Synthesis and Biological Evaluation of PF-543 Derivative
- Authors
- Kim, Seon Woong; Lee, Taeho; Lee, Joo-Youn; Kim, Sanghee; Jun, Hee-Sook; Park, Eun-Young; Baek, Dong Jae
- Issue Date
- Jan-2019
- Publisher
- BENTHAM SCIENCE PUBL LTD
- Keywords
- PF-543; sphingosine kinase; inhibitor; anticancer; derivative; medicinal chemistry
- Citation
- LETTERS IN ORGANIC CHEMISTRY, v.16, no.1, pp.2 - 5
- Journal Title
- LETTERS IN ORGANIC CHEMISTRY
- Volume
- 16
- Number
- 1
- Start Page
- 2
- End Page
- 5
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/2847
- DOI
- 10.2174/1570178615666181009121430
- ISSN
- 1570-1786
- Abstract
- PF-543 has been known as a substance that strongly inhibits SK1. However, it also exhibits antineoplastic activity that is lower than other inhibitors of SK1. In this study, we compared PF-543 and synthesized a newly designed derivative of PF-543 (compound 2) in which two aromatic structures were connected in para-form. The synthesized derivative showed inhibitory effect on SK1, similar to that of PF-543. However, it was more cytotoxic to HT29, AGS, and PC3 cells than PF-543. We also carried out a docking study for SK1 and demonstrated that the synthesized derivative showed interaction with SK1 similar to PF-543. Results obtained from this study suggest that the structure of compound 2 may be well substituted for the structure of PF-543 in terms of biological activity, providing us important structural information for the design of new derivatives of PF-543.
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