Title :

7-chloroquinoline-isatin conjugates: Antimalarial, antitubercular and cytotoxic evaluation

Author(s) :

Raj, Raghu [Auteur]
Biot, Christophe [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Carrère-Kremer, Séverine [Auteur]
Kremer, Laurent [Auteur]
Guerardel, Yann [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Gut, Jiri [Auteur]
Rosenthal, Philip J [Auteur]
Forge, Delphine [Auteur]
Kumar, Vipan [Auteur]

Journal title :

Chemical Biology & Drug Design

Abbreviated title :

Chem Biol Drug Des

Publication date :

2013-12-16

ISSN :

1747-0285

HAL domain(s) :

Chimie/Chimie théorique et/ou physique

English abstract : [en]

A series of twenty piperazine tethered 7-chloroquinoline-isatin hybrids have been synthesized via either direct nucleophilic substitution or Cu(Ι)Cl mediated Mannich reaction. These new conjugates were evaluated for their ...
Show more >A series of twenty piperazine tethered 7-chloroquinoline-isatin hybrids have been synthesized via either direct nucleophilic substitution or Cu(Ι)Cl mediated Mannich reaction. These new conjugates were evaluated for their antimalarial and anti-tubercular efficacy against a chloroquine resistant strain of Plasmodium falciparum and Mycobacterium tuberculosis, respectively, while the cytotoxic profiles were evaluated against 3T6 cell line, a permanent mouse embryonic fibroblast cell line. The most potent of the test compound with IC50 of 0.22 μM against W2 strain of P. falciparum and 31.62 μM against the embryonic fibroblast cell line (cytotoxicity) displayed a high selective index of 143.73. This article is protected by copyright. All rights reserved.Show less >

Language :

Anglais

Administrative institution(s) :

CNRS
Université de Lille

Collections :

• Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576

Research team(s) :

Chemical Glycobiology

Submission date :

2020-02-12T15:11:07Z