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Synthèse d'analogues de 7-chloroquinoléinyl-4-alkylidènes et benzoates avec une potentielle activité cytotoxique-antitumorale et antimalarique

Abstract : This thesis work describes the chemical synthesis of a series of 7-chloroquinoline derivatives substituted at their position 4. These newcompounds resulted from the introduction of thio- and amino-alcohol motifs,followed by a coupling reaction with diversely substituted benzoic acidsorindanones. The sulfur-containing compounds were also oxidized intosulfones. One hundred seven (107) compounds were thus synthesized, andthen carefully purified and fully characterized in the aim of their biologicalevaluation as cytotoxic-antitumoral and antimalarial agents. Among the mainresults: i) the greater the oxidation state of sulfur, the greater the cytotoxic effecton the cell lines studied, ii) the lenght of the alkyl chain and the substitutionpattern are of importance, and iii) no improvement of the antimalarial activitywas observed with classical bioisosterism based on replacement of nitrogen bysulfur in position 4 of the quinolinic ring.
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https://tel.archives-ouvertes.fr/tel-01827247
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Joyce Elena Gutierrez Rivas. Synthèse d'analogues de 7-chloroquinoléinyl-4-alkylidènes et benzoates avec une potentielle activité cytotoxique-antitumorale et antimalarique. Chimie organique. Université de Bordeaux; Universidad central de Venezuela, 2017. Français. ⟨NNT : 2017BORD0956⟩. ⟨tel-01827247⟩

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