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Discovery and Development of Natural Product-Derived Chemotherapeutic Agents Based on a Medicinal Chemistry Approach
Open accessAbstract
Medicinal plants have long been an excellent source of pharmaceutical agents. Accordingly, the long-term objectives of the author's research program are to discover and design new chemotherapeutic agents based on plant-derived compound leads by using a medicinal chemistry approach, which is a combination of chemistry and biology. Different examples of promising bioactive natural products and their synthetic analogues, including sesquiterpene lactones, quassinoids, naphthoquinones, phenylquinolones, dithiophenediones, neo-tanshinlactone, tylophorine, suksdorfin, DCK, and DCP, will be presented with respect to their discovery and preclinical development as potential clinical trial candidates. Research approaches include bioactivity- or mechanism of action-directed isolation and characterization of active compounds, rational drug design-based modification and analogue synthesis, and structure-activity relationship and mechanism of action studies. Current clinical trial agents discovered by the Natural Products Research Laboratories, University of North Carolina, include bevirimat (dimethyl succinyl betulinic acid), which is now in phase IIb trials for treating AIDS. Bevirimat is also the first in a new class of HIV drug candidates called "maturation inhibitors". In addition, an etoposide analogue, GL-331, progressed to anticancer phase II clinical trials, and the curcumin analogue JC-9 is in phase II clinical trials for treating acne and in development for trials against prostate cancer. The discovery and development of these clinical trial candidates will also be discussed.
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Cites
Catalytic Asymmetric Dihydroxylation
Kolb, H. C., VanNieuwenhze, M. S., & Sharpless, K. B. (1994) · Chemical Reviews · doi:10.1021/cr00032a009 · Cited by 3,701
New developments in the chemistry and biology of the bioactive constituents of tanshen
Wang, X., Morris‐Natschke, S. L., & Lee, K. (2007) · Medicinal Research Reviews · doi:10.1002/med.20077 · Cited by 565
Self-citationFujioka, T., Kashiwada, Y., Kilkuskie, R. E., Cosentino, L. M., Ballas, L. M., Jiang, J. B., Janzen, W. P., Chen, I.-S., & Lee, K.-H. (1994) · Journal of Natural Products · doi:10.1021/np50104a008 · Cited by 470
Self-citationLi, F., Goila-Gaur, R., Salzwedel, K., Kilgore, N. R., Reddick, M., Matallana, C., Castillo, A., Zoumplis, D., Martin, D. E., Orenstein, J. M., et al. (2003) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2234683100 · Cited by 426
Mechanism of Action of Antitumor Drug Etoposide: A Review
van Maanen, J. M. S., Retel, J., de Vries, J., & Pinedo, H. M. (1988) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/80.19.1526 · Cited by 295
Betulinic Acid and Dihydrobetulinic Acid Derivatives as Potent Anti-HIV Agents
Kashiwada, Y., Hashimoto, F., Cosentino, L. M., Chen, C.-H., Garrett, P. E., & Lee, K.-H. (1996) · Journal of Medicinal Chemistry · doi:10.1021/jm950922q · Cited by 272
Self-citationIto, J., Chang, F.-R., Wang, H.-K., Park, Y. K., Ikegaki, M., Kilgore, N., & Lee, K.-H. (2001) · Journal of Natural Products · doi:10.1021/np010211x · Cited by 259
Self-citationKashiwada, Y., Yamazaki, K., Ikeshiro, Y., Yamagishi, T., Fujioka, T., Mihashi, K., Mizuki, K., Cosentino, L. M., Fowke, K., Morris-Natschke, S. L., et al. (2001) · Tetrahedron · doi:10.1016/s0040-4020(00)01144-3 · Cited by 238
Self-citationRecent advances in the investigation of curcuminoids
Itokawa, H., Shi, Q., Akiyama, T., Morris-Natschke, S. L., & Lee, K.-H. (2008) · Chinese Medicine · doi:10.1186/1749-8546-3-11 · Cited by 237
Self-citationCytotoxicity of sesquiterpene lactones.
Lee, K., Huang, E., Piantadosi, C. A., Pagano, J. S., & Geissman, T. A. (1971) · PubMed · Cited by 210
Self-citationSesquiterpene Antitumor Agents: Inhibitors of Cellular Metabolism
Lee, K.-H., Hall, I. H., Mar, E.-C., Starnes, C. O., ElGebaly, S. A., Waddell, T. G., Hadgraft, R. I., Ruffner, C. G., & Weidner, I. (1977) · Science · doi:10.1126/science.191909 · Cited by 210
Self-citationSHIKISHIMA, Y., TAKAISHI, Y., HONDA, G., ITO, M., TAKEDA, Y., KODZHIMATOV, O. K., ASHURMETOV, O., & LEE, K.-H. (2001) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.49.877 · Cited by 183
Self-citationLin, L., Shi, Q., Nyarko, A. K., Bastow, K. F., Wu, C.-C., Su, C.-Y., Shih, C. C.-Y., & Lee, K.-H. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm051043z · Cited by 175
Self-citationLee, K.-H. (2004) · Journal of Natural Products · doi:10.1021/np030373o · Cited by 165
Self-citationKupchan, S. M., Britton, R. W., Lacadie, J. A., Ziegler, M. F., & Sigel, C. W. (1975) · The Journal of Organic Chemistry · doi:10.1021/jo00893a023 · Cited by 163
Chen, D.-F., Zhang, S.-X., Xie, L., Xie, J.-X., Chen, K., Kashiwada, Y., Zhou, B.-N., Wang, P., Cosentino, L. M., & Lee, K. (1997) · Bioorganic & Medicinal Chemistry · doi:10.1016/s0968-0896(97)00118-1 · Cited by 156
Self-citationXie, L., Takeuchi, Y., Cosentino, L. M., & Lee, K. (1999) · Journal of Medicinal Chemistry · doi:10.1021/jm9900624 · Cited by 142
Self-citationWu, Y., Hung, Y.-C., Chang, F., et al. (1996) · Journal of Natural Products · doi:10.1021/np960416j · Cited by 138
HIV entry inhibitors and their potential in HIV therapy
Qian, K., Morris-Natschke, S. L., & Lee, K. (2008) · Medicinal Research Reviews · doi:10.1002/med.20138 · Cited by 123
Self-citationAnti-AIDS Agents 69. Moronic Acid and Other Triterpene Derivatives as Novel Potent Anti-HIV Agents
Yu, D., SAKURAI, Y., Chen, C., Chang, F., Huang, L., Kashiwada, Y., & Lee, K. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm0601912 · Cited by 120
Self-citationDuan, H., Takaishi, Y., Imakura, Y., Jia, Y., Li, D., Cosentino, L. M., & Lee, K. (2000) · Journal of Natural Products · doi:10.1021/np990281s · Cited by 110
Self-citationKashiwada, Y., Nishizawa, M., Yamagishi, T., et al. (1995) · Journal of Natural Products · doi:10.1021/np50117a007 · Cited by 108
Antimalaria studies on Qinghaosu.
(1979) · PubMed · Cited by 108
Anti-AIDS Agents. 15. Synthesis and Anti-HIV Activity of Dihydroseselins and Related Analogs
Huang, L., Kashiwada, Y., Cosentino, L. M., Fan, S., Chen, C., McPhail, A. T., Fujioka, T., Mihashi, K., & Lee, K.-H. (1994) · Journal of Medicinal Chemistry · doi:10.1021/jm00049a014 · Cited by 106
Self-citationNishizawa, M., Yamagishi, T., Dutschman, G. E., Parker, W. B., Bodner, A. J., Kilkuskie, R. E., Cheng, Y., & Lee, K. (1989) · Journal of Natural Products · doi:10.1021/np50064a016 · Cited by 88
Self-citationWei, L., Brossi, A. R., Kendall, R., Bastow, K. F., Morris-Natschke, S. L., Shi, Q., & Lee, K. (2006) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2006.06.009 · Cited by 85
Self-citationCho, S. J., Tropsha, A., Suffness, M., Cheng, Y., & Lee, K. (1996) · Journal of Medicinal Chemistry · doi:10.1021/jm9503052 · Cited by 80
Self-citationQian, K., Yu, D., Chen, C., Huang, L., Morris-Natschke, S. L., Nitz, T. J., Salzwedel, K., Reddick, M., Allaway, G. P., & Lee, K. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm900136j · Cited by 79
Self-citationYu, D., Chen, C., Brossi, A. R., & Lee, K. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm0400505 · Cited by 79
Self-citationMechanism of action and resistant profile of anti-HIV-1 coumarin derivatives
Huang, L., Yuan, X., Yu, D., Lee, K. H., & Chen, C. (2005) · Virology · doi:10.1016/j.virol.2004.11.033 · Cited by 76
Self-citationAntitumor agents 247. New 4-ethoxycarbonylethyl curcumin analogs as potential antiandrogenic agents
Li, L., Shi, Q., Su, C.-Y., Shih, C. C.-Y., & Lee, K. (2006) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2005.11.034 · Cited by 76
Self-citationLee, T. T.-Y., Kashiwada, Y., Huang, L., Snider, J., Cosentino, M., & Lee, K. (1994) · Bioorganic & Medicinal Chemistry · doi:10.1016/s0968-0896(00)82054-4 · Cited by 75
Self-citationLee, K., Furukawa, H., & Huang, E. (1972) · Journal of Medicinal Chemistry · doi:10.1021/jm00276a010 · Cited by 71
Self-citationNovel Anti-Prostate Cancer Curcumin Analogues That Enhance Androgen Receptor Degradation Activity
Shi, Q., Shih, C. C.-Y., & Lee, K. H. (2009) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/187152009789124655 · Cited by 68
Self-citationYu, D., Wild, C. T., Martin, D. E., Morris-Natschke, S. L., Chen, C., Allaway, G. P., & Lee, K. (2005) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.14.6.681 · Cited by 52
Self-citationPotent Activity of the HIV-1 Maturation Inhibitor Bevirimat in SCID-hu Thy/Liv Mice
Stoddart, C. A., Joshi, P., Sloan, B. A., Bare, J. C., Smith, P. C., Allaway, G. P., Wild, C. T., & Martin, D. E. (2007) · PLoS ONE · doi:10.1371/journal.pone.0001251 · Cited by 50
Antibiotic resistance versus small molecules, the chemical evolution
LEE, V. J., & Hecker, S. J. (1999) · Medicinal Research Reviews · doi:10.1002/(sici)1098-1128(199911)19:6<569::aid-med7>3.0.co;2-9 · Cited by 46
Xie, L., Yu, D., Wild, C. T., Allaway, G. P., Turpin, J. A., Smith, P. C., & Lee, K. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm030416y · Cited by 41
Self-citationChang, J., Han, F. S., Liu, S.-Y., Wang, Z. Q., Lee, K., & Cheng, Y.-S. (1991) · PubMed · Cited by 39
Self-citationXie, L., Xie, J.-X., Kashiwada, Y., Cosentino, L. M., Liu, S.-H., Pai, R. B., Cheng, Y.-C., & Lee, K.-H. (1995) · Journal of Medicinal Chemistry · doi:10.1021/jm00016a002 · Cited by 33
Self-citationAntitumor Agents 260. New Desmosdumotin B Analogues with Improved In Vitro Anticancer Activity
Nakagawa‐Goto, K., Bastow, K. F., Chen, T.-H., Morris-Natschke, S. L., & Lee, K. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm701208v · Cited by 30
Self-citationLee, K., Okano, M., Hall, I. H., Brent, D. A., & Soltmann, B. (1982) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600710320 · Cited by 27
Self-citationYang, Z.-Y., Yi, X., Xia, P., Brossi, A. R., Cosentino, L. M., & Lee, K.-H. (2000) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(00)00126-8 · Cited by 23
Self-citationPharmacological Evaluation of Medicinal Plants From Western Samoa
Norton, T. R., Bristol, M. L., Read, G. W., Bushnell, O. A., Kashiwagi, M., Okinaga, C. M., & Oda, C. S. (1973) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600620705 · Cited by 23
Apigenin-7-O-β-D-glucopyranoside, an anti-HIV principle from Kummerowia striata
Tang, R., Chen, K., Cosentino, M., & Lee, K. (1994) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/0960-894x(94)80015-4 · Cited by 22
Self-citationAcid Degradation Products of Qinghaosu and Their Structure-Activity Relationships
Imakura, Y., Hachiya, K., Ikemoto, T., Yamashita, S., Kihara, M., Kobayashi, S., Shingu, T., Milhous, W. K., & Lee, K. (1990) · Heterocycles · doi:10.3987/com-90-5396 · Cited by 22
Self-citationYang, Z., Xia, Y., Xia, P., Cosentino, L. M., & Lee, K.-H. (1998) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(98)00254-6 · Cited by 19
Self-citationAntitumor agents 248. Chemistry and antitumor activity of tylophorinerelated alkaloids
Wei, L., Brossi, A. R., Morris-Natschke, S. L., Bastow, K. F., & Lee, K. (2008) · Studies in natural products chemistry · doi:10.1016/s1572-5995(08)80023-3 · Cited by 16
Self-citationAntimalarial Artemisinin Analogs: Synthesis of 2,3-Desethano-12-deoxoartemisinin-related Compounds
Imakura, Y., Hachiya, K., Ikemoto, T., Kobayashi, S., Yamashita, S., Sakakibara, J., Smith, F., & Lee, K. (1990) · Heterocycles · doi:10.3987/com-90-5618 · Cited by 13
Self-citationNakagawa‐Goto, K., Chen, T.-H., Peng, C.-Y., Bastow, K. F., Wu, J.-H., & Lee, K. (2007) · Journal of Medicinal Chemistry · doi:10.1021/jm0702534 · Cited by 12
Self-citation
Cited by
Tsuchiya, H. (2015) · Molecules · doi:10.3390/molecules201018923 · Cited by 237
Metadata
- Authors
- Lee, K.-H.
- Venue
- Journal of Natural Products
- Publisher
- American Chemical Society (ACS)
- Published
- 2010-02-26
- Volume
- 73
- Issue
- 3
- Pages
- 500-516
- ISSN
- 0163-3864 (ISSN-L)
- 1520-6025
- OpenAlex
- W2032253069
- Cited by
- 278
- References
- 50
- FWCI
- 7.77
- Type
- journal article
- Language
- en
- Open access
- green
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