Synthesis of compounds having a oxindole motif, potentials inhibitors of the fibroblastes growth factor(FGFR1)

The growth factors receptors are overexpressed in a great number of cancers and play a very important role in cell proliferation. We were interested in the ATP competitive inhibitors of the tyrosine kinase domain of the growth factors receptors, more particularly of the FGFR1. This receptor constitutes a privileged target for the development of new anti-cancer agents. The first part of this work is a bibliographical study on growth factors receptors. The principal families of growth factors receptors inhibitors are detailed. To design a new model of inhibitors of the FGFR1 tyrosine kinase activity, we prepared three families of compounds. The synthesis of these compounds is reported in the second part. The third part, presents a study of docking and energy minimization by molecular mechanics on the complexes of some of the synthesized compounds in the FGFR1 ATP-site. In the fourth part, the cytoxicity on various tumor and healthy cell lines and the inhibitory activity on various kinases of the new products prepared during this work are detailed.

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Field Value
Source https://theses.hal.science/tel-00683658
Author Sassatelli, Mathieu
Maintainer CCSD
Last Updated May 23, 2026, 05:09 (UTC)
Created May 23, 2026, 05:09 (UTC)
Identifier NNT: 2005CLF21609
Language fr
Rights https://about.hal.science/hal-authorisation-v1/
contributor Institut de Chimie de Clermont-Ferrand (ICCF) ; Université Blaise Pascal - Clermont-Ferrand 2 (UBP)-SIGMA Clermont (SIGMA Clermont)-Institut de Chimie - CNRS Chimie (INC-CNRS)-Centre National de la Recherche Scientifique (CNRS)
creator Sassatelli, Mathieu
date 2005-11-08T00:00:00
harvest_object_id 783fd596-53aa-4995-9737-c67c795e3cdc
harvest_source_id 3374d638-d20b-4672-ba96-a23232d55657
harvest_source_title test moissonnage SELUNE
metadata_modified 2024-04-11T00:00:00
set_spec type:THESE