Qian Shi, PhD

Qian Shi, PhD
  • Research Associate Professor
Contact Info

Chemical Biology and Medicinal Chemistry

qshi1@email.unc.edu

Work: (919) 843-6325
Fax: 919-966-3893

Eshelman School of Pharmacy, , 310 Beard Hall,
Campus Box Campus Box 7568
Chapel Hill NC 27599-7568

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Qian Shi, PhD

RESEARCH SYNOPSIS

Dr. Shi’s research mainly focuses on design, synthesis, biological evaluation, SAR and mechanistic studies of novel bioactive compounds, especially anticancer effective agents. 1) Mechanism of action guided design and synthesis of curcumin derivatives as potent prostate cancer / colon cancer therapeutic and/or preventive agents (by enhancing AR degradation and/or inhibiting PKC or/and EGFR-T/NF-kB signalings).  2) Phenanthroindolizidines and phenanthroquinolizidines series, such as antofine and cryptopleurine analogs as potent anti-lung cancer and/or colon cancer agents.  3) Podophyllotoxin derivatives, such as water soluble prodrugs as topoisomerases II or I inhibitors. 4) Colchicine and thiocolchicine analogs as potent antimitotic antitumor agents through inhibition of tubulin polymerization. 5) Neo-tenshinlactone derivatives as anti-breast cancer agents. In addition, her research also involves discovery of other natural products derived bioactive agents such as taxoid analogs, cuomarine derivatives, etc. as antitumor and anti-HIV agents.  Besides her broad experience and expertise in the field of drug discovery, Dr. Shi is also well knowledgeable and experienced in operation and interpretation of analytical instrumentations and acquired data such as LC/MS/MS, HPLC, FT-IR, NMR(1D/2D), which further implement her drug discovery and development research.

 

SELECT PUBLICATIONS (from 50 publications and patents; * denotes corresponding author ):

  1. Yang, X; Shi*, Q; Yang, S.C; Chen, C.Y; Yu, S. L; Bastow, K. F.; Morris-Natschke, S.L.; Wu, P.C; Lai, C.Y; Wu, T.S . Lee*, K.H. Antitumor Agents 288: Design, Synthesis, SAR, and Biological Studies of Novel Heteroatom-Incorporated Antofine and Cryptopleurine Analogues as Potent and Selective Antitumor Agents. J. Med. Chem., 2011,  54(14), 5097-5107.  
  2. Zhou, T; Shi, Q; Bastow, K.F.; Lee*, K.H. Antitumor agents 286. Design, synthesis, and structure-activity relationships of 3'R,4'R-disubstituted-2',2'-dimethyldihydropyrano[2,3-f]chromone (DSP) analogues as potent chemosensitizers to overcome multidrug resistance. J. Med. Chem., 2010, 53(24), 8700-8708. 
  3. Dong, Y; Shi, Q; Nakagawa-Goto, K.; Yu, D.; Liu, Y.N.; Wu, P.C.; Bastow, K.F.; Morris-Natschke, S. L.; Brossi, A.; Pai, H.C., Peng, C.Y.; Pan, S.L., Teng, C.M.; M.C. Hung,  Lee, E.Y.-H.P. and Lee*, K.H.  Antitumor Agents 272. Structure–Activity Relationships and In Vivo Selective Anti-Breast Cancer Aactivity of Novel Neo-tanshinlactone Analogs, J. Med. Chem. 2010, 53, 2299-2308.
  4. Yang, X.; Shi*, Q.; Bastow, K.F.; Lee, K.H. “Antitumor Agents 274. A Novel Synthetic Strategy for E-Ring SAR study of Antofine and Cryptopleurine Analogs,” Organic. Lett., 2010, 12, 1416-1419.
  5. Kozaka,T.; Nakagawa-Goto, K.; Shi,Q.; . Lai, C.Y.; Hamel, E.K.; Bastow, F.;  Brossi, A.; Lee*, K.H. Antitumor Agents 273. Design and Synthesis of N-Alkyl-thiocolchicinoids as Potential Antitumor Agents. Bioorg. Med. Chem. Lett., 2010, 20, 4091-4094.
  6. Zhou, T., Shi*, Q.; Lee*, K.H. Anti-AIDS Agents 83. Efficient Microwave-assisted One-pot preparation of Angular 2,2-Dimethyl-2H-Chromone Containing Compounds.  Tetrahedron Lett., 2010, 51, 4382-.4386
  7. Dong, Y.; Shi*, Q.; Nakagawa-Goto, K.; Wu, P.C.; Morris-Natschke, S.L.; Brossi, A.; Bastow, K.F.; Lee*, K.H. Antitumor Agents 270.  Novel Substituted 6-Phenyl-4H-Furo[3,2-c]Pyran-4-One Derivatives as Potent and Highly Selective Anti-Breast Cancer Agents.  Bioorg. Med. Chem., 2010, 18, 803-808.
  8. Shi, Q.; Shih, C.Y.; Lee*, K.H. “Antitumor Agents 265. Novel Anti-Prostate Cancer Curcumin Analogs that Enhance Androgen Receptor Degradation Activity,” Anticancer Agents in Medchem. 2009, 9, 904-912.
  9. Dong,Y.; Shi*, Q.; Bastow, K. F.; Lee*, K. H.  Anti-tumor Agents 266.  Design, Synthesis and Biological Evaluation of Novel 2-(Furan-2-yl)Naphthalene-1-ol Derivatives As Potent and Selective Anti-Breast Cancer Agents.  J. Med. Chem.  2009, 52(11), 3586-3590.
  10. Yang, X.; Shi*, Q.; Liu, Y.N.; Bastow, K.F.; Lin, J.C.; Yang, S. C.; Yang, P.C.; Lee*, K.H.   Anti-tumor Agents 268.  Design, Synthesis and Mechanistic Study of New 9-Substituted Phenanthrene-Based Tylophorine Analogs as Potent Antitumor agents. J. Med. Chem.  2009, 52(16), 5262-5268.
  11. Itokawa, H.; Shi, Q.; Akiyama, T.; Morris-Natschke, S.L.; Lee, K.H.  Recent Advance in the Investigation of Curcuminoids.  Chinese Medicine.  2008, 3, 1-13.
  12. Wei, L.; Shi, Q.; Bastow, K.F.; Brossi, A.; Morris-Natschke, S.L.; Wu,T.S.; Lee*, K.H.  Anti-tumor Agents 253.  Design, Synthesis, and Cytotoxic Evaluation of Novel 9-Substituted Phenanthrene-Based Tylophorine Derivatives (PBTs) As Potential Antitumor Agents. J. Med. Chem.  2007, 50(15), 3674-3680.
  13. Lin, L.; Shi, Q.; Nyarko, A.K.K.;  Bastow, K.F.; Su, C. Y.; Shih, C. C.-Y.; Lee*, K.H.  Anti-tumor Agents 250.  Design and Synthesis of New Curcumin Analogs As Potential Anti-Prostate Cancer Agents.  J. Med. Chem.  2006, 49(13), 3963-3972.
  14. Lin, L.; Shi, Q.; Su, C. Y.; Shih, C. C.-Y.; Lee*, K.H.  Anti-tumor Agents 247.  Synthesis and Anti-androgen Activity of 4-Ethoxycarbonylethyl Curcumin Analogs.  Bioorg. & Med. Chem.  2006, 14(8), 2527-2534.
  15. Xiao, Z.Y.; Bastaw, K.F.; Vance,J. R.; Sidwell, R.S.; Wang, H.K.; M. S. Chen, Shi, Q.; Lee*, K. H. Antitumor Agents. 234. Design, Synthesis, and Biological Evaluation of Novel 4ß-[(4”-Benzamido)-Amino]-4’-O-Demethyl-Epipodophyllotoxin Derivatives.  J. Med. Chem. 2004, 47, 5140-5148.
  16. Shi, Q.; Wang, H.K.; Lee*, K. H.  Antitumor Agents 210.  Synthesis and Evaluation of Taxoid-epipodophyllotoxin Conjugates as Novel Cytotoxic Agents. Bioorg. & Med. Chem.  2001, 9, 2999-3004.
  17. Shi, Q.; Chen, K.; Morris-Natschke, S.L.; Lee*, K. H.  Recent Progress in the Development of Tubulin Inhibitors As Antimitotic Antitumor Agents.  Curr. Pharm. Design. 1998, 4, 219-248.
  18. Shi, Q.; Chen, K.; Chen, X.; Brossi, A.; Hamel, E. A.; McPhail,T.; Lee*, K. H.  Syntheses and conformational analyses of allocolchicone and related alcohols and their esters. J. Org. Chem.  1998, 63, 4018-4025.
  19. Shi, Q.; Chen, K.; Verdier-Pinard, P.; Brossi, A.; Hamel, E. A.; McPhail,T.; Lee*, K. H.  Antitumor Agents. 181. Synthesis and biological evaluation of novel allo-congeners of thiocolchicine as antitubulin agents.  Helv. Chim. Acta. 1998, 81, 1023-1037.
  20. Shi, Q.; Verdier-Pinard, P.; Brossi, A.; Hamel, E. A.; Lee*, K. H.  Antitumor Agents 175. Antitubulin Action of (+)-Thiocolchicine Prepared by Partial Synthesis. Bioorg. & Med. Chem.  1997, 5, 2277-2282.
  21. Shi, Q.; Verdier-Pinard, P.; Brossi, A.; Hamel, E. A.; McPhail,T.; Lee*, K. H.  Antitumor Agents. 172.  Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents.  J. Med. Chem   1997, 40, 961-966.
  22. Shih, C.-Y.; Shi, Q.; Wang, H. K.; Su, C. Y.  Preparation and Biological activity of (Substituted Phenyl)-Propenal Compounds, Their Derivatives, and Use Thereof.  PCT Int. Appl. (2008).  WO 2008085984 A1.
  23. Shi, Q. Wang, H. K.; Oyama, M.; Vance, J.R.; Ming, M.S.  Anti-cancer Compounds.  Patent Number: WO 2004033423.  Issued in April 22, 2004.
  24. Lee, K.H.; Shi, Q., Bastow, K.F.  Taxoid Conjugates As Antimitotic And Antitumor Agents.  Patent Number: WO 2002026220.  Issued by April 4, 2002.
  25. Lee, K.H.; Shi, Q.; Yang, X.; Bastow, K.; Yang, P.C. 9-Substituted Phenanthrene Based Tylophorine Derivatives. WO 2010027424.
  26. Lee, K.H.; Dong, Y., Shi, Q., Bastow, K.F.; Wu, P.C.  Preparation of Arylfuropyranone  Derivatives for Use As Antitumor Agents.  Pat. No. WO 2010080415.  
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