Title:Synthesis and Biological Study of Novel Indole-3-Imine-2-on Derivatives as Src Kinase and Glutathione S-Transferase Inhibitors
Volume: 10
Issue: 1
Author(s): Z. Kilic Kurt, D. Aydin, Y. G. Isgor, B. S. Isgor and S. Olgen
Affiliation:
Keywords:
Cancer, Src tyrosine kinase, Isatine, Glutathion-S-transferase, Drug resistance, Synthesis, tyrosine kinases, PTKs, xenobiotic lipophilic, SFK
Abstract: 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.
