蒋晟

个人概况:

姓名 蒋晟                  性别       

出生年月1976614      从事专业∶药物化学        

教育程度∶理学博士           专业技术职务教授,博士生导师

E-mailjiang_shengg@126.com    电话 (Tel.) 18688888237

 

学习经历

19939-19977:中国药科大学,药物化学,学士

19979-20007:中国药科大学,药物化学,硕士

20009-20037:中科院上海有机化学研究所,有机化学,博士

 

工作经历

200311-200711:美国国家健康研究院(NIH)癌症研究所(NCI);药物化学,博士后

200712-2016,12:中科院广州生物与健康研究院,药物化学,博士生导师, 课题组组长。

2017,1-现在:中国药科大学,药物化学,博士生导师, 课题组组长。

 

主要学术成就、科技成果及创新点

蒋晟博士2003年毕业于中国科学院上海有机化学研究所,并获得有机化学博士学位。2003—2007在美国卫生部国立癌症研究所(NCI/NIH)从事博士后研究。2008年归国后,中国科学院广州生物医药与健康研究院“百人计划”研究员、博士生导师, 课题组组长现为中国药科大学药物化学系博士生导师, 课题组组长。兼任美国化学会会员,美国多肽学会会员,中国化学会会员,中国药学会高级会员。被聘为多个国际期刊如J. Med Chem.Bioorg. Med. Chem. Lett. Bioorg. Med. Chem.Eur. J. Med Chem. J. Org. ChemOrganic Letters 等杂志特约审稿人,国家自然科学基金项目等项目评审专家。近年来,发表了68SCI论文,包括:国际核心杂志Angew. Chem. Int. Ed., Organic Letters, Journal of Medicinal Chemistry Journal of The American Chemical Society 等发表的一系列具有创新性的文章。其中,“Rationally Designed Inhibitors Identify STAT3 N-Domain as a Promising Anticancer Drug Target”在国际刊物ACS Chemical Biology 上发表后,引起了国际同行的浓厚兴趣,被评选为该刊物2008 年第一季度最热门文章之一(most-accessed article of the 1st quarter of 2008)。

  同时,完成了以下项目的研究:

1.      完成了抗肿瘤天然产物Annonaceous Acetogenins类似物的设计和合成。我们以天然番荔枝内酯-Bullatacin为模板,简化双四氢呋喃环为乙二醇二醚结构, 保留其基本骨架,利用合理药物设计、平行合成、片断组装等概念,有效的建立了番荔枝内酯类似物分子库,并且此化合物库具有全新的化学结构。其中,化合物AA019 HT-29肿瘤细胞的活性是阿霉素的15倍,并且对正常细胞无毒性。在体外试验中,化合物AA01910mg/kg的口服剂量下能有效地抑制裸鼠上 lewis肺癌的生长(与对照组相比,抑制率达60%以上)。目前,该化合物处于临床前研究。

 

2.      完成了天然环肽(SFTI-1)类似物的设计和合成工作。利用SFTI-1与蛋白裂解酶的结合模型,以计算机辅助药物设计的方法成功设计合成了一系列全新的环肽,其中SFTI-15具有较好的蛋白裂解酶抑制活性(Ki = 10 nM)并且它具有较好的选择性和稳定性。并且,进一步体内与体外实验表明它能够有效抑制肿瘤的生长。

3.      完成了Grb2-SH2的多肽类抑制剂的设计和合成工作。以G1TE为先导物,系统开展了G1TE类似物的设计合成和构效关系研究。其中G177Grb2-SH2的活性是G1TE1000多倍。并且在开发中还发现了一批具有细胞水平抑制肿瘤生长活性的Grb2-SH2 拮抗剂,为抗肿瘤候选药物提供了富有前景的药效团模式和先导化合物。

4.      完成了STAT-3的环肽类抑制剂的设计和合成工作。该项工作以题为“Rationally Designed Inhibitors Identify STAT3 N-Domain as a Promising Anticancer Drug Target”发表在“ACS Chemical Biology”并且被ACS评为2008年第一季度阅读最多的论文(most-accessed article of the 1st quarter of 2008)。

5.      作为主要合作者之一参与美国密西根大学王少蒙教授主持的Bcl-2家族蛋白广谱抑制剂类抗肿瘤药物AT-101Spirooxindolep53-MDM2相互作用阻断剂、异黄酮类Bcl-2家族蛋白抑制剂以及蛋白IAP小分子抑制剂等新型抗肿瘤药的开发。

6.      完成了组蛋白去乙酰化I型酶选择性抑制剂的设计与合成工作。其中化合物Lar-7对肿瘤细胞株的半数抑制浓度(IC50 )最低可达1.0 nM(体外26株细胞株实验显示,对多系列肿瘤细胞的IC501-40 nM之间),抗肿瘤活性是国外已上市同类药物伏立诺他(SAHA10-100倍;并且对正常细胞无毒性。Lar-7的初步体内药效学评价及急性毒性评价同样体现了其低毒、高效的特点:对人前列腺癌Du-145、人乳腺癌MDA-MB-231和人白血病伊马替尼耐药细胞(T315I)裸小鼠皮下移植瘤的生长有明显的抑制作用,其相对肿瘤增殖率(T/c%Day-21)分别为29.64% 20%37%。初步急毒试验表明Lar-7对昆明种小鼠的LD50256.2 mg/kg)远大于国外已上市同类药物Romidepsin3.6 mg/kg),表现极低的毒性。目前,该化合物处于临床前研究。

7.      设计合成新的生物素标记的环肽化合物,利用该标记化合物成功钓到新的蛋白质 “r-catenin” 。我们验证发现该蛋白是白血病肿瘤干细胞自我更新的关键蛋白,我们设计的化合物通过抑制该蛋白可以有效克服伊马替尼耐药的问题。

8.      完成了EGFR, Her-2HDC多重抑制剂的设计与合成工作。其中化合物JSNMPT-17对多系列肿瘤细胞的半数抑制浓度(IC50 )在1-10 nM之间,抗肿瘤活性是国外二期临床的药物(CUC-10150倍左右。目前,JSNMPT-17的体内药效学评价正在进行中。

9.      完成了7个天然产物的全合成工作,它们是Largazole,FK-228,Argyrins A E, (-)-Norsecurinine, (+)-Niruroidine and Flueggine A

10.  完成了IDO抑制剂的设计与合成工作。其中化合物JQIDO-003抗肿瘤活性与国外二期临床的药物相当。目前,  JQIDO-003的体内药效学评价正在进行中。

 

近五年内主持的主要科研项目

 

序号

课题名称

编号

主持或参与

起止时间

经费

(万元)

类别

1

具有干细胞调控活性的化合物及衍生物的合成

2009CB940904

主持

2009.1-

2013.12

690

973项目子课题

2

番荔枝内酯简化类似物AA-005作为抗癌药物的研究

2009ZX09103-101

主持

2009.1-

201012

126

国家新药创制重大专项

3

组蛋白去乙酰化酶抑制剂Lar-7的构效关系及其抗肿瘤活性的研究

 

21172220

 

 

主持

2012.1-

2015.12

 

60

国家自然科学基金

面上项目

 

4

Argyrin A 的全合成研究

20972160

主持

2010.1-

2012.12

35

国家自然科学基金

面上项目

5

蛋白裂解酶环肽抑制剂及其抗肿瘤活性研究

20802078

主持

2009.1-

2011.12

18

国家自然科学基金

青年基金

6

蛋白裂解酶环肽抑制剂的设计与合成

NNCAS-2008-8

主持

2009.1-

201012

50

诺华诺德-中科院联合基金

7

蛋白裂解酶抑制剂及其抗肿瘤活性研究

KSCX2-YW-R-215

主持

2010.1-

2010.12

20

中国科学院知识创新工程重要方向项目

8

蛋白裂解酶小分子抑制剂的设计与合成

 

8151066302000008

主持

2009.1-

2011.12

 

5

 

广东省自然科学基金

 

9

Flueggines A and B的全合成研究

21472191

主持

2015.1-

2018.12

90

国家自然科学基金

面上项目

10

AA-005作为抗癌药物的研究

2013A022100019

参与

2015.1-

2017.12

150

广东省新药创制专项

11

组蛋白去乙酰化I型酶的分子探针的构建及其早期诊治效果的研究

2016A050502036

主持

2016.1-

2018.12

50

广东省国际合作专项

12

组蛋白去乙酰化I型酶的分子探针作为肿瘤早期诊治的研究

 

主持

2017.5-

2020.4

100

广州市产学研协同创新重大专项

 

特邀报告

 

1. Sheng Jiang (invited speaker), “Discovery of Novel Class I Histone Deacetylase Inhibitors through Total Synthesis of Natural Products”, National Cancer Institute 2015 (2015,10,20 Fredercik, US).

2. Sheng Jiang (invited speaker), “Discovery of Novel Class I Histone Deacetylase Inhibitors through Total Synthesis of Natural Products”, Chinese Pharmaceutical University 2015 (2015,7,10 Nanjing, China).

2. Sheng Jiang (invited speaker), “Discovery of Novel Class I Histone Deacetylase Inhibitors through Total Synthesis of Natural Products”, 第四届天然产物全合成-青年学术研讨会 (2015,7, 成都, China).

3. Sheng Jiang (invited speaker), “Discovery of Novel Class I Histone Deacetylase Inhibitors”, 中国化学会第十届全国天然有机化学学术会议 (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 (上海, 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 5th 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”, 232th 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”, 19 th American Peptide Symposium (6/18-23, 2005).

13. Sheng Jiang, et al. “First Chemical Synthesis of Butenolide 2”, The 2nd CCS National Congress on organic chemistry and the 1st CCS National Congress on Chemical Biology (2002, China).

 

奖励及荣誉:

2011  14届中国药学会—施维雅青年药物化学奖

2010    Hundred Talent Award

2007    NIH Fellows award for the Research Excellence        

1996      Excellent Student Scholarship

 

发明专利

 

1.   “Synthesis and application of ether bond modified chiral annonaceous acetogenins compound”

Licensed to Shanghai Institute of Organic Chemistry

Inventors: Z. J. Yao, Y. L. 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, Z.J. 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 C-O coupling reaction”

Inventors: Z. Yao, S. Jiang, 

Patent No. CN 102060790

8.        “Quinoline derivative-N-oxide ligands, their preparation method and application in N-C 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/PCT 090572

 

  

 

从事科研工作以来的代表性论文

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-Catalyzed 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 largazole derivatives: alteration of the zinc-binding domain. Tetrahedron. 2014, 70, 7763-7769.

13.    H. Zhou, S. Jiang, J. Chen, X. Ren, J. Jin, S. B. 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, S. B. 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. Science China: Chemistry. 2014, 57, 823-832.

20.    Q. Meng, F. Li, S. Jiang, Z. Li*. Novel 64Cu-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 C-N 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 C-S 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.

32.    Y. Qiu, Y. Liu, K. Yang, W. Hong, Z. Li, Z. Wang, S. Jiang*. New Ligands That Promote Cross-Coupling Reactions between Aryl Halides and Unactivated Arenes. Org. Letters, 2011, 13, 3556-3559.

33.    K. Yang, Z. Li, Z. Wang, S. Jiang*. Highly Efficient Synthesis of Phenols by Copper-Catalyzed Hydroxylation of Aryl Iodides, Bromides, and Chlorides. Org. Letters, 2011, 13, 4340-4343.

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.

38.    L. Johannessen, J. Remsberg, V. Gaponenko, K. M. Adams, J. J. Barchi, S. G. Tarasov, S. Jiang,  N. I. Tarasova. Peptide Structure Stabilization by Membrane Anchoring and its General Applicability to the Development of Potent Cell-Permeable Inhibitors. ChemBioChem. 2011, 12, 914-921.

39.    Z. Yao, Y. Xu, M. Zhang, S. Jiang, M. C. Nicklaus, C. Liao. Discovery of a novel hybrid from finasteride and epristeride as 5a-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.

43.    X. Zeng, B. Yin, Z. Hu, C. Liao, Z. Li, G. Zhou*, S. Jiang*.Total Synthesis and Biological Evaluation of Largazole and Derivatives with Promising Selectivity for Cancers Cells. Orgainc. Lett. 2010, 12, 1368-1371.

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, K. W. Worthy, R. J. Fisher, T. R. Burke, Jr., M. C. Nicklaus, P. P. 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, P. P. 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, P. P. 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, S. A. Kawamoto, W. Gao, H. Yi, D. Qin, P. P. 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.

49.    O. A. Timofeeva, V. Gaponenko, S. J. Lockett, S. G. Tarasov, S. Jiang, C. J. Michejda, A. O. Perantoni, N. I. Tarasova. Rationally designed inhibitors identify STAT3 N-domain as a promising anticancer drug target. ACS Chem Biol. 2007, 2, 799-809.

50.    S. Jiang, P. Li, S. L. Lee, C. Y. Lin, Y.Q Long, M. D. Johnson, R. B. Dickson, P. P. Roller. Design and Synthesis of redox stable analogues of Sunflower Trypsin inhibitors (SFTI-1) on solid support, potent inhibitors of Matriptase. Orgainc. Lett. 2007, 9, 9-12.

51.    H-X. Liu, G-R. Huang, H-M Zhang, S. Jiang, J.-R. Wu, Z. -J. Yao. A Structure-Activity Guided Strategy for Fluorescent Labeling of Annonaceous Acetogenin Mimetics and their Application in Cell Biology. ChemBioChem. 2007, 8, 172-177.

52.    P. Li, S. Jiang, S. L. Lee, C. Y. Lin, M. D. Johnson, C. J. Michejda, R. B. Dickson, P. P. 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.

53.    P. Li, S. Jiang, P. C. Stephanie, O. Lyn, D. N. Krag, P. P. Roller. Design and Synthesis of Water-Soluble Conjugates of Paclitaxel to Extracellular Doma in of ErbB2-Recognizing Peptide. Biopolymers. 2007, 87, 225-230.

54.    H. Sun, Z. Nikolovska-Coleska, J. Lu, J. Meagher, C. Yang, S. Qiu, Y. Tomita, Y. Ueda, S. Jiang, Krajewski, P. P. Roller, J. A. 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 Domains in XIAP. J. Am. Chem. Soc.  2007, 129, 15279-15294.

55.    G. Z. Tang, C. Y. Yang, Z. Nikolovska-Coleska, J. Guo, S. Qiu, R. X. Wang, W. Gao, G. P. Wang, J. Stuckey, K. Krajewski, S. Jiang, P. P. Roller, S. Wang. Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins. J. Med. Chem. 2007, 50, 1723-1726.

56.    G. Z. Tang, K. Ding, Z. Nikolovska-Coleska, C. Y. Yang, S. Qiu, S. Shangary, R. X. Wang, J. Guo, W. Gao, J. Meaghe, J. Stuckey, K. Krajewski, S. Jiang, P. P. Roller, S. Wang. Structure-Based Design of Flavonoid Compounds As a New Class of Small-Molecule Inhibitors of the Anti-apoptotic Bcl-2 Proteins. J. Med. Chem. 2007, 50, 3163-3166.

57.    J. Chen, Z. Nikolovska-Coleska, C. Y. 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, C. C. Lai, J.A. 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, R. J. Fisher, T. R. Burke, M. Nicklaus, P. P. 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, C. C. Lai, J. A. Kelley, P. P. Roller. A  Practical Synthesis of Fully Protected L-γ-Carboxyglutamic Acid (L-Gla). Tetrahedron. Lett. 2006, 47, 23-25.

61.    G. P. Wang, Z. Nikolovska-Coleska, C. Y. Yang, R. X. Wang, G. Z. Tang, J. Guo, S.   Shanggary, S. Qiu, W. Gao, D. J. Yang, J. Meagher, J. Stuckey, K. Krajewski, S. Jiang, P. P. Roller, H.O. Abbaan, Y. Tomita, S. Wang. Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. J. Med. Chem. 2006, 49, 6139-6142.

62.    Y. Zhao, S. Jiang, Y. W. 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, X. G. Chen, T. S. Hu, Y. L. Wu, Z.-J. Yao. Parallel fragment assembly strategy towards multiple-ether mimicry of anticancer annonaceous acetogenins. Angew. Chem. Int. Ed.  2004, 43, 329-334.

64.    G. R. Huang, S. Jiang, Y. L. Wu, Z. J. Yao, J.R. Wu. Induction of cell death of gastric cancer cells by a modified compound of the annonaceous acetogenin family. Chem BioChem 2003, 4, 1216-1221.

65.    B.B. Zeng, Y.K. Wu, S. Jiang, Q. Yu, Z.J. Yao, Z. Liu, H. Li, Y. Li, X. Chen, Y.L. Wu. Studies on Mimicry of Naturally occuring Annonaceous Acetogenins: Non-THF Analogues Leading to Remarkable Selective Cytotoxicity Against Human Tumor cells. Chem. Eur. J. 2003, 9, 282-290.

66.    S. Jiang, Y.L. Wu, Z.J. 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, Y.L. Wu, Z.J. Yao. First Synthesis of Mosquito larvicidal Butenolides I and II. Chinese J. Chem. 2002, 20, 692-696.

68.        S. Jiang, Z. Liu, G. Sheng, B. B. Zeng, X. G. Cheng, Y.L. Wu, Z.J. Yao. Mimicking of Annonaceous Acetogenins: Enantionselective Synthesis of a (4R)-Hydroxy Analog Having Potent Antitumor Activity. J. Org. Chem, 2002, 67, 3404-3408.