Lan Xie, Ph.D. Email: Lxie@Email.Unc.Edu; Adjunct Professor Tel: 919-445-2933 (O) Education DEGREE YY/MM Major Wuhan University, Wuhan, China B.S

Dr. L. Xie’s brief resume, 2020

Lan Xie, Ph.D. Email: [email protected]; Adjunct Professor Tel: 919-445-2933 (O) Education DEGREE YY/MM Major Wuhan University, Wuhan, China B.S. 1978/03 – 1982/01 Organic Chemistry University of North Carolina at Chapel Hill, NC, USA Ph.D. 1995/08 – 1999/09 Medicinal Chemistry

Employment and Positions 2002/04 – 2016/12 Professor, Beijing Institute of Pharmacology and Toxicology, Beijing, China. 2000/12 – 2002/03 Scientist, Chemistry Department, Triad Therapeutics, Inc., San Diego, CA, USA 1999/10 – 2000/11 Postdoctoral Fellow, School of Pharmacy, UNC-CH, NC, USA 1993/06 – 1995/07 Visiting scholar, School of Pharmacy, UNC-CH , NC, USA 1982/02 – 1993/05 Assistant Researcher (1982-86) and Associate Researcher (1987-93), Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China. Other Experience and Professional Memberships 2007 – present Adjunct professor, UNC Eshelman School of Pharmacy, UNC-CH, NC, USA 2004 – present Editorial Board Member of Acta Pharmaceutica Sinica, China.

Research Areas: Medicinal Chemistry for discovery and optimizations of novel drug leads and candidates with anti-HIV and antitumor activities, including design, synthesis, biological evaluation, and druggability assessments.

Publications (Partial of >90, including 12 articles in J. Med. Chem.):

1. Jiang, L.; Goto, M.; Zhu, D. Q.; Hsu, P. L.; Li, K. P.; Cui, M.T.; He, X. Y.; Morris-Natschke, S. L.; Lee, K. H.; Xie, L.*

Scaffold hopping-driven optimization of 4-(quinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)ones as novel tubulin inhibitors. ACS Med. Chem. Lett. 2020, 11, 83-89. 2. Yu, F.; Li, W.; Wang, L.; Dai, Y.; Lu, X.; Wang, Q.; Xie, L.; Jiang, S. Combining new non-nucleoside reverse transcriptase inhibitors (RTIs) with AZT results in strong synergism against multi-RTI-resistant HIV-1 strains. Molecules, 2018, 23, 1599-1605. 3. Huang, L.; Lai, W. H.; Zhu, L.; Wei, L.; Li, W.; Lee, K. H.; Xie, L.; Chen, C. H. Elimination of HIV-1 latently infected cells by gnidimacrin and a selective HDAC inhibitor. ACS Med. Chem. Lett, 2018, 9, 268-273 4. Cui, M. T.; Jiang, L.; Goto, M.; Hsu, P. L.; Li, L.; Zhang, Q.; Wei, L.; Yuan, S. J.; Hamel, E.; Morris-Natschke, S. L.; Lee, K. H.; Xie, L.* In vivo and mechanistic studies on antitumor lead 7‑methoxy-4-(2-methyl quinazolin-4-yl)- 3,4-dihydroquinoxalin-2(1H)‑one and its modification as a novel class of tubulin-binding tumor-vascular disrupting agents. J. Med. Chem., 2017, 60, 5586-5598. 5. Wei, L.; Wang, H. L.; Huang, L.; Chen, C. H.; L. Xie, Morris-Natschke, S. L.; Lee, K. H.; Xie, L.* Drug-like property- driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against riplivirine-resistant mutant virus. Bioorg. Med. Chem. Lett., 2017, 27, 2788-2792. 6. N. Liu, L. Wei, L. Huang, F. Yu, W. Zheng, B. Qin, D. Q. Zhu, S. L. Morris-Natschke, S. Jiang, C. H. Chen, K. H. Lee, L. Xie. Novel HIV-1 NNRTI agents: optimization of diarylanilines with high potency against wild-type and rilpivirine-resistant E138K mutant virus. J. Med. Chem., 2016, 59, 3689-3704 7. Wang, S. B.; Cui, M. T.; Wang, X. F.; Ohkoshi, E.; Goto, M.; Yang, D. X.; Li, L.; Yuan, S.; Morris-Natschke, S. L.; Lee, K. H.; Xie, L.* Synthesis, biological evaluation, and physicochemical property assessment of 4-substituted 2-phenylamino quinazolines as Mer tyrosine kinase inhibitors, Bioorg. Med. Chem., 2016, 24, 3083-3092 8. S. B. Wang, X. F. Wang, B. Qin, E. Ohkoshi, K. Y. Hsien, E. Hamel, M. T. Cui, D. Q. Zhu, M. Goto, S. L. Morris-Natschke, K. H. Lee, L. Xie,* Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors. Bioorg. Med. Chem. 2015, 23, 5740-5747 9. X. F. Wang, F. Guan, E. Ohkoshi, W. Guo, L. Wang, D. Q. Zhu, S. B. Wang, L. T. Wang, E. Hamel, D. Yang, L. Li, K. Qian, S. L. Morris-Natschke, S. Yuan, K. H. Lee, L. Xie*, Optimization of 4-(N-cycloamino)phenyl quinazolines as a novel class of tubulin-polymerization inhibitors targeting the colchicine site. J. Med. Chem. 2014, 57, 1390-1402

Dr. L. Xie’s brief resume, 2020

10. N. Liu, B. Qin, L. Q. Sun, F. Yu, L. Lu, S. Jiang, K. H. Lee, L. Xie* Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors, Bioorg. Med. Chem. Lett., 2014, 24, 3719-3725 11. Z. Y. Wu, N. Liu, B. Qin, L. Huang, F. Yu, K. Qian, S. Jiang, C. H. Chen, K. H. Lee, L. Xie,* Optimization of antiviral potency and molecular properties of halogenated 2,6-diarylpyridinamines (DAPAs) as a novel class of HIV-1 NNRTIs. ChemMedChem, 2014, 9(7), 1546-1555 12. F. L. Yu, X. Y. He, C. Gu, E. Ohkoshi, L. T. Wang, C. Y. Lai, L. Yu, S. B. Wang, S. L. Morris-Natschke, K. H. Lee, S. Liu, L. Xie* Synthesis and biological evaluation of dibenzocyclooactatetraene derivatives and related unsymmetrical biphenyls as new antitumor agents inhibiting NF-κB signaling pathway. Bioorg. Med. Chem. 2014, 22(1), 325-333 13. X. F. Wang, S.B. Wang, E. Ohkoshi, L. T. Wang, E. Hamel, K. Qian, S. L. Morris-Natschke, K. H. Lee, L. Xie* Discovery of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as a novel class of antitumor agents targeting at colchicine binding site of tubulin, Eur. J. Med. Chem. 2013, 67, 196-207 14. X. Y. He, L. Lu, J. Qiu, P. Zou, X. K. Jiang, L. Li, S. Jiang, S. Liu, L. Xie* Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5- (3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl) -N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41, Bioorg. Med. Chem. 2013, 21, 7539-7548 15. L. Q. Sun, L. Zhu, K. Qian, B. Qin, L. Huang, C. H. Chen, K. H. Lee, L. Xie* Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 NNRTI drug candidates, J. Med. Chem. 2012, 55(16), 7219-7229 16. X. Y. He, P. Zou, J. Qiu, L. Hou, S. Jiang, S. Liu, L. Xie*, Design, synthesis and biological evaluation of 3-substituted 2,5-dimethyl-N-(3-(1H-tetrazol-5-yl)phenyl)pyrroles as novel potential HIV-1 gp41 inhibitors, Bioorg. Med. Chem. 2011, 19(22)：6726-6734 17. X. T. Tian, B. J. Qin, Z. Y. Wu, H. Lu, X. F. Wang, S. Jiang, C. H. Chen, K. H. Lee, L. Xie*. Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors, J. Med. Chem. 2010, 53(23), 8287-8297 18. B. Qin, X. K. Jiang, H. Lu, X. T. Tian, F. Barbault, K. Qian, C. H. Chen, S. Jiang, R. Huang, K. H. Lee, L. Xie*. Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors, J. Med. Chem. 2010, 53(13), 4906-4916 19. K. Liu, H. Lu, L. Hou, Z Qi, C. Teixeiral, F. Barbault, B. T. Fan, S. Jiang, L. Xie*, Design, synthesis, and anti-HIV activity of N-carboxyphenylpyrrole derivatives as potent small molecule fusion inhibitors targeting gp41, J. Med. Chem. 2008, 51(24), 7843-7854 20. L. Xie*, H. F. Guo, H. Lu, X. M. Zhuang, A. M. Zhang, G. Wu, J. X. Ruan, T. Zhou, D. Yu, K. Qian, K. H. Lee, S. Jiang, Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3- cyanomethyl- 3',4'-di-O-(S)- camphanoyl-4-methyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK), J. Med. Chem. 2008, 51(24), 7689-7696 21. G. Wu, H. F. Guo, K. Gao, Y. N. Liu, K. F. Bastow, S. L. Morris-Natschke, K. H. Lee, L. Xie*, Synthesis of unsymmetrical biphenyls as potent cytotoxic agents, Bioorg. Med. Chem. Lett. 2008, 18, 5272-6 22. L. Xie*, C. H. Zhao, T. Zhuo, H. F. Chen, B. T. Fan, J. Z. Mao, J. Y. Li, Z. Y. Bao, D. Yu, and K. H. Lee, Molecular modeling, design, synthesis, and biological evoluation of novel 3', 4'-Di-O-(S)-camphanoyl-(+)- cis-khellactone (DCK) analogues as potent anti-HIV agents, Bioorg. Med. Chem. 2005, 13：6435-49 23. L. Xie, D. Yu, C. Wild, G. Allaway, J. Turpin, P. C. Smith, and K. H. Lee, Anti-AIDS agents 52. synthesis and anti-HIV activity of hydroxymethyl (3'R,4'R)-3', 4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives, J. Med. Chem. 2004, 47, 756-760 24. L. Xie, G. Allaway, C. Wild, N. Kilgore, and K. H. Lee, Anti-AIDS agents 47. Synthesis and anti-HIV activity of 3-sustituted 3’, 4’-di-O-(S)-camphanoyl- (+)-cis-khellactone (DCK) analogues, Bioorg. Med. Chem. Lett. 2001, 11(17), 2291-2293 25. L. Xie, Y. Takeuchi, L. M. Cosentino, and K. H. Lee, Anti-AIDS agents 42. synthesis and anti-HIV activity of di-sustituted 3’, 4’-di-O-(S)-camphanoyl- (+)-cis-khellactone (DCK) analogues, J. Med. Chem. 2001, 44(5): 664-671

Dr. L. Xie’s brief resume, 2020 26. L. Xie, Y.Takeuchi; L. M. Cosentino; , K. H. Lee. Anti-AIDS agents 37. Synthesis and structure-activity relationships of (3'R,4'R)-(+)-cis-khellactone derivatives as novel potent anti-HIV agents, J. Med. Chem. 1999, 42(14): 2662-2672