Enone- and chalcone-chloroquinoline hybrid analogues: In silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies

Journal of Medicinal Chemistry

Volumn 54, Issue 10, 2011, Pages 3637-3649

  Guantai, Eric M ^a   Ncokazi, Kanyile ^a   Egan, Timothy J ^a   Gut, Jiri ^b   Rosenthal, Philip J ^b   Bhampidipati, Ravi ^c   Kopinathan, Anitha ^c   Smith, Peter J ^a   Chibale, Kelly ^a  

^a UNIVERSITY OF CAPE TOWN   (South Africa)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c MONASH UNIVERSITY   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

3 [3 [4 (7 CHLOROQUINOLIN 4 YL)PIPERAZIN 1 YLMETHYL] 4 HYDROXY 5 METHOXYPHENYL] 1 (2,4 DIMETHOXYPHENYL)PROPENONE; 3 [3 [4 (7 CHLOROQUINOLIN 4 YL)PIPERAZIN 1 YLMETHYL] 4 HYDROXYPHENYL] 1 (2,4 DIMETHOXYPHENYL)PROPENONE; CHALCONE DERIVATIVE; CHLOROQUINE; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTIMALARIAL ACTIVITY; ARTICLE; CIS TRANS ISOMERISM; DRUG DESIGN; DRUG GLUCURONIDATION; DRUG MECHANISM; DRUG METABOLISM; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MOUSE; NONHUMAN;

ANIMALS; ANTIMALARIALS; ANTIPARASITIC AGENTS; CACO-2 CELLS; CHALCONE; CHEMISTRY, PHARMACEUTICAL; COMPUTATIONAL BIOLOGY; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; HYDROGEN-ION CONCENTRATION; INHIBITORY CONCENTRATION 50; LIVER; PERMEABILITY; QUINOLINES;

EID: 79957779087     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200149e     Document Type: Article

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