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Synthesis and Biological Evaluation of BODIPY-PF-543

College of Pharmacy, Mokpo National University, Jeonnam 58554, Korea
Department of Chemistry, Kyungpook National University, Daegu 41566, Korea
College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Korea
Department of Food and Nutrition, Eulji University, Seongnam 13135, Korea
Department of Chemistry, Sogang University, Seoul 04107, Korea
College of Pharmacy, Seoul National University, Seoul 08826, Korea
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2019, 24(23), 4408;
Received: 24 October 2019 / Revised: 29 November 2019 / Accepted: 30 November 2019 / Published: 2 December 2019
Sphingosine-1-phosphate (S1P) regulates the proliferation of various cells and promotes the growth of cancer cells. Sphingosine kinase (SK), which transforms sphingosine into S1P, has two isotypes: SK1 and SK2. To date, both isotypes are known to be involved in the proliferation of cancer cells. PF-543, an SK1 inhibitor developed by Pfizer, strongly inhibits SK1. However, despite its strong SK1 inhibitory effect, PF-543 shows low anticancer activity in vitro. Therefore, additional biological evidence on the anticancer activity of SK1 inhibitor is required. The present study aimed to investigate the intracellular localization of PF-543 and identify its association with anticancer activity by introducing a fluoroprobe into PF-543. Boron–dipyrromethene (BODIPY)-introduced PF-543 has a similar SK1 inhibitory effect as PF-543. These results indicate that the introduction of BODIPY does not significantly affect the inhibitory effect of SK1. In confocal microscopy after BODIPY-PF-543 treatment, the compound was mainly located in the cytosol of the cells. This study demonstrated the possibility of introducing fluorescent material into an SK inhibitor and designing a synthesized compound that is permeable to cells while maintaining the SK inhibitory effect. View Full-Text
Keywords: sphingosine kinase; PF-543; BODIPY; inhibitor; confocal microscopy sphingosine kinase; PF-543; BODIPY; inhibitor; confocal microscopy
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Shrestha, J.; Hwang, G.T.; Lee, T.; Kim, S.W.; Oh, Y.S.; Kwon, Y.; Hong, S.W.; Kim, S.; Seop Moon, H.; Baek, D.J.; Park, E.-Y. Synthesis and Biological Evaluation of BODIPY-PF-543. Molecules 2019, 24, 4408.

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