Synthesis and Pharmacological Evaluation of 4-Iminothiazolidinones for Inhibition of PI3 Kinase.

Jo-Anne Pinson,Oleg Schmidt-Kittler,Mark Frazzetto,Zhaohua Zheng,Ian G Jennings,Kenneth W Kinzler,Bert Vogelstein,David K Chalmers,Philip E Thompson

AUSTRALIAN JOURNAL OF CHEMISTRY（2012）

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摘要

The thiazolidinedione, compound 1, has previously shown pan-inhibition of the phosphoinositide 3-kinase (PI3K) class I isoforms. We hypothesized the derivatization of the thiazolidinedione core of compound 1 could introduce isoform selectivity. We report the synthesis, characterization, and inhibitory activity of a novel series of 4-iminothiazolidin-2-ones for inhibition of the class I PI3K isoforms. Their synthesis was successfully achieved by multiple pathways described in this paper. Initial in vitro data of 28 analogues demonstrated poor inhibition of all class I PI3K isoforms. However, we identified an alternate target, the phosphodiesterases, and present preliminary screening results showing improved inhibitory activity.

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关键词

electrochemistry,analytical chemistry,spectroscopy,ionic liquids,kinetics,pharmaceutical chemistry,crystallography,density functional theory,educational,peptide,polymer chemistry,mass spectrometry,colloids,reaction mechanisms,photochemistry,sensors,macromolecules,nanotechnology,structure,medicinal chemistry,crystal structures,organic chemistry,quantum chemistry,self assembly,interfaces,proteins,biosensors,combinatorial,ab initio calculations,amino acids,bioinformatics,catalysis,biological chemistry,enzymes,inorganic chemistry,physical chemistry,biocatalysis,biomedical research,combinatorial chemistry,green chemistry,computational chemistry,surface chemistry,supramolecular chemistry

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