Abstract
A major effort in Alzheimers disease therapeutic development has targeted Aβ and downstream events. We have synthesized a small library of tricyclic pyrone compounds. Their protective action in MC65 cells and inhibition of ACAT along with the upregulation of cholesterol transporter gene were investigated. Five active compounds exhibited potencies in the nanomolar ranges. The multiple effects of the compounds on Aβ and cellular cholesterol pathways could be potential mechanisms underlying the protective effects in vivo.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 8969-8973 |
| Number of pages | 5 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 55 |
| Issue number | 20 |
| DOIs | |
| State | Published - Oct 25 2012 |
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ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
Cite this
Inhibition of Acyl-CoA : Cholesterol acyltransferase (ACAT), overexpression of cholesterol transporter gene, and protection of amyloid β (Aβ) oligomers-induced neuronal cell death by tricyclic pyrone molecules. / Pokhrel, Laxman; Maezawa, Izumi; Nguyen, Thi D T; Chang, Kyeong Ok; Jin, Lee-Way; Hua, Duy H.
In: Journal of Medicinal Chemistry, Vol. 55, No. 20, 25.10.2012, p. 8969-8973.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Inhibition of Acyl-CoA
T2 - Cholesterol acyltransferase (ACAT), overexpression of cholesterol transporter gene, and protection of amyloid β (Aβ) oligomers-induced neuronal cell death by tricyclic pyrone molecules
AU - Pokhrel, Laxman
AU - Maezawa, Izumi
AU - Nguyen, Thi D T
AU - Chang, Kyeong Ok
AU - Jin, Lee-Way
AU - Hua, Duy H.
PY - 2012/10/25
Y1 - 2012/10/25
N2 - A major effort in Alzheimers disease therapeutic development has targeted Aβ and downstream events. We have synthesized a small library of tricyclic pyrone compounds. Their protective action in MC65 cells and inhibition of ACAT along with the upregulation of cholesterol transporter gene were investigated. Five active compounds exhibited potencies in the nanomolar ranges. The multiple effects of the compounds on Aβ and cellular cholesterol pathways could be potential mechanisms underlying the protective effects in vivo.
AB - A major effort in Alzheimers disease therapeutic development has targeted Aβ and downstream events. We have synthesized a small library of tricyclic pyrone compounds. Their protective action in MC65 cells and inhibition of ACAT along with the upregulation of cholesterol transporter gene were investigated. Five active compounds exhibited potencies in the nanomolar ranges. The multiple effects of the compounds on Aβ and cellular cholesterol pathways could be potential mechanisms underlying the protective effects in vivo.
UR - http://www.scopus.com/inward/record.url?scp=84867786264&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84867786264&partnerID=8YFLogxK
U2 - 10.1021/jm3012189
DO - 10.1021/jm3012189
M3 - Article
C2 - 23025824
AN - SCOPUS:84867786264
VL - 55
SP - 8969
EP - 8973
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 20
ER -