Evaluation of Indole Esters As Inhibitors of p60c-Src Receptor Tyrosine Kinase and Investigation of the Inhibition Using Receptor Docking Studies |
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| Authors: | Sureyya Olgen Eiichi Akaho Dogu Nebioglu |
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| Institution: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, Tandogan, 06100, Ankara, Turkeyolgen@pharmacy.ankara.edu.tr;3. Faculty of Pharmaceutical Sciences and High Technology Research Institute, Kobe Gakuin University, 518 Arise, Ikawadani-cho, Nishiku, 651-2180, Kobe, Japan;4. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, Tandogan, 06100, Ankara, Turkey |
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| Abstract: | Several indole esters were tested as inhibitors of tyrosine kinase p60c-Src. Compound (4) was found fairly active against the enzyme with IC50=1.34?μM. DOCK methodology was used to asses our inhibitors for their inhibitory potency against tyrosine kinase. The docking results showed that compounds (4), (25) and (26) were bound to the active site of the enzyme Lys 295 of p60c-Src tyrosine kinase. Both activity and docking studies showed a parallel result, with compound (4) having a better interaction with the enzyme active site and also greater activity than the other compounds, indicating a potential role as new lead inhibitor. |
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| Keywords: | Tyrosine kinase Inhibition Docking Indole esters Active site Enzyme interaction p60 |
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