Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis and Biological Evaluation of Novel 4-indolyl-5-phenyl(indolyl)- 1,2-dihydropyrazol-3-ones as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors

Author(s): Hong Yin, Fengying Sui, Xinji Yang, Yingying Shangguan, Guojie Song.


Nineteen novel 4-indolyl-5-phenyl(indolyl)-1,2-dihydropyrazol-3-ones were synthesized and evaluated for their GSK-3β inhibitory activity. Half of the tested compounds showed moderate GSK-3β inhibitory activity. Preliminary structure-activity relationships were discussed, which showed that the presence of 3,4,5-trimethoxy group on the benezene ring enhanced potency while the existence of an electron-withdrawing group at the 4-position of the benezene ring deceased activity. Compounds 11c and 14, the most potent compounds with IC50 values of 9.28 and 8.98 μM, respectively, would be promising candidates for further development of novel GSK-3β inhibitors.

Keywords: 4-Indolyl-5-phenyl(indolyl)-1, 2-dihydropyrazol-3-ones, Synthesis, GSK-3β inhibitors, metabolism, Staurosporine, biochemical properties, Mammalian GSK-3, pyrazolone ring, Val135

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Article Details

Year: 2012
Page: [780 - 788]
Pages: 9
DOI: 10.2174/157018012802652912
Price: $58