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Conception et Synthèse d'Hétérocycles Azotés Polyfonctionnalisés Biologiquement Actifs: Des Acridines aux Quinazolines

Abstract : This work concerns the design of aminoacridine and quinazoline derivatives. In a first part, we have prepared ortho-hydroxymethyl aminoacridine derivatives. To synthesize these derivatives we designed an effective and general strategy involving the preparation of a key- intermediate that can be functionnalised. We therefore prepared derivatives substituted by a guanidine moiety. We also prepared a derivative substituted with an iodine atom to study its cellular distribution by ionic microscopy (SIMS). The biological properties (IC50 and cellular distribution) of these new compounds have been investigated on various cancer cells and the data point out the interest of this new family of aminoacridine as anticancer dyes.
In a second part we designed a new methodology of synthesis of 2-alkylamino-4(3H)-quinazolinones. We have prepared various derivatives containing a quinazolinone moiety from aromatic and heterocyclic amines. Some of these derivatives were given for preliminary biological studies (IC50, DNA-quadruplex ligand) and the first results are very encouraging.
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https://tel.archives-ouvertes.fr/tel-00221136
Contributor : Walid Zeghida <>
Submitted on : Thursday, January 31, 2008 - 12:40:01 AM
Last modification on : Friday, November 6, 2020 - 4:11:28 AM
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  • HAL Id : tel-00221136, version 2

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Walid Zeghida. Conception et Synthèse d'Hétérocycles Azotés Polyfonctionnalisés Biologiquement Actifs: Des Acridines aux Quinazolines. Autre. Université Joseph-Fourier - Grenoble I, 2007. Français. ⟨tel-00221136v2⟩

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