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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Biological Study of Novel Indole-3-Imine-2-on Derivatives as Src Kinase and Glutathione S-Transferase Inhibitors

Author(s): Z. Kilic Kurt, D. Aydin, Y. G. Isgor, B. S. Isgor and S. Olgen

Volume 10 , Issue 1 , 2013

Page: [19 - 26] Pages: 8

DOI: 10.2174/1570180811309010019

Price: $65


The aim of this study is to design and synthesize novel dual inhibitors of Src protein tyrosine kinase (PTK) and Glutathione S-transferases (GSTs), as a potential drug lead with therapeutic efficacy on cancer and immune disorders. The biological activity profiling of small molecule inhibitors via miniaturized biochemical techniques compatible with medium throughput screening and focused screening methodologies were performed. To determining the effects of small molecule inhibitors on Src kinase and Phase II detoxification enzyme GST isozymes in liver homogenates used to verify their roles in drug resistance mechanism for cancer chemotherapeutics. In this study, 14 indole-3-imine-2-on and N-benzyl indole-3-imine-2-on derivatives were synthesized for dual activities against Src and GST. The chemical structures and purities of compounds were verified by IR, 1H NMR, MASS spectroscopy, and elemental analysis. The compounds 2, 3 and 9 are found slightly active against both enzyme Src and GST.

Keywords: Cancer, Src tyrosine kinase, Isatine, Glutathion-S-transferase, Drug resistance, Synthesis, tyrosine kinases, PTKs, xenobiotic lipophilic, SFK

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