Synthesis and biological evaluation of L-alpha-phosphatidyl-D-3-deoxy-3-heteromethyl-myo-inositols as phosphoinositide 3-kinase inhibitors.

Paper

Synthesis and biological evaluation of L-alpha-phosphatidyl-D-3-deoxy-3-heteromethyl-myo-inositols as phosphoinositide 3-kinase inhibitors.

Published 2001 · D. S. Wang, C. S. Chen

Bioorganic & medicinal chemistry

Q2 SJR score

3

Citations

0

Influential Citations

Semantic Scholar

Abstract

We have synthesized a series of 3-deoxy-3-heteromethyl derivatives of L-alpha-phosphatidyl-D-myo-inositol as part of our effort to develop specific, reversible inhibitors of phosphoinositide (PI) 3-kinase. Among various derivatives examined, phosphatidyl-D-3-deoxy-3-aminomethyl-myo-inositol displays the highest potency in inhibiting PI 3-kinase both in vitro and in cells. It effectively suppressed antigen-stimulated degranulation in mast cells (IC(50), 17 microM), suggesting a potential application of this PI 3-kinase inhibitor as a mast cell-stabilizing agent.

In Vitro Study

Study Snapshot

Phosphatidyl-D-3-deoxy-3-aminomethyl-myo-inositol effectively inhibits phosphoinositide 3-kinase and suppresses mast cell degranulation, suggesting potential as a mast cell-stabilizing agent.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Paper

Synthesis and biological evaluation of L-alpha-phosphatidyl-D-3-deoxy-3-heteromethyl-myo-inositols as phosphoinositide 3-kinase inhibitors.

Sign up to use Study Snapshot

References

Citations

New Insights into PI3K Inhibitor Design using X-ray Structures of PI3Kα Complexed with a Potent Lead Compound

YXY-4F, a moderate PI3K inhibitor with low molecular weight, promotes flexible conformational changes in residues Ser773 and Ser774, potentially guiding further optimization of PI3K inhibitors for cancer treatment.

A formal stereoselective synthesis of (−)-brevisamide

This study presents a efficient stereoselective formal synthesis of ()-brevisamide using syn-Aldol reaction, Sharpless asymmetric epoxidation, and 6-endo-cyclization of hydroxy styrylepoxide.

Therapeutic potential of phosphoinositide 3-kinase inhibitors

PI 3-K inhibitors show potential in treating cancer, cardiovascular disorders, autoimmune diseases, and inflammation, but require further validation in human clinical trials.