| dc.contributor.author |
Christodoulou, MS |
en |
| dc.contributor.author |
Fokialakis, N |
en |
| dc.contributor.author |
Passarella, D |
en |
| dc.contributor.author |
Garcia-Argaez, AN |
en |
| dc.contributor.author |
Gia, OM |
en |
| dc.contributor.author |
Pongratz, I |
en |
| dc.contributor.author |
Dalla Via, L |
en |
| dc.contributor.author |
Haroutounian, SA |
en |
| dc.date.accessioned |
2014-06-06T06:52:51Z |
|
| dc.date.available |
2014-06-06T06:52:51Z |
|
| dc.date.issued |
2013 |
en |
| dc.identifier.issn |
09680896 |
en |
| dc.identifier.uri |
http://dx.doi.org/10.1016/j.bmc.2013.05.012 |
en |
| dc.identifier.uri |
http://62.217.125.90/xmlui/handle/123456789/6214 |
|
| dc.subject |
Biphasic mesothelioma (MSTO-211H) |
en |
| dc.subject |
Breast cancer (MCF-7) |
en |
| dc.subject |
Cervix adenocarcinoma (HeLa) |
en |
| dc.subject |
Tamoxifen derivatives |
en |
| dc.subject |
Topoisomerase |
en |
| dc.subject.other |
DNA topoisomerase |
en |
| dc.subject.other |
DNA topoisomerase (ATP hydrolysing) |
en |
| dc.subject.other |
estradiol |
en |
| dc.subject.other |
hydroxytamoxifen |
en |
| dc.subject.other |
n [4 [1',2' bis(4'',4''' hydroxyphenyl)but 1' enyl]phenyl] 1,1 diethylurea |
en |
| dc.subject.other |
n [4 [1',2' bis(4'',4''' hydroxyphenyl)but 1' enyl]phenyl] 1,1 dimethylurea |
en |
| dc.subject.other |
n [4 [1',2' bis(4'',4''' hydroxyphenyl)but 1' enyl]phenyl]hexanamide |
en |
| dc.subject.other |
n [4 [1',2' bis(4'',4''' hydroxyphenyl)but 1' enyl]phenyl]isobutyramide |
en |
| dc.subject.other |
n [4 [1',2' bis(4'',4''' hydroxyphenyl)but 1' enyl]phenyl]piperidine 1 carboxamide |
en |
| dc.subject.other |
n [4 [1',2' bis(4'',4''' hydroxyphenyl)but 1' enyl]phenyl]propionamide |
en |
| dc.subject.other |
n [4 [1',2' bis(4'',4''' hydroxyphenyl)but 1' enyl]phenyl]pyrrolidine 1 carboxamide |
en |
| dc.subject.other |
tamoxifen |
en |
| dc.subject.other |
tamoxifen derivative |
en |
| dc.subject.other |
unclassified drug |
en |
| dc.subject.other |
animal cell |
en |
| dc.subject.other |
antineoplastic activity |
en |
| dc.subject.other |
antiproliferative activity |
en |
| dc.subject.other |
article |
en |
| dc.subject.other |
cancer cell culture |
en |
| dc.subject.other |
cell strain MCF 7 |
en |
| dc.subject.other |
concentration response |
en |
| dc.subject.other |
controlled study |
en |
| dc.subject.other |
drug design |
en |
| dc.subject.other |
drug mechanism |
en |
| dc.subject.other |
drug screening |
en |
| dc.subject.other |
drug structure |
en |
| dc.subject.other |
drug synthesis |
en |
| dc.subject.other |
enzyme activity |
en |
| dc.subject.other |
enzyme inhibition |
en |
| dc.subject.other |
female |
en |
| dc.subject.other |
HeLa cell |
en |
| dc.subject.other |
human |
en |
| dc.subject.other |
human cell |
en |
| dc.subject.other |
mouse |
en |
| dc.subject.other |
nonhuman |
en |
| dc.subject.other |
Antineoplastic Agents |
en |
| dc.subject.other |
Breast Neoplasms |
en |
| dc.subject.other |
Cell Line, Tumor |
en |
| dc.subject.other |
Cell Proliferation |
en |
| dc.subject.other |
Endometrial Neoplasms |
en |
| dc.subject.other |
Female |
en |
| dc.subject.other |
Humans |
en |
| dc.subject.other |
Molecular Structure |
en |
| dc.subject.other |
Receptors, Estrogen |
en |
| dc.subject.other |
Tamoxifen |
en |
| dc.title |
Synthesis and biological evaluation of novel tamoxifen analogues |
en |
| heal.type |
journalArticle |
en |
| heal.identifier.primary |
10.1016/j.bmc.2013.05.012 |
en |
| heal.publicationDate |
2013 |
en |
| heal.abstract |
A collection of compounds, structurally related to the anticancer drug tamoxifen, used in breast cancer therapy, were designed and synthesized as potential anticancer agents. McMurry coupling reaction was used as the key synthetic step in the preparation of these analogues and the structural assignment of E, Z isomers was determined on the basis of 2D-NOESY experiments. The compounds were evaluated for their antiproliferative activity on breast cancer (MCF-7), cervix adenocarcinoma (HeLa) and biphasic mesothelioma (MSTO-211H) human tumor cell lines. The estrogen like properties of the novel compounds were compared with those of the untreated controls using an estrogen responsive element-based (ERE) luciferase reporter assay and compared to 17β-estradiol (E2). Finally, with the aim to correlate the antiproliferative activity with an intracellular target(s), the effect on relaxation activity of DNA topoisomerases I and II was assayed. © 2013 Elsevier Ltd. All rights reserved. |
en |
| heal.journalName |
Bioorganic and Medicinal Chemistry |
en |
| dc.identifier.issue |
14 |
en |
| dc.identifier.volume |
21 |
en |
| dc.identifier.doi |
10.1016/j.bmc.2013.05.012 |
en |
| dc.identifier.spage |
4120 |
en |
| dc.identifier.epage |
4131 |
en |