TY - JOUR
T1 - Antimalarial activity of 2,6-dibenzylidenecyclohexanone derivatives
AU - Eagon, Scott
AU - Hammill, Jared T.
AU - Fitzsimmons, Kasey
AU - Sienko, Natalie
AU - Nguyen, Brandon
AU - Law, Jarvis
AU - Manjunath, Aashrita
AU - Wilkinson, Steven P.
AU - Thompson, Kara
AU - Glidden, Julia Elizabeth
AU - Rice, Amy L.
AU - Falade, Mofolusho O.
AU - Kimball, Joshua J.
AU - DiBernardo, Celine
AU - Guy, R. Kiplin
N1 - Publisher Copyright:
© 2021 The Author(s)
PY - 2021/9/1
Y1 - 2021/9/1
N2 - Malaria remains one of the deadliest infectious diseases worldwide and continues to infect hundreds of millions of individuals each year. Here we report the discovery and derivatization of a series of 2,6-dibenzylidenecyclohexanones targeting the chloroquine-sensitive 3D7 strain of Plasmodium falciparum. While the initial lead compound displayed significant toxicity in a human cell proliferation assay, we were able to identify a derivative with no detectable toxicity and sub-micromolar potency.
AB - Malaria remains one of the deadliest infectious diseases worldwide and continues to infect hundreds of millions of individuals each year. Here we report the discovery and derivatization of a series of 2,6-dibenzylidenecyclohexanones targeting the chloroquine-sensitive 3D7 strain of Plasmodium falciparum. While the initial lead compound displayed significant toxicity in a human cell proliferation assay, we were able to identify a derivative with no detectable toxicity and sub-micromolar potency.
KW - 2,6-Dibenzylidenecyclohexanone
KW - Malaria
KW - Michael system
KW - Plasmodium falciparum
KW - Structure activity relationship
UR - http://www.scopus.com/inward/record.url?scp=85108955110&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85108955110&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2021.128216
DO - 10.1016/j.bmcl.2021.128216
M3 - Article
C2 - 34157390
AN - SCOPUS:85108955110
SN - 0960-894X
VL - 47
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
M1 - 128216
ER -