In:
Australian Journal of Chemistry, CSIRO Publishing, Vol. 65, No. 10 ( 2012), p. 1396-
Abstract:
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.
Type of Medium:
Online Resource
ISSN:
0004-9425
Language:
English
Publisher:
CSIRO Publishing
Publication Date:
2012
