Elsevier
Tetrahedron
,  volume 92 ,  pages 132248

Structural modification and biological activity studies of tagitinin C and its derivatives

Thi Huong Au 1
, 
Charles Skarbek 1
, 
Stéphanie Pethe 1
, 
Raphaël Labruère 1
, 
Jean-Pierre Baltaze 1
, 
Thi Hong Nguyen 2
, 
Vu Thi Bich 2
, 
Giang Vo Thanh 1
1
 
2
 
National Key Laboratory for Petrochemical and Refinery Technologies, Hanoi, Viet Nam | 
Publication type: Journal Article
Publication date: 2021-07-01
Elsevier
scimago Q3
wos Q2
SJR: 0.426
CiteScore: 4.1
Impact factor: 2.2
ISSN: 00404020, 14645416
Organic Chemistry
Drug Discovery
Biochemistry
Abstract
The Michael addition reaction of amines, phosphonates and thiols to Tagitinin C containing in its structure an α-methylene-γ-lactone motif and two α,β-unsaturated ketone systems has been described. 27 Tagitinin C derivatives were synthesized and isolated in good to excellent yield (up to 99% yield) under mild reaction conditions. The biological activity of Tagitinin C and its derivatives were evaluated against three human cancer cell lines (breast human cancer cells MCF-7, breast human cancer cells multi-resistant to drugs MCF7-MDR, pancreas cancer cells MiaPaCa-2) and on normal cell line (HEK-293) as control. We showed that the biological activity of Tagitinin C derivatives is remained. These compounds presented an enhanced water solubility that could improve their bioavailability and their pharmacological profiles.
Found 
Found 

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GOST Copy
Au T. H. et al. Structural modification and biological activity studies of tagitinin C and its derivatives // Tetrahedron. 2021. Vol. 92. p. 132248.
GOST all authors (up to 50) Copy
Au T. H., Skarbek C., Pethe S., Labruère R., Baltaze J., Nguyen T. H., Thi Bich V., Vo Thanh G. Structural modification and biological activity studies of tagitinin C and its derivatives // Tetrahedron. 2021. Vol. 92. p. 132248.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.tet.2021.132248
UR - https://doi.org/10.1016/j.tet.2021.132248
TI - Structural modification and biological activity studies of tagitinin C and its derivatives
T2 - Tetrahedron
AU - Au, Thi Huong
AU - Skarbek, Charles
AU - Pethe, Stéphanie
AU - Labruère, Raphaël
AU - Baltaze, Jean-Pierre
AU - Nguyen, Thi Hong
AU - Thi Bich, Vu
AU - Vo Thanh, Giang
PY - 2021
DA - 2021/07/01
PB - Elsevier
SP - 132248
VL - 92
SN - 0040-4020
SN - 1464-5416
ER -
BibTex
Cite this
BibTex (up to 50 authors) Copy
@article{2021_Au,
author = {Thi Huong Au and Charles Skarbek and Stéphanie Pethe and Raphaël Labruère and Jean-Pierre Baltaze and Thi Hong Nguyen and Vu Thi Bich and Giang Vo Thanh},
title = {Structural modification and biological activity studies of tagitinin C and its derivatives},
journal = {Tetrahedron},
year = {2021},
volume = {92},
publisher = {Elsevier},
month = {jul},
url = {https://doi.org/10.1016/j.tet.2021.132248},
pages = {132248},
doi = {10.1016/j.tet.2021.132248}
}