The Natural Products Research Laboratories (NPRL) has established an exceptional research program in rational drug discovery. Current research programs in the NPRL include the following:

1. Medicinal Chemistry
2. Bioactive Natural Products
3. New Anticancer and Anti-AIDS Drug Discovery and Development
4. Chinese Medicine

Research Highlights

The following example bioactive compounds discovered by the NPRL are currently in clinical trials or preclinical studies:

1. GL-331, a synthetic etoposide analog developed in the NPRL, was in Phase II clinical trial as an anticancer drug.
2. Bevirimat (PA-457, DSB, MPC-4326), a modified triterpene natural product, licensed previously to Panacos Pharmaceuticals, Inc. and now to Myriad Pharmaceutical Company, has succeeded in Phase IIa anti-AIDS clinical trials.  Phase III clinical trials plan to begin in 2011, following the completion of Phase IIb clinical trials.  Bevirimat is a first-in-class maturation inhibitor.
3. Novel curcumin analogs discovered and developed in the NPRL were licensed to AndroScience Corporation of San Diego, CA.  One compound, JC-9, is currently in a Phase II clinical trial for treating acne.  JC-9 is planned for a clinical trial for prostate cancer in the near future.
4. A 2-phenyl-4-quinolone analog, CHM-2133-P, has shown excellent in vivo antitumor activity against ovarian cancer. Effpha Corp., Taiwan, has licensed this technology and is in process for initiating a Phase I clinical trial as an anticancer drug.
5. Preclinical studies on numerous novel promising natural product-based leads including DCP analogs as anti-AIDS agents as well as analogs of tylophorine and neotanshinlactone as drugs for treating lung and breast cancers are in progress.

Current Lab Personnel

Joshua Brattlie

Masuo Goto, PhD

Po-Yen Liu

Ying-Qian Liu, PhD

Yan Lu, PhD

Susan Morris-Natschke, PhD

Kyoko Nakagawa-Goto, PhD

Emika Ohkoshi, PhD

Keduo Qian, PhD

Qian Shi, PhD

Chih-Ya Wang

Qiang Wang, PhD

Xiaoming Yang, PhD

Examples of Recent Publications & Patents Selected from More than 740 articles and 77 patents

1. K.H. Lee, "Antitumor Agents 275 and Anti-AIDS Agents 80. Discovery and Development of Natural Product-derived Chemotherapeutic Agents Based on a Medicinal Chemistry Approach,” J. Nat. Prod., 73, 500-516 (2010) and literature cited therein. 2009 Norman R. Farnsworth Research Achievement Award from American Society of Pharmacognosy
2. Y. Dong, Q. Shi, H.C. Pai, C.Y. Peng, S.L. Pan, C.M. Teng, K. Nakagawa-Goto, D. Yu, Y.N. Liu, P.C. Wu, K.F. Bastow, S.L. Morris-Natschke, A. Brossi, J.Y. Lang, J. L. Hsu, M.C. Hung, E.Y.-H.P. Lee, and K.H. Lee, “Antitumor Agents 272. Structure–Activity Relationships and In Vivo Selective Anti-Breast Cancer Activity of Novel Neo-tanshinlactone Analogs,” J. Med. Chem., 53, 2299-2308 (2010).
3. K. Qian, R.Y. Kuo, C.H. Chen, L. Huang, S.L. Morris-Natschke, and K. H. Lee, “Anti-AIDS Agents 81. Design, Synthesis and Structure-Activity Relationship Study of Betulinic Acid and Moronic Acid Derivatives as Potent HIV Maturation Inhibitors”, J. Med. Chem., 53, 3133-3141 (2010).
4. X. Yang, Q. Shi, S.C. Yang, C.Y. Chen, S.L. Yu, K.F. Bastow, S.L. Morris-Natschke, P.C. Wu, C.Y. Lai, T.S. Wu, S.L. Pan, C.M. Teng, J.C. Lin, P.C. Yang, and K.H. Lee, “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., 54, 5097-5107 (2011).
5. K.H. Lee, X.H. Wang, K.F. Bastow, and T.S. Wu, "Neo-tanshinlactone and Analogs as Potent and Selective Anti-breast Cancer Agents," US Patent No. 7,495,026 B2: Issued 2/24/2009.

About Dr. Lee

Dr. Lee combines the fields of natural products and synthetic medicinal chemistry research to discover and develop bioactive natural products and their analogs as clinical trials drug candidates. Since 1971, the NPRL has discovered several thousand novel bioactive natural products and synthetic analogs. These discoveries are used as new leads to develop future pharmaceuticals agents in the same manner that numerous previously discovered bioactive natural products (including ephredrine, taxol, and artemisinin) were developed as current pharmaceutical agents to treat cancers and other diseases. Using basic natural products and medicinal chemistry principles coupled with modern technologies, including new computational techniques and mechanism of action or target-based and genomic evaluation methods, our newly discovered lead compounds will provide a solid foundation of potential chemotherapeutic drug candidates in the twenty-first century.