or Benzoamides, Molecule Diversity, 15:971–977.
5. Chunyan Han, Jinlan Zhang, Li Li, Mingyue Zheng, Yao Xiao, Yan Li*, Gang Liu*. Correlation of the physicochemical and pharmacokinetic properties of bicyclic privileged structures for the determination of their drug-likeness. Molecule Diversity, 15:857–876.
6. Yu YAN, Jianjun ZHANG, Zijie LIU, Ruiming XU, Xiao HU, Gang LIU*, A reversal method of diversity introduction of benzimidazole to synthesize H⁺/K⁺-ATP enzyme inhibitors, Bioorg. & Med. Chem. Lett., 2011, 21, 4189-4192.
7. Nan Zhao, Yao Ma, Shengmei Zhang, Xin Fang, Zhenglun Liang, Gang Liu*, New muramyl dipeptide (MDP) mimics without the carbohydrate moiety as potential adjuvant candidates for a therapeutic hepatitis B vaccine (HBV), Bioorg. & Med. Chem. Lett., 2011, 21, 4292-4295.
8. Yao Ma, Nan Zhao, Gang Liu*, Muramyl Dipeptide’s Derivative and Paclitaxel Conjugate (MTC-220) Simultaneously Prevents Tumor Growth and Metastasis in Mice, Journal of Medicinal Chemistry, 2011, 54(8): 2767-77.
9. Ning Zhu, Fa Zhang, Gang Liu*, Dynamic Covalent Chemistry of Disulfides Offers a Highly Efficient Synthesis of Diverse Benzofused Nitrogen-Sulfur Heterocycles in One Pot. Journal of Combinatorial Chemistry, 2010, 12, 531-540.
10. Gang Li, Dongmei Wang, Mingna Sun, Guangyan Li, Jinfeng Hu, Yun Zhang, Yuhe Yuan, Haijie Ji, Naihong Chen*, Gang Liu^*. Discovery and Optimization of Novel 3-Piperazinyl Coumarin Antagonist of Chemokine – like factor 1 with oral Anti-asthma activity in mice. Journal of Medicinal Chemistry, 2010, 53 (4), 1741–1754.
11. Hai Xue, Xiaofan Lu, Purong Zheng, Li LIU, Chunyan Han, Jinping HU, Zijie Liu, Tao MA, Yan LI, Lin WANG , Zhiwei CHEN*, Gang LIU*, Highly suppressing wide type HIV-1 and Y181C mutation by 10-Chloromethyl-11-Demethyl-12-oxo calanolide A with druggable profile. Journal of Medicinal Chemistry, 2010, 53, 1397–1401.
12. Hao Wu, Xilei Xie, Gang Liu*, 3, 6, 7-Diversities of 4(3H)-Quinazolinones and Anti Tumor Activities, Journal of Combinatorial Chemistry, 2010, 12, 346–355.
13. Leilei Zhang, Yu Yan, Zijie Liu, Abliz Zeper, Gang Liu*, Identification of Peptide Substrate and Small Molecule Inhibitors of Testis-specific Serine/Threonine Kinase1 (TSSK1) By the Developed Assays, Journal of Medicinal Chemistry, 2009, 52, 4419-4428.
14. Dongmei Wang, Mingna Sun, Gang Liu*, Substituent Diversity-Directed Synthesis of Indole Derivatives, Journal of Combinatorial Chemistry, 2009, 11, 556–575.
15. Fa Zhang, Wei Zhang, Yan Zhang,  Dennis P. Curran, and Gang Liu*, Synthesis and Applications of Light-Fluorous Glycosyl Donor, The Journal of Organic Chemistry, 2009, 74 (6), 2594-2597.
16. Tao MA, Li LIU, Hai XUE, Li LI, Chunyan HAN, Lin WANG, Zhiwei CHEN, Gang LIU*, The Chemical Library and Structure-Activity Relationship of Calanolide-A Analogues against HIV-1, Journal of Medicinal Chemistry, 2008, 51, 1432–1446.
17. Yu-Yan Chen, Wen-Yi He, Yan Wu, Chang-Qun Niu, and Gang Liu*, Dynamic Selection of Novel Vancomycin N-Terminal Derivatives by Resin-bound Reversed D-Ala-D-Ala, Journal of Combinatorial Chemistry, 2008, 10, 914-922.
18. Xuqin Li, Junli Yu, Song Xu, Nan Wang, Hongzhen Yang, Zheng Yan, Guifang Cheng, Gang Liu*, Chemical Conjugation of Muramyl Dipeptide and Paclitaxel to Explore the Combination of Immunotherapy and Chemotherapy for Cancer, Glycoconjugate Journal, 2008, 25: 415–425.
19. Tao MA, Qi GAO, Zhiwei Chen, Lin WANG, Gang LIU*, Chemical Resolutions of (±)-Calanolide A, (±)-Cordatolide A and Their 11-Demethyl Derivatives, Bioorg. & Med. Chem. Letts. 2008， 18, 1079–1083.
20. Hai-Yan Zhao, Gang Liu* Solution-Phase Parallel Synthesis of Diverse 1,5-Benzodiazepin-2-ones, Journal of Combinatorial Chemistry, 2007, 9, 1164 - 1176.
21. Li Li, Zhanguo Wang, Yuyan Chen, Yunyun Yuan, Guanxin Wang, Gang Liu*, Design and Synthesis of Novel Tricyclic Compounds Based On 4H-Benzo[1,4]thiazin-3-one and 1,1-Dioxo-1,4-dihydro-2H-1l⁶-benzo[1,4]thiazin-3-one, Journal of Combinatorial Chemistry, 2007, 9, 959 - 972.
22. Hai-Yan Zhao, Gang Liu*, Solution-Phase Synthesis of 2, 3-Dihydro-1,5-benzothiazepin-4 (5H)-ones, Journal of Combinatorial Chemistry, 2007, 9, 756-772.
23. Zhanguo Wang, Yunyun Yuan, Yuyan Chen, Ganghcun Sun, Xianghong Wu, Shenmei Zhang, Chunyan Han, Guanxing Wang, Li Li, and Gang Liu*, Design and Parallel Solution-phase Synthesis of Diverse Scaffold Compounds Based On 3,4-Dihydrogen-3-oxo-1,4-benzothiazine, Journal of Combinatorial Chemistry, 2007, 9, 652-660.
24. Yunyun Yuan, Gang Liu,* Li Li, Zhanguo Wang, and Lin Wang, Synthesis of Benzo[1,4]oxazin-3-one-based Diverse Compounds Using 1, 5-Difluoro-2, 4-dinitrobenzene, Journal of Combinatorial Chemistry, 2007, 9, 158-170.
25. Tian-Ming Yang, Gang Liu*, Solution-Phase Parallel Synthesis of 3-Substituted Indolin-2-ones, Journal of Combinatorial Chemistry, 2007, 9, 86-95.
26. Gang Liu,* Li Li, Binbin Kou, Suode Zhang, Liang Zhang, Yunyun Yuan, Tao Ma, Yan Shang, and Yuancheng Li, Benzofused Tricycles Based On 2-Quinoxalinol, Journal of Combinatorial Chemistry, 2007,  9, 70-78.

联系方式：

电话&传真：010-62797740
邮箱地址：gangliu27@tsinghua.edu.cn