李學耘(Lee, Hsueh-Yun)　教授

Email
hyl@tmu.edu.tw
現   職
藥物科學學科 教授

學經歷

學　歷

畢業學校與學位[修業時間]
國立台灣大學藥學所 博士
2002/09~2010/01
臺北醫學大學藥學系 學士
1997/09~2001/06

本校學術經歷

任職單位與職稱[起迄時間]
藥物科學學科教授
2022/02/01~
藥物科學學科副教授
2018/02/01~2022/01/31
藥物科學學科助理教授
2015/08/01~2018/01/31
藥物科學學科專案助理教授
2013/02/01~2015/07/31
藥物科學學科助理研究員
2012/10/01~2013/01/31

本校兼職教學行政經歷

服務單位與職稱[起迄時間]
(舊)臨床藥物基因體學暨蛋白質體學碩士學位學程副教授
2020/04/01 ~
(舊)生技醫療產業研發博士學位學程助理教授
2016/09/01 ~ 2017/08/31

其它經歷

任職單位與職稱[起迄時間]
台北醫學大學博士後研究
2011/08/01~2012/09/30
國立清華大學博士後研究
2010/02/01~2011/07/31

專長與研究領域

學門領域
藥學
有機化學
學術專長
天然物化學
天然物化學
藥物化學
藥物化學
藥物設計
藥物設計
有機合成
organic synthesis
微波加速化學反應

論文著作

清冊下載

論文 Journal Paper


1. 2024 Lee, H. Y.,Hsu, M. J.,Chang, H. H.,Chang, W. C.,Huang, W. C.,Cho, E. C.. Enhancing anti-cancer capacity: Novel class I/II HDAC inhibitors modulate EMT, cell cycle, and apoptosis pathways. . Bioorg. Med. Chem. .2024 ;(109):117792

2. 2023 Chang, C. D.,Chao, M. W.,Lee, H. Y.,Liu, Y. T.,Tu, H. J.,Lien, S. T., Lin, T. E., Sung, T. Y., Yen, S. C., Huang, S. H., Hsu, K. C., Pan, S. L.. In silico identification and biological evaluation of a selective MAP4K4 inhibitor against pancreatic cancer . J. Enzyme Inhib. Med. Chem. .2023 ;(38):2166039

3. 2023 Peng, C. M.,Wang, S. W.,Hwang, Y. L.,Sun, W. C.,Chiu, L. P.,Liu, Y. T., Lai, Y. W., Lee, H. Y.. CuI-mediated synthesis of 1-aryl-5,6,7-trimethoxybenzimidazoles as potent antitubulin agents . RSC Adv. .2023 ;(13):13169-13176

4. 2023 Kumar, M.,Gaivin, R. J.,Khan, S.,Fedorov, Y.,Adams, D. J.,Zhao, W., Lee, H. Y., Dai, X., Dealwis, C. G., Schelling, J. R.*. Definition of fatty acid transport protein-2 (FATP2) structure facilitates identification of small molecule inhibitors for the treatment of diabetic complications . Int. J. Biol. Macromol. .2023 ;(244):125328

5. 2023 Narwanti, I.,Yu, Z. Y.,Sethy, B.,Lai, M. J.,Lee, H. Y.,Olena, P., Lee, S. B., Liou, J. P.. 6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers . Eur. J. Med. Chem. .2023 ;(258):115505

6. 2023 Lee, S.,Chao, M. W.,Wu, Y. W.,Hsu, C. M.,Lin, T. E.,Hsu, K. C., Pan, S. L., Lee, H. Y.*. Synthesis and evaluation of potent (iso)ellipticine-based inhibitors of MYLK4 accessed via expeditious synthesis from isoquinolin-5-ol. . RSC Adv. .2023 ;(13):31595-31601

7. 2022 Lee, H. Y.,Tang, D. W.,Liu, C. Y.,Cho, E. C.*. A novel HDAC1/2 inhibitor suppresses colorectal cancer through apoptosis induction and cell cycle regulation . Chem. Biol. Interact. .2022 ;(352):109778

8. 2021 Cho, E. C.,Liu, C. Y.,Tang, D. W.,Lee, H. Y.*. Ring size changes in the development of class I HDAC inhibitors . J. Enzyme Inhib. Med. Chem. .2021 ;(36):1387-1401

9. 2021 Lee, S.,Wang, S. W.,Yu, C. L.,Tai, H. C.,Yen, J. Y.,Tuan, Y. L., Wang, H. H., Liu, Y. T., Chen, S. S.*, Lee, H. Y.*. Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2 . Bioorg. Med. Chem. .2021 ;(50):116454

10. 2021 Lee, S. B.,Chang, T. Y.,Lee, N. Z.,Yu, Z. Y.,Liu, C. Y.,Lee, H. Y.*. Design, synthesis and biological evaluation of bisindole derivatives as anticancer agents against Tousled-like kinases . Eur. J. Med. Chem. .2021 ;(227):113904

11. 2021 Lin, T. E.,Sung, L. C.,Chao, M. W.,Li, M.,Zheng, J. H.,Sung T. Y., Hsieh, J. H., Yang, C. R., Lee, H. Y., Cho, E. C.*, Hsu, K. C.*. Structure-based virtual screening and biological evaluation of novel small-molecule BTK inhibitors . J. Enzyme Inhib. Med. Chem. .2021 ;(37):226-235

12. 2020 Wang, S. W.,Lin, M. H.,Hsu, F. C.,Chen, M. C.,Liou, J. P.,Liu, Y. T., Chen, S. S., Lee, H. Y.*. Synthesis and biological evaluation of 2-quinolineacrylamides . Bioorg. Med. Chem. .2020 ;(28):115250

13. 2020 Fang, Y. C.,Chan, L.,Liou, J. P.,Tu, Y. K.,Lai, M. J.,Chen, C. I., Vidyanti, A. N., Lee, H. Y.*, Hu, C. J.*. HDAC inhibitor protects chronic cerebral hypoperfusion and oxygen-glucose deprivation injuries via H3K14 and H4K5 acetylation-mediated BDNF expression . J. Cell. Mol. Med. .2020 ;(24):6966-6977

14. 2020 Mehndiratta, S.,Chen, M. C.,Chao,Y. H.,Lee, C. H.,Liou, J. P.,Lai, M. J.*, Lee, H. Y.*. Effect of 3-subsitution of quinolinehydroxamic acids on selectivity of histone deacetylase isoforms . J. Enzyme Inhib. Med. Chem. .2020 ;(36):74-84

15. 2020 Kaur, N.,Fang, Y. C.,Lee, H. Y.,Singh, A.,Nepali, K.,Lin, M. H., Yeh, T. K., Lai, M. J., Chan, L., Tu, Y. K., Banerjee, S., Hu, C. J.*, Liou, J. P.*. Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment . Eur. J. Med. Chem. .2020 ;(187):111915

16. 2019 Misko, T. A. ,Liu, Y. T.,Harris, M. E.,Oleinick, N. L.,Pink, J.,Lee, H. Y.*, Dealwis, C. G.*. Structure-guided design of anti-cancer ribonucleotide reductase inhibitors . J. Enzyme Inhib. Med. Chem. .2019 ;(34):438-450

17. 2019 Nepali, K.,Lee, H. Y.,Liou, J. P.*. Nitro-Group-Containing Drugs . J. Med. Chem. .2019 ;(6):2851-2893

18. 2019 Lai, M. J.,Ojha, R.,Lin, M. H.,Liu, Y. M.,Lee, H. Y.,Lin, T. E., Hsu, K. C., Chang, C. Y., Chen, M. C., Nepali, K., Chang, J. Y.*, Liou, J. P.*. 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase . Eur. J. Med. Chem. .2019 ;(162):612-630

19. 2018 Wu, Y. W.,Hsu, K. C.,Lee, H. Y.,Huang, T. C.,Lin, T. E.,Chen, Y. L.,Sung, T. Y., Liou, J. P., Hwang-Verslues, W. W., Pan, S. L., HuangFu, W. C.*. A novel dual HDAC6 and tubulin inhibitor, MPT0B451, displays anti-tumor ability in human cancer cells in vitro and in vivo . Front Pharmacol. .2018 ;(9):205

20. 2018 Lee, H. Y. ,Nepali, K. ,Huang, F. I.,Chang, C. Y. ,Lai, M. J. ,Li, Y. H., Huang, H.L., Yang, C. R.*, Liou, J. P.*. (N‑Hydroxycarbonylbenylamino)quinolines as selective histone deacetylase 6 inhibitors suppress growth of multiple myeloma in vitro and in vivo . J. Med. Chem. .2018 ;(61):905-917

21. 2018 Lee, H. Y.,Fan, S. J.,Huang, F. I.,Chao, H. Y.,Hsu, K. C.,Lin, T. E., Yeh, T. K., Lai, M. J., Li, Y. H., Huang, H. L., Yang, C. R.*, Liou, J. P.*. 5-Aroylindoles act as selective histone deacetylase 6 inhibitors ameliorating Alzheimer's disease phenotypes . J. Med. Chem. .2018 ;(61):7087-7102

22. 2017 Lee, H. Y.,Lee, J. F.,Kumar, S.,Wu, Y. W.; ,HuangFu, W. C.. 3-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity. . Eur. J. Med. Chem. .2017 ;(125):1268-1278

23. 2017 Nepali, K.,Lee, H. Y.,Lai, M. J.,Ojha, R.,Wu, T. Y.,Wu, G. X.; Chen, M. C.*; Liou, J. P.. Ring-opened tetrahydro-γ-carbolines display cytotoxicity and selectivity with histone deacetylase isoforms. . Eur. J. Med. Chem. .2017 ;(127):115-127

24. 2017 Kumar, S.,Lee, H. Y.,Liou, J. P.. Total Synthesis of Two Glycosylated Stilbenes, Oxyresveratrol 2-O-β- d -Glucopyranoside and 2,3,5,4′-Tetrahydroxystilbene 2-O-β- d -Glucopyranoside . Journal of Natural Products .2017 ;(80):1294-1301

25. 2017 Kumar, S.,Lee, H. Y.,Liou, J. P.. Total synthesis of two glycosylated stilbenes, oxyresveratrol 2-O-β-D-glucopyranoside and 2,3,5,4’-tetrahydroxystilbene 2-O-β-D-glucopyranoside . J. Nat. Prod. .2017 ;(80):1294-1301

26. 2016 Lee, H. Y.,Kumar, S.,Lin, T. C.,Liou, J. P.. Total synthesis of denbinobin . J. Nat. Prod. .2016 ;(79):1170-1173

27. 2016 Lee, H. Y.,Chang, C. Y.,Su, C. J.,Huang, H. L.,Mehndiratta, S.,Chao, Y. H.; Hsu, C. M.; Kumar, S.; Sung, T. Y.; Huang, Y. Z.; Li, Y. H.; Yang, C. R.*; Liou, J. P.. 2-(Phenylsulfonyl)quinoline N-hydroxyacrylamides as potent anticancer agents inhibiting histone deacetylase. . Eur. J. Med. Chem. .2016 ;(122):92-101

28. 2015 Lee HY,Chang CY,Lai MJ,Chuang HY,Kuo CC,Chang CY, Chang JY, Liou JP. Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes. . Bioorg. Med. Chem. .2015 ;(23):4230-4236

29. 2015 Lai MJ,Lee HY,Chuang HY.,Chang LH,Tsai AC,Chen MC, Huang HL, Wu YW, Teng CM, Pan SL, Liu YM, Mehndiratta S, Liou JP. N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling. . J. Med. Chem. .2015 ;(58):6549-6558

30. 2015 Liu YM,Lee HY,Lai MJ,Pan SL,Huang HL,Kuo FC, Chen MC*, Liou JP*. Pyrimidinedione-mediated selective histone deacetylase 6 inhibitors with antitumor activity in colorectal cancer HCT116 cells . Org. Biomol. Chem. .2015 ;(13):10226-10235

31. 2015 Nepali K,Kumar S,Huang HL,Kuo FC,Lee CH,Kuo CC, Yeh TK, Li YH, Chang JY, Liou JP and Lee HY*. 2-Aroylquinoline-5,8-diones as potent anticancer agents displaying tubulin and heat shock protein 90 (HSP90) inhibition . Org. Biomol. Chem. .2015

32. 2015 Nepali K,Kumar S,Huang HL,Kuo FC,Lee CH,Kuo CC2, Yeh TK, Li YH, Chang JY, Liou JP, Lee HY*. 2-Aroylquinoline-5,8-diones as potent anticancer agents displaying tubulin and heat shock protein 90 (HSP90) inhibition. . Org. Biomol. Chem. .2015 ;(14):716-723

33. 2015 Liu, Y. M.,Lee, H. Y.,Chen, C. H.,Lee, C. H.,Wang, L. T.,Pan, S. L., Lai, M. J., Yeh, T. K., Liou, J. P.. 1-Arylsulfonyl-5-(N-hydroxyacrylamide)tetrahydroquinolines as potent histone deacetylase inhibitors suppressing the growth of prostate cancer cells. . Eur. J. Med. Chem. .2015 ;(89):320-330

34. 2015 Yang, C. R.,Shih, K. S.,Liou, J. P.,Wu, Y. W.,Hsieh, I. N.,Lee, H. Y., Lin, T. C., Wang, J. H.. Denbinobin upregulates miR-146a expression and attenuates IL-1β-induced upregulation of ICAM-1 and VCAM-1 expressions in osteoarthritis fibroblast-like synoviocytes. . J. Mol. Med. (Berl). .2015

35. 2015 Mehndiratta, S.,Chiang, Y. F.,Lai, M. J.,Lee, H. Y.,Chen, M. C.,Kuo, C. C., Chang, C. Y., Chang, J. Y., Liou, J. P.. Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents. . Bioorg. Med. Chem. .2015 ;(22):4917-4923

36. 2015 Mehndiratta, S.,Hsieh, Y. L.,Liu, Y. M.,Wang, A. W.,Lee, H. Y.,Liang, L. Y., Kumar, S., Teng, C. M., Yang, C. R., Liou, J. P.. Indole-3-ethylsulfamoylphenylacrylamides: potent histone deacetylase inhibitors with anti-inflammatory activity. . Eur. J. Med. Chem. .2015 ;(85):468-479

37. 2014 Lee HY,Tsai AC,Chen MC,Shen PJ,Cheng YC,Kuo CC, Pan SL, Liu YM, Liu JF, Yeh TK, Wang JC, Chang CY, Chang JY, Liou JP. Azaindolylsulfonamides, with a More Selective Inhibitory Effect on Histone Deacetylase 6 Activity, Exhibit Antitumor Activity in Colorectal Cancer HCT116 Cells . Journal of Medicinal Chemistry .2014 ;(57):4009-4022

38. 2014 Chang CY,Chuang HY,Lee HY,Yeh TK,Kuo CC,Chang CY, Chang JY, Liou JP. Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones . European Journal of Medicinal Chemistry .2014 ;(77):306-314

39. 2014 Liu YM,Chen HL,Lee HY,Liou JP. Tubulin inhibitors: a patent review . Expert Opinion on Therapeutic Patents .2014 ;(24):69-88

40. 2014 Hsieh IN,Liou JP,Lee HY,Lai MJ,Li YH,Yang CR. Preclinical anti-arthritic study and pharmacokinetic properties of a potent histone deacetylase inhibitor MPT0G009 . Cell Death & Disease .2014 ;(5):e1166

41. 2014 Wang, C. Y.,Liou, J. P,Tsai, A. C,Lai, M. J.,Liu, Y. M.,Lee, H. Y., Wang, J. C., Pan, S. L., Teng, C. M.. A novel action mechanism for MPT0G013, a derivative of arylsulfonamide, inhibits tumor angiogenesis through up-regulation of TIMP3 expression. . Oncotarget .2014 ;(5):9838-9850

42. 2014 Lee, H. Y.,Wang, L. T.,Li, Y. H.,Pan, S. L.,Chen, Y. L,Teng, C. M., Liou, J. P.. Effect of C7-substitution of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indolines on the selectivity towards a subclass of histone deacetylases. . Org. Biomol. Chem. .2014 ;(12):8966-8976

43. 2013 Lee HY,Pan SL,Su MC,Liu YM,Kuo CC,Chang YT, Wu JS, Nien CY, Mehndiratta S, Chang CY, Wu SY, Lai MJ, Chang JY*, Liou JP*. Furanylazaindoles: Potent Anticancer Agents in Vitro and in Vivo . Journal of Medicinal Chemistry .2013 ;(53):8008-8018

44. 2013 Lee HY,Yang CR,Lai MJ,Huang HL,Hsieh YL,Liu YM, Yeh TK. Li YH, Mehndiratta S, Teng CM, Liou JP*. 1-Arylsulfonyl-5-(N-hydroxyacrylamide)indolines Histone Deacetylase Inhibitors Are Potent Cytokine Release Suppressors . CHEMBIOCHEM .2013 ;(14):1248-1254

45. 2012 Lai, M. J.,Huang, H. L.,Pan, S. L.,Liu, Y. M.,Peng, C. Y.,Lee, H. Y., Yeh, T. K., Hung, P. H., Teng, C. M., Chen, S. H., Chuang, H. Y., Liou, J. P.. Synthesis and Biological Evaluation of 1-Arylsulfonyl-5-(N-hydroxyacrylamide) indoles as Potent Histone Deacetylase Inhibitors with Antitumor Activity in vivo. . J. Med. Chem. .2012 ;(55):3777-3791

46. 2012 Lee, H. Y.,Lee, L. W.,Nien, C. Y.,Kuo, C. C.,Lin, P. Y.,Chang, C. Y., Chang, J. Y., Liou, J. P.. Application of Suzuki arylation, Sonogashira ethynylation and Rosenmund-von Braun cyanation in the exploration of substitution effects on the anticancer activity of 2-aroylquinolines. . Org. Biomol. Chem .2012 ;(10):9593-9600

47. 2012 Huang, H. L,Lee, H. Y.,Tsai, A. C.,Peng, C. Y.,Lai, M. J.,Wang, J. C., Pan, S. L., Teng, C. M., Liou, J. P.. Anticancer Activity of MPT0E028, a Novel Potent Histone Deacetylase Inhibitor, in Human Colorectal Cancer HCT116 Cells In Vitro and In Vivo. . PLoS ONE .2012 ;(8):e43645-e43645

48. 2011 Chuang, H. Y.,Chang, J. Y.,Lai, M. J.,Kuo, C. C.,Lee, H. Y.,Hsieh, H. P., Chen, Y. J., Chen, L. T., Pan, W. Y., Liou, J. P.. 2-Amino-3,4,5-Trimethoxybenzophenones as Potent Tubulin Polymerization Inhibitors. . ChemMedChem .2011 ;(6):450-456

49. 2011 Lee, H. Y.,Chang, J. Y.,Chang, L. Y.,Lai, W. Y.,Lai, M. J.,Shih, K. H., Kuo, C. C., Hsieh, H. P., Chang, C. Y., Liou, J. P.. Concise syntheses of N-aryl-5,6,7-trimethoxyindoles as antimitotic and vascular disrupting agents: application of the copper-mediated Ullmann-type arylation. . Org. Biomol. Chem. .2011 ;(9):3154-3157

50. 2011 Hsieh, C. C.,Lee, H. Y.,Nien, C. Y.,Kuo, C. C.,Chang, C. Y.,Chang, J. Y., Liou, J. P.. Synthesis and Biological Evaluation of 4-Aroyl-6,7,8-Trimethoxyquinolines as a Novel Class of Anticancer Agents . Molecules .2011 ;(16):2274-2284

51. 2011 Lai, M. J.,Chang, J. Y.,Lee, H. Y.,Kuo, C. C.,Lin, M. H.,Hsieh, H. P., Chang, C. Y., Wu, J. S., Wu, S. Y., Shey, K. S., Liou, J. P.. Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents. . Eur. J. Med. Chem. .2011 ;(46):3623-3629

52. 2011 Lee HY,Chang JY,Nien CY,Kuo CC,Shih KH,Wu CH, Chang CY, Lai WY, Liou JP*. 5-Amino-2-aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors. Part 2. The Impact of Bridging Groups at Position C-2 . Journal of Medicinal Chemistry .2011 ;(54):8517-8525

53. 2010 Lee, H. Y.,Chen, G. S.,Chen, C. S.,Chern, J. W.. Efficient microwave-assisted synthesis of ellipticine through N-(1,4-dimethyl-9H-carbazol-3-ylmethyl)-N-tosylaminoacetaldehyde diethyl acetal. . J. Heterocyclic Chem. .2010 ;(47):454-458

54. 2009 Chang, P. T.,Kung, F. L.,Talekar, R. S.,Chen, C. S.,Lai, S. Y.,Lee, H. Y., Chern, J. W.. An improved screening model to identify inhibitors targeting zinc-enhanced amyloid aggregation. . Anal. Chem. .2009 ;(81):6944-6951

會議論文 Conference Paper


1. 2016 Lee HY. Development of Bioactive 1,4-Benzoquinone-Containing Derivatives . .2016

2. 2016 Chang HH,Lee HY. 2-(Phenylsulfonyl)quinoline N-Hydroxyacrylamides as Potent Anticancer Agents Inhibiting Histone Deacetylase . .2016

3. 2016 Nepali K,Huang HL,Kuo FC,Lee CH,Kuo CC,Li YH, Chang JY, Liou JP, Lee HY. 2-Aroylquinoline-5,8-diones as Potent Anticancer Agents Displaying Tubulin and Heat Shock Protein 90 (HSP90) Inhibition . .2016

研究計畫

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113 貴機構延攬印度籍DEEPA LANDGE 蒂朴蘭格君參與「優化與開發紡錘體檢查點抑制劑用於治療三陰性乳癌」研究計畫案
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113 優化與開發紡錘體檢查點抑制劑用於治療三陰性乳癌(1/3)
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112 新穎藥物合成研究計畫
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111 開發高選擇性PLK2抑制劑並探討其對大腸直腸癌之功效與機轉
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111 112年度(第61屆)國外短期研究案-於淋巴結轉移之腫瘤免疫逃脫中啟動表觀遺傳調節刺激
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111 112年度(第61屆)國外短期研究案-開發組蛋白離胺酸甲基轉移酶抑制劑作為抗癌分子
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111 開發具胰臟癌抑制活性之激酶抑制劑
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110 開發1,3-二芳基取代之五元雜環作為抗胰臟癌劑(3/3)
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科技部
計畫名稱
110 藥學系（所）李學耘副教授申請補助延攬科技人才印度籍Sundaramoorthi Sarathkumar 薩拉特君參與「開發1,3-二芳基取代之五元雜環作為抗胰臟癌劑」研究計畫案，業經核定以「博士級研究人員」資格補助(MOST 110-2811-B-038-518)，補助項目為研究費、年終獎金、離職儲金、保險費等，請查照
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109 開發1,3-二芳基取代之五元雜環作為抗胰臟癌劑(2/3)
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108 開發1,3-二芳基取代之五元雜環作為抗胰臟癌劑(1/3)
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108 協助於 本（108）年8月30日舉辦「台日六校聯合國際研討會」會 議經費事
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107 設計與合成benzimidazole衍生物作為改善神經退化疾病之化合物
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104 設計與合成芳醯基雜環之抗癌化合物
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104 新聘教師研究補助
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臺北醫學大學