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成果及论文

55. Liang, X.; Liu, H.*; Zhang, Y.* Novel-targeted therapy for hematological malignancies with JAK and HDAC dual inhibitors. Future Med. Chem. 2019, 11 (15), 1849-1852. (Invited Editorial)

54. Liang, X.; Zang, J.; Li, X.; Tang, S.; Huang, M.; Geng, M.; Chou, C. J.; Li, C.; Cao, Y.; Xu, W.; Liu, H.*; Zhang, Y.* Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies. J. Med. Chem. 2019, 62 (8), 3898-3923. (Cover Paper, F1000Prime recommended)

53. Cao, J.; Zang, J.; Kong, X.; Zhao, C.; Chen, T.; Ran, Y.; Dong, H.; Xu, W.; Zhang, Y.* Leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry. Part II. Bioorg. Med. Chem. 2019, 27 (6), 978-990.

52. Dong, H.; Yin, H.; Zhao, C.; Cao, J.; Xu, W. Zhang, Y.* Design, Synthesis and Biological Evaluation of Novel Osimertinib-Based HDAC and EGFR Dual Inhibitors. Molecules 2019, 24, 2407.

51. Zang, J.; Liang, X.; Huang, Y.; Jia, Y.; Li, X.; Xu, W.; Chou, C. J.; Zhang, Y.* Discovery of Novel Pazopanib-based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously. J. Med. Chem. 2018, 61 (12), 5304-5322.

50. Cao, J.; Ma, C.; Zang, J.; Gao, S.; Gao, Q.; Kong, X.; Yan, Y.; Liang, X.; Ding, Q.; Zhao, C.; Wang, B.; Xu, W.*; Zhang, Y.* Novel leucine ureido derivatives as aminopeptidase N inhibitors using click chemistry. Bioorg. Med. Chem. 2018, 26 (12), 3145-3157.

49. Zhao, C.; Zang, J.; Ding, Q.; Inks, E. S.; Xu, W.; Chou, C. J.; Zhang, Y.* Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors. Eur. J. Med. Chem. 2018, 150, 282-291.

48. Jiang, Y.; Li. X.; Hou, J.; Huang, Y.; Wang, X.; Jia, Y.; Wang, Q.; Xu, W.; Zhang, J.*; Zhang, Y.* Synthesis and biological characterization of ubenimex-fluorouracil conjugates for anti-cancer therapy. Eur. J. Med. Chem. 2018, 143, 334-347.

47. Cao, J.; Zang, J.; Ma, C.; Li, X.; Hou, J.; Li, J.; Huang, Y.; Xu, W.*; Wang, B.; Zhang, Y.* Design, synthesis and biological evaluation of new pyrazoline-based hydroxamic acid derivatives as aminopeptidase N (APN) inhibitors. ChemMedChem. 2018, 13 (5), 431-436.

46. Gao, Q.; Liang, X.; Shaikh, A. S.; Zang, J.; Xu, W.*; Zhang, Y.* JAK/STAT signal transduction: Promising attractive targets for immune, inflammatory and hematopoietic diseases. Curr. Drug Targets 2018, 19 (5), 487-500.

45. Chen, F.; Liu, C.; Zhang, J.; Xu, W.*; Zhang, Y.* Progress of CDK4/6 inhibitor palbociclib in the treatment of cancer. Anti-Cancer Agent. ME. 2018, 18 (9), 1241-1251.

44. Zhang, Y.*; Yan, J.; Yao, T-P.* Discovery of a fluorescent probe with HDAC6 selective inhibition. Eur. J. Med. Chem. 2017, 141, 596-602.

43. Zhou, N.;# Yan, Y.;# Liu, C.; Hou, J.; Xu, W.; Zhang, Y.* Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability. Bioorg. Med. Chem. 2017, 25 (17), 4614-4619.

42. Li, X.;# Zhang, Y.#*; Jiang, Y.; Wu, J.; Inks, E. S.; Chou, C. J.; Gao, S.; Hou, J.; Ding, Q.; Li, J.; Wang, X.; Huang, Y.; Xu, W. Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study. Eur. J. Med. Chem. 2017, 134, 185-206.

41. Gao, S.; Zang, J.; Gao, Q.; Liang, X.; Ding, Q.; Li, X.; Xu, W.; Chou, C. J.; Zhang, Y.* Design, synthesis and anti-tumor activity study of novel histone deacetylase inhibitors containing isatin-based caps and o-phenylenediamine-based zinc binding groups. Bioorg. Med. Chem. 2017, 25 (12), 2981-2994.

40. Zang, J.; Shi, B. Liang, X.; Gao, Q.; Xu, W.*; Zhang, Y.* Development of N-hydroxycinnamamide-based HDAC inhibitors with improved HDAC inhibitory activity and in vitro antitumor activity. Bioorg. Med. Chem. 2017, 25 (9), 2666-2675.

39. Yan, Y.; Chen, X.; Yang, X.; Xu, W.*; Zhang, Y.* Sulfoxide Analogs of TAK-875 as GPR40 Agonists: Synthesis, Determination of Absolute Configuration and Biological Activity. Chin. J. Org. Chem. 2017, 37 (4), 858-865. (Cover Paper)

38. Gao, S.; Li, X.; Zang, J.; Xu, W.*; Zhang, Y.* Preclinical and clinical studies of chidamide (CS055/HBI-8000), an orally available subtype-selective HDAC inhibitor for cancer therapy. Anti-Cancer Agent. ME. 2017, 17 (6), 802-812.

37. Jiang, Y.; Hou, J.; Li. X.; Huang, Y.; Wang, X.; Wu, J.; Zhang, J.; Xu, W.; Zhang, Y.* Discovery of a novel chimeric ubenimex-gemcitabine with potent oral antitumor activity. Bioorg. Med. Chem. 2016, 24 (22), 5787-5795.

36. Ding, Q.; Zang, J.; Gao, S.; Gao, Q.; Duan, W.; Li, X.; Xu, W.*; Zhang, Y.* Nitric oxide donor hybrid compounds as promising anticancer agents. Drug Discov. Ther. 2016, 10 (6), 276-284.

35. Liang, X.; Zang, J.; Zhu, M.; Gao, Q.; Wang, B.*; Xu, W.; Zhang, Y.* Design, Synthesis, and Antitumor Evaluation of 4Amino-2 (1H)pyrazole Derivatives as JAKs Inhibitors. ACS Med. Chem. Lett. 2016, 7 (10), 950-955.

34. Li, J.; Li, X.; Wang, X.; Hou, J.; Zang, J.; Gao, S.; Xu, W.; Zhang, Y.* PXD101 analogs with L-phenylglycine-containing branched cap as histone deacetylase inhibitors. Chem. Biol. Drug Des. 2016, 88 (4), 574-584.

33. Jiang, Y.; Hou, J.; Li. X.; Xu, W.*; Zhang, Y.* Design, Synthesis and Biological Evaluation of Novel Tamibarotene Derivative as Multitarget Anticancer Agent. Lett. Drug Des. Discov. 2016, 13 (8), 729-733.

32. Jiang, Y.; Li. X.; Hou, J.; Huang, Y.; Jia, Y.; Zou, M.; Zhang, J.; Wang, X.*; Xu, W.*; Zhang, Y.* Discovery of BC-01, a novel mutual prodrug (hybrid drug) of ubenimex and fluorouracil as anticancer agent. Eur. J. Med. Chem. 2016, 121, 649-657.

31. Liang, X.; Huang, Y.; Zang, J.; Gao, Q.; Wang, B.*; Xu, W.; Zhang, Y.* Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors. Bioorg. Med. Chem. 2016, 24 (12), 2660-2672.

30. Jiang, Y.; Li. X.; Li, X.; Hou, J.; Ding, Y.; Zhang, J.; Xu, W.*; Zhang, Y.* Discovery of Multi-target Anticancer Agents Based on HDAC Inhibitor MS-275 and 5-FU. Med. Chem. 2016, 12 (1), 30-36.

29. Ma, C.; Cao, J.; Liang, X.; Huang, Y.; Wu, P.; Li, Y.; Xu, W.; Zhang, Y.* Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation. Eur. J. Med. Chem. 2016, 108, 21-27.

28. Zhang, Y.*; Li, X.; Hou, J.; Huang, Y.; Xu, W.* Design, synthesis, and antitumor evaluation of histone deacetylase inhibitors with L-phenylglycine scaffold. Drug Des. Dev. Ther. 2015, 9, 5553-5567.

27. Yan, Y.; Chen, X.; Yang, X.; Zhang, J.; Xu, W.*; Zhang, Y.* Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase. Bioorg. Med. Chem. 2015, 23 (20), 6632-6640.

26. Li, X.; Wu, J.; Li, X.; Mu, W.; Liu, X.; Jin, Y.; Xu, W.; Zhang, Y.* Development of N-hydroxybenzamide derivatives with indole containing cap group as histone deacetylases inhibitors. Bioorg. Med. Chem. 2015, 23 (19), 6258-6270.

25. Shi, F.; Zhang, Y.*; Xu, W.* Discovery of a series of novel compounds with moderate anti-hepatitis C virus NS3 protease activity in vitro. Bioorg. Med. Chem. 2015, 23 (17), 5539-5545.

24. Duan, W.; Hou, J.; Chu, X.; Li, X.; Zhang, J.; Li, J.; Xu, W.; Zhang, Y.* Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity. Bioorg. Med. Chem. 2015, 23 (15), 4481-4488.

23. Zhou, N.; Xu, W.*; Zhang, Y.* Histone deacetylase inhibitors merged with protein tyrosine kinase inhibitors. Drug Discov. Ther. 2015, 9 (3), 147-155.

22. Duan, W.; Li, J.; Inks, E. S.; Chou, C. J.; Jia, Y.; Chu, X.; Li, X.; Xu, W.*; Zhang, Y.* Design, Synthesis and Antitumor Evaluation of Novel Histone Deacetylase (HDAC) Inhibitors Equipped with Phenylsulfonylfuroxan Module as Nitric Oxide (NO) Donor. J. Med. Chem. 2015, 58 (10), 4325-4338.

21. Li, J.; Wang, X.; Hou, J.; Huang, Y.; Zhang, Y.*; Xu, W.* Enhanced anticancer activity of 5-FU in combination with Bestatin: Evidence in human tumor-derived cell lines and an H22 tumor-bearing mouse. Drug Discov. Ther. 2015, 9 (1), 45-52.

20. Zhang, Y.*; Xu, W. Isoform-selective histone deacetylase inhibitors: the trend and promise of disease treatment. Epigenomics 2015, 7 (1), 5-7. (Invited Editorial)

19. Li, X.; Hou, J.; Li, X.; Jiang, Y.; Liu, X.; Mu, W.; Jin, Y.; Zhang, Y.*; Xu, W.* Development of 3-hydroxycinnamamide-based HDAC inhibitors with potent in vitro and in vivo anti-tumor activity. Eur. J. Med. Chem. 2015, 89, 628-637.

18. Xie, Y.; Xu, D.; Huang, B.; Ma, X.; Qi, W.; Shi, F.; Liu, X.*; Zhang, Y.*; Xu, W.* Discovery of N-substituted Oseltamivir Derivatives as Potent and Selective Inhibitors of H5N1 Influenza Neuraminidase. J. Med. Chem. 2014, 57 (20), 8445-8458.

17. Li, X.; Inks, E. S.; Li, X.; Hou, J.; Chou, C. J.; Zhang, J.; Jiang, Y.; Zhang, Y.*; Xu, W.* Discovery of the First N-hydroxycinnamamide-based Histone Deacetylase 1/3 Dual Inhibitors with Potent Oral Antitumor Activity. J. Med. Chem. 2014, 57 (8), 3324-3341. (SciBX special report, Global Medical Discovery special report)

16. Yang, H.; Xu, W.; Li, Y.; Lan, P.; Zhang, J.; Zhang, Y.*; Zhang, C.* Superior activity of a new histone deacetylase inhibitor (ZYJ-34c) in inhibiting growth of human leukemia cells by induction p21WAF1 expression and cell cycle arrest. Anti-Cancer Drugs 2014, 25 (7), 767-777.

15. Li, X.; Zhang, J.; Xie, Y.; Jiang, Y.; Zhang, Y.*; Xu, W.* Progress of HDAC inhibitor panobinostat in the treatment of cancer. Curr. Drug Targets 2014, 15 (6), 622-634.

14. Xu, F.; Xu, H.; Wang, X.; Zhang, L.; Wen, Q.; Zhang, Y.*; Xu, W.* Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl) -sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III. Bioorg. Med. Chem. 2014, 22 (4), 1487-1495.

13. Liang, X.; Xu, F.; Ma, C.; Zhang, Y.*; Xu, W.* VEGF signal system: the application of antiangiogenesis. Curr. Med. Chem. 2014, 21 (7), 894-910.

12. Xu, F.; Zhang, L.; Jia, Y.; Wang, X.; Li, X.; Wen, Q.; Zhang, Y.*; Xu, W.* Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part II. Eur. J. Med. Chem. 2013, 69, 191-200.

11. Zhang, Y.; Yang, P.; Chou, C. J.; Liu, C.; Wang, X.; Xu, W.* Development of N-Hydroxycinnamamide-Based Histone Deacetylase Inhibitors with an Indole-Containing Cap Group. ACS Med. Chem. Lett. 2013, 4 (2), 235-238.

10. Zhang, Y.; Inks, E. S.; Zhu, M.; Chou, C. J.; Fang, H.; Li, M.; Shen, Y.; Yi, F.; Xu, W.* Discovery of a pair of diastereomers as potent HDACs inhibitors: determination of absolute configuration, biological activity comparison and computational study. RSC Adv. 2013, 3 (43), 21106-21109.

9. Zhang, Y.; Liu, C.; Chou, C. J.; Wang, X.; Jia, Y.; Xu, W.* Design and synthesis of a tetrahydroisoquinoline-based hydroxamate derivative (ZYJ-34v), an oral active histone deacetylase inhibitor with potent antitumor activity. Chem. Biol. Drug Des. 2013, 82 (2), 125-130. (Cover Paper)

8. Zhang, Y.; Fang, H.; Feng, J.; Jia, Y.; Wang, X.; Xu, W.* Discovery of a Tetrahydroisoquinoline-Based Hydroxamic Acid Derivative (ZYJ-34c) as Histone Deacetylase Inhibitor with Potent Oral Antitumor Activities. J. Med. Chem. 2011, 54 (15), 5532-5539.

7. Zhang, Y.; Feng, J.; Jia, Y.; Wang, X.; Zhang, L.; Liu, C.; Fang, H.; Xu, W.* Development of Tetrahydroisoquinoline-based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in vitro and in vivo Antitumor Activities. J. Med. Chem. 2011, 54 (8), 2823-2838.

6. Zhang, Y.; Feng, J.; Jia, Y.; Xu, Y.; Liu, C.; Fang, H.; Xu, W.* Design, synthesis and primary activity assay of tripeptidomimetics as histone deacetylase inhibitors with linear linker and branched cap group. Eur. J. Med. Chem. 2011, 46 (11), 5387-5397.

5. Zhang, Y.; Feng, J.; Liu, C.; Fang, H.; Xu, W.* Design, synthesis and biological evaluation of tyrosine-based hydroxamic acid analogs as novel histone deacetylases (HDACs) inhibitors. Bioorg. Med. Chem. 2011, 19 (15), 4437-4444.

4. Zhang, Y.; Fang, H.; Xu, W.* Applications and modifications of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) in peptides and peptidomimetics design and discovery. Curr. Protein Pept. Sci. 2010, 11 (8), 752-758.

3. Zhang, Y.; Feng, J.; Liu, C.; Zhang, L.; Jiao, J.; Fang, H.; Su, L.; Zhang, X.; Zhang, J.; Li, M.; Wang, B.; Xu, W.* Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors. Bioorg. Med. Chem. 2010, 18 (5), 1761-1772.

2. Zhang, Y.; Fang, H.; Jiao, J.; Xu, W.* The Structure and Function of Histone Deacetylases: The Target for Anti-cancer Therapy. Curr. Med. Chem. 2008, 15 (27), 2840-2849.

1. Zhang, Y.; Xu, W.* Progress on Kinesin Spindle Protein Inhibitors as Anti-Cancer Agents. Anti-Cancer Agent. ME. 2008, 8 (6), 698-704.