Diversity-oriented synthesis yields novel multistage antimalarial inhibitors

Nature

Volumn 538, Issue 7625, 2016, Pages 344-349

  Kato, Nobutaka ^a   Comer, Eamon ^a   Sakata Kato, Tomoyo ^b   Sharma, Arvind ^c   Sharma, Manmohan ^c   Maetani, Micah ^a,d   Bastien, Jessica ^a   Brancucci, Nicolas M ^b   Bittker, Joshua A ^a   Corey, Victoria ^e   Clarke, David ^b   Derbyshire, Emily R ^a,f,g   Dornan, Gillian L ^h   Duffy, Sandra ⁱ   Eckley, Sean ^j   Itoe, Maurice A ^b   Koolen, Karin M J ^k   Lewis, Timothy A ^a   Lui, Ping S ^b   Lukens, Amanda K ^a,b   Lund, Emily ^b   March, Sandra ^a,l   Meibalan, Elamaran ^b   Meier, Bennett C ^a,d   McPhail, Jacob A ^h   Mitasev, Branko ^j   Moss, Eli L ^a   Sayes, Morgane ^a   Van Gessel, Yvonne ^j   Wawer, Mathias J ^a   Yoshinaga, Takashi ^m   Zeeman, Anne Marie ⁿ   Avery, Vicky M ⁱ   Bhatia, Sangeeta N ^a,l   Burke, John E ^h   Catteruccia, Flaminia ^b   Clardy, Jon C ^a,f   Clemons, Paul A ^a   Dechering, Koen J ^k   Duvall, Jeremy R ^a   Foley, Michael A ^a   Gusovsky, Fabian ^j   Kocken, Clemens H M ⁿ   Marti, Matthias ^b   Morningstar, Marshall L ^a   Munoz, Benito ^a   Neafsey, Daniel E ^a   Sharma, Amit ^c   Winzeler, Elizabeth A ^e   Wirth, Dyann F ^a,b   Scherer, Christina A ^a   Schreiber, Stuart L ^a,d   more..

^a BROAD INSTITUTE OF MIT AND HARVARD   (United States)

^b HARVARD SCHOOL OF PUBLIC HEALTH   (United States)

^c INTERNATIONAL CENTRE FOR GENETIC ENGINEERING AND BIOTECHNOLOGY   (Italy)

^d HARVARD UNIVERSITY   (United States)

^e UNIVERSITY OF CALIFORNIA   (United States)

^f HARVARD MEDICAL SCHOOL   (United States)

^g DUKE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^h UNIVERSITY OF VICTORIA   (Canada)

ⁱ GRIFFITH UNIVERSITY   (Australia)

^j EISAI INC   (United States)

^k Current affiliation: TropIQ Health Sciences   (Netherlands)

^l Department of Electrical Engineering and Computer Science   (United States)

^m EISAI CO LTD   (Japan)

ⁿ Biochemical Primate Research Centre   (Netherlands)

more..

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; ATOVAQUONE; AZETIDINE DERIVATIVE; BRD 0026; BRD 0185; BRD 1095; BRD 2132; BRD 2936; BRD 3316; BRD 3444; BRD 4716; BRD 4873; BRD 5349; BRD 5774; BRD 6479; BRD 73842; BRD 7539; BRD 7929; BRD 8260; BRD 8493; BRD 8805; BRD 9185; BRD 9599; CYTOCHROME; GENOMIC DNA; PHENYLALANINE TRANSFER RNA LIGASE; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG; AZABICYCLO DERIVATIVE; BRD7929; CARBANILAMIDE DERIVATIVE;

ANTIMALARIAL AGENT; DISEASE TRANSMISSION; DISEASE TREATMENT; DRUG; ENZYME ACTIVITY; INHIBITOR; PARASITE; RODENT;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BIOLUMINESCENCE; CONTROLLED STUDY; CRYSTAL STRUCTURE; CYTOTOXICITY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SAFETY; DRUG SCREENING; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; EC50; ERYTHROCYTE; FEMALE; GAMETOCYTE; HEPG2 CELL LINE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IN VITRO STUDY; LIVER CELL; LIVER MICROSOME; MALARIA FALCIPARUM; METABOLIC STABILITY; MOUSE; NONHUMAN; PARASITEMIA; PHOTOTOXICITY; PILOT STUDY; PLASMA PROTEIN BINDING; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; RODENT MALARIA; SINGLE DRUG DOSE; SPOROZOITE; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; VOLUME OF DISTRIBUTION; VOLUME OF DISTRIBUTION AT STEADY-STATE; ANIMAL; ANTAGONISTS AND INHIBITORS; CYTOLOGY; CYTOSOL; DISEASE MODEL; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYMOLOGY; GROWTH, DEVELOPMENT AND AGING; LIFE CYCLE STAGE; LIVER; MALARIA, FALCIPARUM; MALE; PARASITOLOGY; RHESUS MONKEY; SAFETY; SYNTHESIS; TRANSMISSION;

MUS;

ANIMALS; ANTIMALARIALS; AZABICYCLO COMPOUNDS; AZETIDINES; CYTOSOL; DISEASE MODELS, ANIMAL; DRUG DISCOVERY; FEMALE; LIFE CYCLE STAGES; LIVER; MACACA MULATTA; MALARIA, FALCIPARUM; MALE; MICE; PHENYLALANINE-TRNA LIGASE; PHENYLUREA COMPOUNDS; PLASMODIUM FALCIPARUM; SAFETY;

EID: 84992417810     PISSN: 00280836     EISSN: 14764687     Source Type: Journal    
DOI: 10.1038/nature19804     Document Type: Article

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