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Archives of Pharmacal Research

, Volume 29, Issue 11, pp 1006–1017 | Cite as

Comparison of some 3-(substituted-benzylidene)-1, 3-dihydro-indolin derivatives as ligands of tyrosine kinase based on binding mode studies and biological assay

  • Süreyya Ölgen
Articles Drug Development

Abstract

A series of 3-(substituted-benylidene)-1, 3-dihydro-indolin-2-one, 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione and 2, 2′-dithiobis 3-(substituted-benylidene)-1, 3-dihydro-indole derivatives was investigated as inhibitor of p60c-Src tyrosine kinase by performing receptor docking studies and inhibitory activity toward tyrosine phosphorylation. Some compounds were shown to be docked at the site, where the selective inhibitorPP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidine-4-yl-amine] was embedded at the enzyme active site. Evaluation of all compounds for the interactions with the parameters of lowest binding energy levels, capability of hydrogen bond formations and superimposibility on enzyme active site by docking studies, it can be assumed that 3-(substituted- benzylidene)-1, 3-dihydro-indolin-2-one and thione derivatives have better interaction with enzyme active site then 2, 2′-dithiobis 3-(substituted- benzylidene)-1, 3-dihydro indole derivatives. The test results for the inhibitory activity against tyrosine kinase by Elisa method revealed that 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione derivatives have more activity then 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one derivatives.

Key words

Protein tyrosine kinase p60c-Src N-Substituted indole derivatives Dock 4.0 

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Copyright information

© The Pharmaceutical Society of Korea 2006

Authors and Affiliations

  1. 1.Department of Pharmaceutical Chemistry, Faculty of PharmacyUniversity of AnkaraAnkaraTurkey

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