pf-543 and 4-4-difluoro-4-bora-3a-4a-diaza-s-indacene

pf-543 has been researched along with 4-4-difluoro-4-bora-3a-4a-diaza-s-indacene* in 2 studies

Other Studies

2 other study(ies) available for pf-543 and 4-4-difluoro-4-bora-3a-4a-diaza-s-indacene

Article	Year
Verification of the Necessity of the Tolyl Group of PF-543 for Sphingosine Kinase 1 Inhibitory Activity. Molecules (Basel, Switzerland), 2020, May-27, Volume: 25, Issue:11 PF-543, the most potent sphingosine kinase (SK) inhibitor, does not demonstrate effective anticancer activity in some cancer cells, unlike other known SK1 inhibitors. PF-543 has a non-lipid structure with a unique toluene backbone; however, the importance of this structure remains unclear. Therefore, the purpose of this study was to investigate changes in SK inhibitory and anticancer activities and to explore the role of the tolyl group structure of PF-543 through various modifications. We transformed the methyl group of PF-543 into hydrogen, fluorine, and hydroxy. PF-543 derivatives in which the methyl group was substituted by hydrogen and fluorine (compound Topics: Animals; Boron Compounds; Dogs; Humans; Methanol; Mice; Microsomes, Liver; Phosphotransferases (Alcohol Group Acceptor); Pyrrolidines; Rats; Structure-Activity Relationship; Sulfones	2020
Synthesis and Biological Evaluation of BODIPY-PF-543. Molecules (Basel, Switzerland), 2019, Dec-02, Volume: 24, Issue:23 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. Topics: Boron Compounds; Chemistry Techniques, Synthetic; Enzyme Inhibitors; Methanol; Molecular Structure; Phosphotransferases (Alcohol Group Acceptor); Pyrrolidines; Spectrum Analysis; Structure-Activity Relationship; Sulfones	2019

Article

Year

Verification of the Necessity of the Tolyl Group of PF-543 for Sphingosine Kinase 1 Inhibitory Activity.

Molecules (Basel, Switzerland), 2020, May-27, Volume: 25, Issue:11

PF-543, the most potent sphingosine kinase (SK) inhibitor, does not demonstrate effective anticancer activity in some cancer cells, unlike other known SK1 inhibitors. PF-543 has a non-lipid structure with a unique toluene backbone; however, the importance of this structure remains unclear. Therefore, the purpose of this study was to investigate changes in SK inhibitory and anticancer activities and to explore the role of the tolyl group structure of PF-543 through various modifications. We transformed the methyl group of PF-543 into hydrogen, fluorine, and hydroxy. PF-543 derivatives in which the methyl group was substituted by hydrogen and fluorine (compound

Topics: Animals; Boron Compounds; Dogs; Humans; Methanol; Mice; Microsomes, Liver; Phosphotransferases (Alcohol Group Acceptor); Pyrrolidines; Rats; Structure-Activity Relationship; Sulfones

2020

Synthesis and Biological Evaluation of BODIPY-PF-543.

Molecules (Basel, Switzerland), 2019, Dec-02, Volume: 24, Issue:23

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.

Topics: Boron Compounds; Chemistry Techniques, Synthetic; Enzyme Inhibitors; Methanol; Molecular Structure; Phosphotransferases (Alcohol Group Acceptor); Pyrrolidines; Spectrum Analysis; Structure-Activity Relationship; Sulfones

2019