Personal profiles:
Name :Jiang Sheng Gender : male
Date of Birth :June 14 , 1976 _ _ Specialties : Medicinal Chemistry
Education : Doctor of Science Professional Technical Position : Professor, Doctoral Supervisor
E-mail : jiang_shengg @ 126.com Telephone (Tel.) : 18688888237
learning experience
1993 , 9-1997 , 7 : China Pharmaceutical University, Medicinal Chemistry, Bachelor
1997 , 9-2000 , 7 : China Pharmaceutical University, Medicinal Chemistry, Master
2000 , 9-2003 , 7 : Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Organic Chemistry, Ph.D.
work experience
2003 , 11-2007 , 11 : National Institutes of Health ( NIH ) Cancer Institute ( NCI ); Medicinal Chemistry, Postdoc
2007 , 12-2016 , 12 : Guangzhou Institute of Biology and Health, Chinese Academy of Sciences, medicinal chemistry, doctoral supervisor ,Research group leader.
2017,1 - PRESENT : China Pharmaceutical University, medicinal chemistry, doctoral supervisor ,Research group leader.
Main academic achievements, scientific and technological achievements and innovations
Dr. Jiang Sheng graduated from the Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences in 2003 with a Ph.D. in organic chemistry. From 2003 to 2007 , he worked as a postdoctoral researcher at the National Cancer Institute ( NCI/NIH ) of the U.S. Department of Health. After returning to China in 2008 , he served as a researcher and doctoral tutor of the "Hundred Talents Program" of Guangzhou Institute of Biomedicine and Health , Chinese Academy of Sciences .Research group leader . Now he is a doctoral supervisor of the Department of Medicinal Chemistry, China Pharmaceutical University .Research group leader. He is also a member of the American Chemical Society, a member of the American Peptide Society, a member of the Chinese Chemical Society, and a senior member of the Chinese Pharmaceutical Association. Employed for several international journals such as J. Med Chem. , Bioorg. Med. Chem. Lett. , Bioorg. Med. Chem. , Eur. J. Med Chem. , J. Org. Chem , Organic LettersSpecial reviewer for other journals, and review expert for projects such as the National Natural Science Foundation of China. In recent years, a total of 68 SCI papers have been published, including a series of innovative articles published in the international core journals Angew. Chem. Int. Ed., Organic Letters, Journal of Medicinal Chemistry and Journal of The American Chemical Society . Among them, " Rationally Designed Inhibitors Identify STAT3 N-Domain as a Promising Anticancer Drug Target " was published in the international publication ACS Chemical BiologyAfter it was published, it aroused strong interest from international peers and was selected as one of the most-accessed articles of the 1st quarter of 2008 .
At the same time, research on the following projects was completed:
1. Completed the design and synthesis of the anti-tumor natural product Annonaceous Acetogenins analogs. We used the natural annua lactone- Bullatacin as a template, simplified the double tetrahydrofuran ring into a ethylene glycol diether structure , retained its basic skeleton, and used the concepts of rational drug design, parallel synthesis, fragment assembly, etc. , to effectively establish annua lactone. A library of analog molecules with completely new chemical structures. Among them, the activity of compound AA019 on HT-29 tumor cells was 15 times that of doxorubicin , and it was not toxic to normal cells. In the in vitro test, the compound AA019 can effectively inhibit the growth of lewis lung cancer in nude mice at an oral dose of 10 mg/kg (compared with the control group, the inhibition rate is more than 60% ). Currently, the compound is in preclinical studies.
2. Completed the design and synthesis of natural cyclic peptide ( SFTI-1 ) analogs. Using the binding model of SFTI-1 and protease, a series of novel cyclic peptides were successfully designed and synthesized by computer-aided drug design method. Among them, SFTI-15 had better proteolytic activity ( Ki = 10 nM ) and It has good selectivity and stability. Moreover, further in vivo and in vitro experiments showed that it can effectively inhibit tumor growth.
3. Completed the design and synthesis of Grb2-SH2 polypeptide inhibitors. Taking G1TE as the lead, the design, synthesis and structure-activity relationship of G1TE analogs were systematically carried out . Among them , the activity of G177 on Grb2-SH2 is more than 1000 times that of G1TE . A batch of Grb2-SH2 antagonists with cell-level tumor growth inhibitory activity were also discovered during development, providing promising pharmacophore patterns and lead compounds for anti-tumor drug candidates.
4. Completed the design and synthesis of cyclic peptide inhibitors of STAT-3 . This work was published in "ACS Chemical Biology" titled "Rationally Designed Inhibitors Identify STAT3 N-Domain as a Promising Anticancer Drug Target" and was named the most-accessed article of the first quarter of 2008 by ACS . 1st quarter of 2008 ).
5. Participated in the University of Michigan as one of the main collaboratorsWang ShaomengProfessor presided over the new anti-tumor drug AT-101 , a broad-spectrum inhibitor of Bcl-2 family proteins, a Spirooxindole class of p53-MDM2 interaction blockers, isoflavone class Bcl-2 family protein inhibitors and protein IAP small molecule inhibitors, etc. Development of antineoplastic drugs.
6. Completed the design and synthesis of selective inhibitors of histone deacetylation type I enzymes. Among them, the median inhibitory concentration ( IC50 ) of compound Lar-7 on tumor cell lines can reach as low as 1.0 nM ( 26 cell line experiments in vitro showed that the IC50 for multiple series of tumor cells was between 1-40 nM ), and the anti-tumor activity was A similar drug vorinostat ( SAHA ) has been listed abroad 10-100 times; and it is non-toxic to normal cells. The preliminary in vivo pharmacodynamic evaluation and acute toxicity evaluation of Lar-7 also reflect its low toxicity and high efficiency: it is resistant to human prostate cancer Du-145 , human breast cancer MDA-MB-231 and human leukemia imatinib Cells ( T315I ) subcutaneously transplanted tumor in nude mice had obvious inhibitory effect, and the relative tumor proliferation rates ( T/c% , Day-21 ) were 29.64% , 20% and 37% , respectively . Preliminary acute toxicity test showed that the LD50 of Lar-7 in Kunming mice( 256.2 mg/kg ) is far greater than that of the similar drug Romidepsin ( 3.6 mg/kg ) that has been marketed abroad, showing extremely low toxicity. Currently, the compound is in preclinical studies.
7. Design and synthesize a new biotin-labeled cyclic peptide compound , and successfully " catch " a new protein "r-catenin" with the labeled compound . We verified and found that this protein is a key protein in the self-renewal of leukemia cancer stem cells , and the compounds we designed can effectively overcome the problem of imatinib resistance by inhibiting this protein.
8. Completed the design and synthesis of multiple inhibitors of EGFR, Her-2 and HDC . Among them, the median inhibitory concentration ( IC50 ) of compound JSNMPT-17 on multiple series of tumor cells is between 1-10 nM , and its anti-tumor activity is about 50 times that of a foreign phase II clinical drug ( CUC-101 ) . Currently , the in vivo pharmacodynamic evaluation of JSNMPT-17 is in progress.
9. Completed the total synthesis of 7 natural products , they are Largazole, FK-228, Argyrins A and E, (-)-Norsecurinine, (+)-Niruroidine and Flueggine A.
10. Completed the design and synthesis of IDO inhibitors. Among them, the antitumor activity of the compound JQIDO-003 is comparable to that of foreign phase II clinical drugs. Currently , the in vivo pharmacodynamic evaluation of JQIDO-003 is ongoing.
Major scientific research projects hosted in the past five years
serial number | Subject name | Numbering | host or participate | Start and end time | expenses ( 10,000 yuan ) | category |
1 | Synthesis of Compounds and Derivatives with Stem Cell Regulation Activity | 2009CB940904 | host | 2009.1- 2013.12 | 6.9 million | 973 project sub-topics |
2 | Study on the simplified analog AA-005 of annua lactone as an anticancer drug | 2009ZX09103-101 | host | 2009.1- 2010 ．12 | 1.26 million | National New Drug Innovation Major Project |
3 | Structure-activity relationship and antitumor activity of histone deacetylase inhibitor Lar-7 | 21172220
| host | 2012.1- 2015.12 | 600,000 _ | National Natural Science Foundation of China surface item |
4 | Total Synthesis of Argyrin A | 20972160 | host | 2010.1- 2012.12 | 350,000 _ | National Natural Science Foundation of China surface item |
5 | Proteolytic enzyme cyclic peptide inhibitor and its antitumor activity | 20802078 | host | 2009.1- 2011.12 | 180,000 _ | National Natural Science Foundation of China Youth Fund |
6 | Design and Synthesis of Cyclic Peptide Inhibitors of Proteolytic Enzymes | NNCAS-2008-8 | host | 2009.1- 2010 ．12 | 500,000 _ | Novartis Nordisk - Chinese Academy of Sciences Joint Fund |
7 | Proteolytic enzyme inhibitors and their antitumor activity | KSCX2-YW-R-215 | host | 2010.1- 2010.12 | 200,000 _ | Important direction project of knowledge innovation project of Chinese Academy of Sciences |
8 | Design and synthesis of small molecule inhibitors of proteolytic enzymes | 8151066302000008 | host | 2009.1- 2011.12 | 50,000 _ | Natural Science Foundation of Guangdong Province |
9 | Total Synthesis of Flueggines A and B | 21472191 | host | 2015.1- 2018.12 | 900,000 _ | National Natural Science Foundation of China surface item |
10 | Study on AA-005 as Anticancer Drug | 2013A022100019 | participate | 2015.1- 2017.12 | 1.5 million | Guangdong Province New Drug Creation Project |
11 | Construction of Molecular Probes for Histone Deacetylation Type I Enzymes and Research on Early Diagnosis and Treatment | 2016A050502036 | host | 2016.1- 2018.12 | 500,000 _ | Guangdong Province International Cooperation Project |
12 | Molecular probes of histone deacetylation type I enzymes as early diagnosis and treatment of tumors | | host | 2017.5- 2020.4 | 1 million | Guangzhou Industry-University-Research Collaborative Innovation Major Project |
1. Sheng Jiang (invited speaker), “Discovery of Novel Class I Histone Deacetylase Inhibitors through Total Synthesis of Natural Products”, National Cancer Institute 2015 (2015,10,20Fredercik, US).
2. Sheng Jiang (invited speaker), “Discovery of Novel Class I Histone Deacetylase Inhibitors through Total Synthesis of Natural Products”, Chinese Pharmaceutical University 2015 (2015,7,10Nanjing, China).
2. Sheng Jiang (invited speaker), "Discovery of Novel Class I Histone Deacetylase Inhibitors through Total Synthesis of Natural Products", The 4th Natural Product Total Synthesis - Youth Symposium (2015,7, Chengdu , China).
3. Sheng Jiang (invited speaker), "Discovery of Novel Class I Histone Deacetylase Inhibitors", 10th National Natural Organic Chemistry Conference of Chinese Chemical Society (2014,11 Guangzhou, China).
4. Sheng Jiang (invited speaker), “Design, Synthesis and Biological Evaluation of Novel Class I Histone Deacetylase Inhibitors through Total Synthesis of Natural Products”, 2012 ( Shanghai , China).
5. Sheng Jiang (invited speaker), “From Total Synthesis of Natural Products to Discovery of New Histone Deacetylase Inhibitors”, The 4th China-Thailand Workshop on Natural Products and Drug Discovery, Trang Province, Thailand, November 26-30, 2012
6. Sheng Jiang (invited speaker), “Discovery of New Histone Deacetylase Inhibitors”, The 28th CCS National Congress (2012,Chendu, China)
7. Sheng Jiang (invited speaker), “Design and synthesis New Histone Deacetylase 1 (HDAC1) inhibitors as potential anticancer drugs”, National Cancer Institute, Frederick, MD, 2010
8. Sheng Jiang (invited speaker), “Total Synthesis of Largazole and its analogues potential anticaner drugs”, The 5 th CCS National Congress on organic chemistry (2009, Xian,China).
9. Sheng Jiang (invited speaker), “Potent antagonists of the Grb2-SH2 domain: Not relying on phosphotyrosine mimics”, Chinese Pharmaceutical University 2006 (2006,Nanjing, China).
10. Sheng Jiang , et al. “Potent antagonists of the Grb2-SH2 domain: Not relying on phosphotyrosine mimics”, 232 th American Chemical Society Meeting (9/10-9/14, 2006).
11. Sheng Jiang , et al. “Synthesis and Evaluation of Analogs of SFTI-1, Potent Inhibitors of the Type II Transmembrane serine protease, Matriptase”, 230th American Chemical Society Meeting (8/28-9/1, 2005).
12. Sheng Jiang , et al. “Synthesis of Symmetrical Dimeric Dicarboxylic Acid Linked Peptides on Solid support”, 19th American Peptide Symposium (6/18-23, 2005).
13. Sheng Jiang , et al. “First Chemical Synthesis of Butenolide2", The 2 nd CCS National Congress on organic chemistry and the 1 st CCS National Congress on Chemical Biology (2002, China).
2011 The 14th Chinese Pharmaceutical Association - Servier Youth Medicinal Chemistry Award
20 10 Hundred Talent Award
20 07 NIH Fellows award for the Research Excellence
1996 Excellent Student Scholarship
1. “Synthesis and application of ether bond modified chiral annonaceous acetogenins compound”
Licensed to Shanghai Institute of Organic Chemistry
Inventors: ZJ Yao, YL Wu and S. Jiang.
Patent No. CN1477103
2. “Method for synthesis of largazole and its analogs as antitumor agents.”
Inventors: S. Jiang, G. Zhou, B. Yin, X. Zeng, and Z. Hu.
Patent No. CN 101781321
3. “Annonaceous acetogenins analogs as antitumor agents and their preparation, pharmaceutical compositions and use in the treatment of cancer”
Inventors: S. Jiang, ZJ Yao, G. Zhou, Q. Xiao, Y. Liu
Patent No. CN 101982464
4. “Preparation of cyclopeptides as histone deacetylase inhibitors”
Inventors: S. Jiang, S. Li, Y. Yao, F. Zhang, Y. Chao, H. Ye, M. Chen
CN Patent Serial No. CN102391359
5. “Preparation of triazole compounds as histone deacetylase inhibitors.”
Inventors: S. Jiang, Z.Tu, Y. Yao, C. Liu, H. Yao, X. Xue,
Patent No. CN 102311398
6. “Process for preparation of FK228”
Inventors: S. Jiang, J. Xu, S. Li, H. Yao, X. Zeng, Y. Yao,
Patent No. CN 102276689
7. “Quinoxalinyl bis(N-oxide) derivatives and their application as ligands in Cu-catalyzed CO coupling reaction”
Inventors: Z. Yao, S. Jiang,
Patent No. CN 102060790
8. “Quinoline derivative-N-oxide ligands, their preparation method and application in NC coupling”
Inventors: Z. Yao, S. Jiang,
Patent No. CN 101899003
9. “Method for preparing epichlorohydrin tetramer and its reaction with formaldehyde derivative”
Inventors: D. Zhang, J. Su, S. Jiang,
Patent No. CN 103864727
10. “Preparation of largazole analog compounds as antitumor agents”
Inventors: S. Jiang, Z. Tu, X. Li, Y. Yao, Y. Qiu
Patent No. CN 103601742
11. “13-membered cyclic peptide as histone deacetylase inhibitor and its preparation”
Inventors: H. Xiang, G. Wang, S. Jiang, Z. Tu,
Patent No. CN 103232474
12. "Preparation of N-containing heterocyclic derivatives as histone deacetylase I inhibitor"
Inventors: S. Jiang , Z. Tu, Q. Sun, C. Liu, Y. Yao, Y. Qiu,
Patent No. CN 103086971
13. “Preparation of 3-(pyridin-3-yl)acrylamide derivatives as nicotinamide phosphoribosyltransferase inhibitors useful for the treatment of cancer”
Inventors: S. Jiang, Z. Tu, D. Zheng, D. Qin, J. Bai, X. Qin, Y. Yao, Y. Liu, Y. Qiu, J. Chen
Patent No. CN 104557863/PCT090572
Representative papers since engaging in scientific research
1. J. Bai, , C. Liao, D. Qin, Y. Liu, X. Qing, J. Chen, Z. Li, Z. Tu, S. Jiang.* Structure-Based Design of Potent Nicotinamide Phosphoribosyltransferase Inhibitors with Promising In Vitro and in Vivo Antitumor Activities. J. Med. Chem . 2016 , 59 , 5766-5779.
2. N. Ma, Y. Luo, Y. Wang, C. Liao, W.-C. Ye*, S. Jiang* .Selective histone deacetylase inhibitors with anticancer activity. Curr. Top. Med. Chem. 2016 , 16 , 415-426.
3. Y. Jin, Y. Yao, L. Chen, X. Zhu, B. Jin, Y. Shen, J. Li, X. Du, Y. Lu, S. Jiang* , J. Pan*.Depletion of γ-catenin by Histone Deacetylase Inhibition Confers Elimination of CML Stem Cells in Combination with imatinib. Theranostics . 2016 , 6, 1947-1962.
4. Y. Yao,Z. Tu,C. Liao, Z. Wang, S. Li, H. Yao, Z. Li, S. Jiang* .Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro Selectivity for Cancers Cells and in Vivo Antitumor Activities. J. Med. Chem . 2015 , 58 , 7672-7680.
5. Y. Yao,Z. Li, Y. Qiu, J. Su, S. Jiang* .Unprecedented reactions: from epichlorohydrin to epoxyglycidyl substituted divinyl ether and its conversion into epoxyglycidyl propargyl ether . Scientific Reports . 2015, 5 , srep14231.
6. N. Ma, Y. Wang, B. Zhao, W.-C. Ye*, S. Jiang* .The application of click chemistry in the synthesis of agents with anticancer activity. Drug Design, Development and Therapy . 2015 , 50 , 1585-1599.
7. J. Zhang, H. Zhou, S. Jiang, J. Jin, W. Li, W. Wang, S. Su. AA092, an annonaceous acetogenin mimetic, attenuates angiogenesis in a mouse model of inflammation-induced corneal neovascularization. International Immunopharmacology . 2015 , 28 , 997-1002.
8. Y. Zhou, G. Hou, S. He, Z. Xiao, H. Xu, Y. Qiu,S. Jiang, H. Zheng, Z. Li. Psora-4, a Kv1.3 Blocker, Enhances Differentiation and Maturation in Neural Progenitor Cells. CNS Neuroscience & Therapeutics . 2015 , 21 , 558-567.
9. N. Ma, Y. Yao, B.-X. Zhao, Y. Wang, W.-C. Ye*, S. Jiang* .Total synthesis of securinega alkaloids (-)-norsecurinine, (-)-niruroidine and (-)-flueggine A. Chem. Commun . 2014 , 50 , 9284-9287.
10. X. Zhu, L. Chen, S. Jiang , C. Chen, Y. Yao, D. Chen, H. Xue, J. Pan * .PQJS380: a novel lead compound to induce apoptosis in acute lymphoblastic leukemia cells. Cancer Biology & Therapy . 2014 , 15 , 119-127.
11. J. Su, Y. Qiu, S. Jiang*, D. Zhang*.New Ligands for Copper-Catalyst C[n.63743]N Coupling Reactions at Gentle Temperature. Chinese Journal of Chemistry . 2014 , 32(8) , 685-688.
12. J. Su, Y. Qiu, K. Ma, Y. Yao, Z. Wang, X. Li, D. Zhang, Z. Tu, S. Jiang* .Design, synthesis, and biological evaluation of larga zole derivatives: alteration of the zinc-binding domain. Tetrahedron. 2014 , 70 , 7763-7769.
13. H. Zhou, S. Jiang, J. Chen, X. Ren, J. Jin, SB Su*. Largazole, an inhibitor of class I histone deacetylases, attenuates inflammatory corneal neovascularization. European Journal of Pharmacology. 2014 , 740 , 619-626.
14. H. Zhou,S. Jiang, J. Chen, SB Su*. Suberoylanilide hydroxamic acid suppresses inflammation-induced neovascularization.Can. J. Physiol. Pharmacol. 2014 , 92 , 879-885.
15. Y. Liu, Y. Liu, Z. Liu, G. Zhou, Z.-J.Yao* , S. Jiang* . Identification of novel bivalent mimetics of annonaceous acetogenins via a scaffold-hopping strategy. Bioorg. Med. Chem. Lett. 2014 , 24 , 1650-1653.
16. Y. Liu, Q. Xiao, Y. Liu, Z. Li, Y. Qiu, G.-B. Zhou, Z.-J.Yao, S. Jiang* . Biological evaluation of new mimetics of annonaceous acetogenins: alteration of right scaffold by click linkage with aromatic functionalities. Eur. J. Med. Chem . 2014 , 78 , 248-258.
17. Y. Yao, C. Liao, Z. Li, Z. Wang, Q. Sun, C. Liu, Z. Tu * , S. Jiang* . Design, Synthesis, and Biological Evaluation of 1, 3-Disubstituted- Pyrazole Derivatives as New Class I and IIb Histone Deacetylase Inhibitors. Eur. J. Med. Chem . 2014 , 86 , 639-652.
18. Y. Zhao, X. Fang, Y. Wang, J. Zhang, S. Jiang , Z. Liu, Z. Ma, L. Xu, E. Li, K. Zhang. Comprehensive Analysis for Histone Acetylation of Human Colon Cancer Cells Treated with a novel HDAC Inhibitor. Current Pharmaceutical Design . 2014 , 20 , 1866-1873.
19. D. Zou, Y. Qiu, Z. Tu, C. Liao, J. Luo, Q. Meng, R. Yao, Z. Li, S. Jiang* .. Biological evaluation of 2-methylpyrimidine derivatives as active pan Bcr-Abl inhibitors. ScienceChina: Chemistry . 2014 , 57 , 823-832.
20. Q. Meng, F. Li,S. Jiang, Z. Li*.Novel 64 Cu-labeled CUDC-101 for in vivo PET Imaging of histone deacetylases. ACS Medicinal Chemistry Letters . 2013 , 4, 858-862.
21. L. Wu, Z. Wen, Y. Qiu, X. Chen, H. Chen, M. Wei, Z. Liu, S. Jiang*, G. Zhou*.Largazole arrests cell cycle at G1 phase and triggers proteasomal degradation of E2F1 in lung cancer cells; ACS Medicinal Chemistry Letters . 2013 , 4, 921-926.
22. Y. Yao, H. Yao,S. Jiang*, X. Xue*.Progress in clinical study of histone deacetylase inhibitors as anticancer agents; Chinese J New Drugs . 2013 , 22 (3), 1-7.
23. Q. Sun , Y. Yao, C. Liu, H. Li, H. Yao, X. Xue, J. Liu, Z. Tu * , S. Jiang* . Design, Synthesis, and Biological Evaluation of Novel Histone Deacetylase 1 Inhibitors through click chemistry. Bioorg. Med. Chem. Lett. 2013 , 23, 3295-3299.
24. X. Li, Z. Tu, H. Li, C. Liu, Z. Li, Q. Sun, Y. Yao, J. Liu, S. Jiang* .Biological evaluation of new largazole analogues: Alteration of macrocyclic scaffold with Click chemistry; ACS Medicinal Chemistry Letters . 2013 , 4 , 132-136.
25. Y. Qiu, W. Jia, Z. Yao, F. Wu, S. Jiang *. 2-Carbomethoxy-3-hydroxyquinoxaline-di- N - oxide as a novel ligand for the copper-catalyzed coupling reaction of phenols and aryl halides. Organic & Biomolecular Chemistry. 2013 , 11, 1502-1510.
26. Yang, Mei; He, Jiangbo; Cheng, Yongxian; Jiang, Sheng* . Synthesis of 3-[(Z)-pentadec-8-enyl]catechol and its anti-angiogenesis activity. Chinese Journal of Organic Chemistry . 2013 , 33(6), 1319-1325.
27. D. Che, K. Yang, H. Xiang,S. Jiang* . New ligands for copper-catalyzed CN coupling reactions with aryl halides; Tetrahedron Letters . 2012 , 53, 7121-7124.
28. Y. Liu, X. Cheng, L. Guo, C. Mao, Y. Chen, H. Liu, Q. Xiao, S. Jiang , Z. Yao, G. Zhou. Identification of an annonaceous acetogenin mimetic, AA005 , as an AMPK activator and autophagy inducer in colon cancer cells; PLoS One . 2012 , 7 , e47049.
29. K. Su, Y. Qiu,; Y.Yao,; D. Zhang, S. Jiang* . 8-hydroxyquinolin-N-oxide-promoted copper-catalyzed CS cross-coupling of thiols with aryl iodides; Synlett . 2012 , 23, 2853-2857.
30. Q. Xiao, Y. Liu, Y. Qiu, G. Zhou, C. Mao, Z. Li, Z.-J. Yao * , S. Jiang* . Potent Antitumor Mimetics of Annonaceous Acetogenins Embedded with an Aromatic Moiety in the Left Hydrocarbon Chain Part; J. Med. Chem. 2011 , 54 , 525-533.
31. K. Yang, Y. Qiu, Z. Li, Z. Wang, S. Jiang* , Ligands for Copper-Catalyzed C-N Bond Forming Reactions with 1 Mol% CuBr as Catalyst. J. Org. Chem , 2011 , 76, 3151-3159.
34. W. Wu, Z. Li, G. Zhou, S. Jiang* . Total synthesis of argyrins A and E. Tetrahedron. Lett . 2011 , 52 , 2488-2491.
35. Z. Yao, X. Zeng, W. Yi,S. Jiang* . Stereoselective Synthesis of (S,E)-2-(trimethylsilyl)ethyl 3-hydroxy-7-(tritylthio) hept-4-enoate. Letters in Organic Chemistry, 2011 , 8 , 66-69.
36. Q. Xiao, Y. Liu, Y. Qiu, Z. Yao, G. Zhou, Z.-J.Yao* , S. Jiang* . Design, synthesis of symmetrical bivalent mimetics of annonaceous acetogenins and their cytotoxicities. Bioorg. Med. Chem. Lett. 2011 , 21 , 3613-3615.
37. S. Li, H. Yao, J. Xu * , S. Jiang* . Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors. Molecules , 2011 , 16 , 4681-4694.
39. Z. Yao, Y. Xu, M. Zhang, S. Jiang , MC Nicklaus, C. Liao. Discovery of a novel hybrid from finasteride and episteride as5a-reductase inhibitor. Bioorg. Med. Chem. Lett, 2011 , 21 , 475-478.
40. W. Hong, Y. Qiu, Z. Yao, Z. Wang,S. Jiang* . Palladium-Catalyzed Direct C–H Arylation of Unactivated Arenes with Aryl Halides. Tetrahedron. Lett . 2011 , 52, 4916-4919.
41. X. Zeng, W. Huang, Y. Qiu, S. Jiang *. Efficient Copper-Catalyzed Synthesis of Anilines by Employing Aqueous Ammonia. Organic & Biomolecular Chemistry. 2011 , 9, 8224-8227.
42. Y. Xu, F. Wu, Z. Yao, S. Jiang . Synthesis of quinoxaline 1,4-di-N-oxide analogues and crystal structure of 2-carbomethoxy-3-hydroxyquinoxaline-di-N-oxide. Molecules , 2011 , 6894-6901 .
44. J. Zheng, B. Yin, W. Huang, X. Li, H. Yao, Z. Liu, S. Jiang *. Efficient and selective cleavage of the t -butoxycarbonyl group from di- t -butylimidodicarbonate using catalytic bismuth (III) bromide in acetonitrile. Tetrahedron. Lett . 2009 , 50 , 5094-5097.
45. S. Jiang* , C. Liao, L. Bindu, B. Yin, KW Worthy, RJ Fisher, TR Burke, Jr., MC Nicklaus, PP Roller. Discovery of thioether-bridged cyclic pentapeptides binding to Grb2-SH2 domain with high affinity. Bioorg. Med. Chem. Lett.2009 , 19 , 2693-2698.
46. Z. Nikolovska-Coleska, J. Meagher, S. Jiang, C. Yang, S. Qiu, PP Roller, J. Stuckey, S. Wang. Interaction of a Cyclic, Bivalent Smac Mimetic with the X-Linked Inhibitor of Apoptosis Protein. Biochemistry . 2008 , 47 , 9811-9824.
47. S. Jiang *, Z. Li, K. Ding, PP Roller. Recent Progress of Synthetic Studies to Peptide and Peptidomimetic Cyclization. Current Organic Chemistry. 2008 , 12 , 1502-1542.
48. Z. Nikolovska-Coleska, J. Meagher, S. Jiang, SA Kawamoto, W. Gao, H. Yi, D. Qin, PP Roller, J. Stuckey, S. Wang. Design and characterization of bivalent Smac-based peptides as antagonists of XIAP and development and validation of a fluorescence polarization assay for XIAP containing both BIR2 and BIR3 domains. Anal Biochem. 2008 , 374 , 87-98.
52. P. Li, S. Jiang, SL Lee, CY Lin, MD Johnson, CJ Michejda, RB Dickson, PP Roller.Synthesis and evaluation of analogs of SFTI-1, potent inhibitors of the Type II transmembrane serine protease, Matriptase. J. Med. Chem. 2007 , 50, 5976-5983.
54. H. Sun, Z. Nikolovska-Coleska, J. Lu, J. Meagher, C. Yang, S. Qiu, Y. Tomita, Y. Ueda, S. Jiang, Krajewski, PP Roller, JA Stuckey, S.Wang.Design, Synthesis and Characterization of A Potent, Non-Peptide, Cell-Permeable, Bivalent Smac Mimetic that Concurrently Targets both the BIR2 and BIR3 Domainsin XIAP. J. Am. Chem. Soc. 2007 , 129, 15279-15294.
57. J. Chen, Z. Nikolovska-Coleska, CY Yang, C. Gomez, W. Gao, K. Krajewski, S. Jiang , P. P. Roller, S. Wang. Design and synthesis of a new, conformationally constrained , macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.Bioorg. Med. Chem. Lett.2007 , 17 , 3939-3942.
58. S. Jiang, P. Li, CC Lai, JA Kelley,P. Roller.Design and Practical Synthesis of Fully Protected analogs of L-γ-Carboxyglutamic Acid. J. Org. Chem. 2006 , 71 , 7307-7314.
59. S. Jiang, P. Li, M. Peach, RJ Fisher, TR Burke, M. Nicklaus, PP Roller. Structure-based design of potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics. Biochem. Biophys. Res. Commun. 2006 , 349 , 497-503.
60. S. Jiang, CC Lai, JA Kelley, PP Roller. A Practical Synthesis of Fully Protected L-γ-Carboxyglutamic Acid (L-Gla). Tetrahedron. Lett . 2006 , 47, 23-25.
62. Y. Zhao, S. Jiang, YW Guo, Z.-J.Yao. Synthesis of two naturally occurring 4-hydroxylated butenolides with PTP1B inhibitory activity. Chinese. J. Chem . 2005 , 23 , 173-175.
63. S. Jiang , Y. Li, XG Chen, TS Hu, YL Wu, Z.-J. Yao. Parallel fragment assembly strategy towards multiple-ether mimicry of anticancer annonaceous acetogenins. Angew. Chem. Int. Ed . 2004 , 43 , 329-334.
66. S. Jiang , YL Wu, ZJ Yao. Synthesis of A Mimicking Hybrid of Annonaceous acetogenin with Steroid for considerable Antitumor Activity Investigation.Chinese J. Chem. 2002 , 20 , 1393-1400.
67. S. Jiang , YL Wu, ZJ Yao. First Synthesis of Mosquito larvicidal Butenolides I and II. Chinese J. Chem. 2002 , 20 , 692-696.
Research areas
1. Rational design, synthesis and structure-activity relationship research of active small molecules and polypeptide compounds targeting specific pathogenic genes.
2. Total synthesis of natural products with antitumor activity and discovery of new leading drugs.
Admissions Information
Admissions Major
100701 - Medicinal Chemistry
Admissions direction
Design and Synthesis of
Anticancer Drugs Design and Synthesis of Anticancer Drugs
Education background
Bachelor of Science
-- PhD
study abroad
2003, 11~ 2007, 11 National Cancer Institute, National Institutes of Health (NIH, NCI), Postdoctoral fellow
work experience
2007, 11 ~ present, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences
Publication information
Published papers
(1) Total synthesis of argyrins A and E, Tetrahedron. Lett., 2011, corresponding author
(2) Design, synthesis of symmetrical bivalent mimetics of annonaceous acetogenins and their cytotoxicities, Bioorg. Med. Chem. Lett., 2011, corresponding author
(3) Potent Antitumor Mimetics of Annonaceous Acetogenins Embedded with an Aromatic Moiety in the Left Hydrocarbon Chain Part, J. Med. Chem, 2011, corresponding author
(4) Ligands for Copper Catalyzed CN Bond Forming Reactions with CuBr as Catalyst, J. Org Chem, 2011, corresponding author
(5) Synthetic Routes and Biological Evaluation of Largazole and Its Analogues as Potent Histone Deacetylase Inhibitors, Molecules, 2011, corresponding author
(6) New Ligands That Promote Cross-Coupling Reactions between Aryl Halides and Unactivated Arenes, Org. Letters, 2011, corresponding author
(7) Total Synthesis and Biological Evaluation of Largazole and Derivatives with Promising Selectivity for Cancers Cells, Organicc. Lett., 2010, corresponding author
Research activities
scientific research projects
Presided over the National Natural Science Foundation of China, the 973 sub-project, and the National New Drug Creation Major Project.
guide students
Currently guiding students
Xiao Qicai Master student 077901-Medicinal chemistry
Wu Wenbin Postgraduate 077901-Medicinal Chemistry
Liu Yanghan Postgraduate 077901-Medicinal Chemistry
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