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The research focus of the laboratory is the discovery, and pre-clinical development of anti-herpes and anti-tumor agents as investigational tools and as potential drug candidates. The principal approach used for antiviral compounds is ligand-based design around the acridone template (1) and several interesting hits with novel mechanism are under investigation [1-5]. The anti-tumor work, largely done in conjunction with the Natural Products Laboratory (NPL), uses both target-based (i.e. DNA topoisomerases I and II) and ligand-based methods to identify hits and develop leads. For example; Neotanshinlactone (2) was identified as a new chemical entity with selective in vitro anti-breast cancer activity [6]; the C4’-acyl analogue (3) of GL331 retains Top II inhibition and superior drug-resistance activity profile [7]. Other examples highlighting recent significant discoveries are provided below [8-12].
[1] Akanitapichat, P. et al., (2000) Antiviral Research 45, 123-134.
[2] Akanitapichat, P.and Bastow, K. F (2002) Antiviral Research 53, 113-126.
[3] Lowden, C. T.; Bastow, K. F. (2003) Antiviral Research 59, 143-154.
[4] Lowden, C. T. and Bastow, K. F. (2003) J. Med. Chem., 46, 5015-5020.
[5] Bastow, K. F. (2004) Current Drug Targets: Infectious Disorders, 4323-330.
[6] Wang, Xihong et al., (2004) J. Med. Chem., 47, 5816-5819
[7] Han, S et al., (2004) Bioorg. & Med. Chem. Let. 14, 2979-2982.
[8] Krishnan, P. and K.F. Bastow, K.F. (2000) Biochem. Pharmacol., 60, 1367-1379
[9] US Patent No. 6,420,377 (2002)
[10] Nakanishi, Y et al., (2003) J. Med. Chem., 46, 3185-3188
[11] Hyashi, K. et.al., (2004) J. Nat. Prod. (2004), 67, 990-993.
[12] US patent No. 6,916,831 (2005)
Current Members:
Visiting Pre-doctoral Scientists from National Taiwan University Taiwan University, Tapei, Taiwan
Current Support: NIH-NCI (CA 17625) entitled “Plant Anti-tumor Agents," 6/10/05 - 5/31/10