50 0

Synthesis and anticancer activity of 4-aza-daurinol derivatives

Title
Synthesis and anticancer activity of 4-aza-daurinol derivatives
Author
이주연
Keywords
Daurinol; Anticancer; Bioisosteric; Aryltetrahydronaphthalene; Structure-activity relationship; TAIWANIN-C; ARYLNAPHTHALENE LACTONES; ARYLPROPIOLATE ESTERS; JUSTICIDIN-E; DRUG DESIGN; INHIBITOR; DAURINOL; LIGNANS; BIOISOSTERISM; ETOPOSIDE
Issue Date
2015-11
Publisher
PHARMACEUTICAL SOC KOREA
Citation
ARCHIVES OF PHARMACAL RESEARCH, v. 38, No. 11, Page. 1975-1982
Abstract
Daurinol, a natural aryl naphthalene lactone, has been reported to have antiproliferative activity against various cell lines, and has also been shown to be efficacious in an in vivo xenograft mouse model. In this study, we tried to discover a new scaffold that enables both rapid structure-activity relationship study of daurinol and scalable synthesis of active compounds. 4-Aza-daurinol, a bioisosterism-based scaffold of daurinol, was designed and 17 analogues were synthesized and evaluated against five representative cancer cell lines. Among them, the 2,3-dihydrobenzo[b][1,4]dioxinyl derivative was found to be the most potent and showed similar activity and tendency as daurinol.
URI
https://link.springer.com/article/10.1007/s12272-015-0619-2http://hdl.handle.net/20.500.11754/40890
ISSN
0253-6269; 1976-3786
DOI
10.1007/s12272-015-0619-2
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE