| dc.contributor.author |
Christodoulou, MS |
en |
| dc.contributor.author |
Colombo, F |
en |
| dc.contributor.author |
Passarella, D |
en |
| dc.contributor.author |
Ieronimo, G |
en |
| dc.contributor.author |
Zuco, V |
en |
| dc.contributor.author |
De Cesare, M |
en |
| dc.contributor.author |
Zunino, F |
en |
| dc.date.accessioned |
2014-06-06T06:51:28Z |
|
| dc.date.available |
2014-06-06T06:51:28Z |
|
| dc.date.issued |
2011 |
en |
| dc.identifier.issn |
09680896 |
en |
| dc.identifier.uri |
http://dx.doi.org/10.1016/j.bmc.2011.01.039 |
en |
| dc.identifier.uri |
http://62.217.125.90/xmlui/handle/123456789/5533 |
|
| dc.subject |
Analogues of pifithrin-β |
en |
| dc.subject |
Benzothiazole derivatives |
en |
| dc.subject |
Biochemical and biological evaluation |
en |
| dc.subject |
Combined treatment with taxanes |
en |
| dc.subject |
p53 Inhibitors |
en |
| dc.subject |
Tetrahydrobenzothiazole derivatives |
en |
| dc.subject.other |
4 (5',6',7',8' tetrahydroimidazo[2,1 b]benzothiazol 2' yl)benzenamine |
en |
| dc.subject.other |
4 (5',6',7',8' tetrahydroimidazo[2,1 b]benzothiazol 2' yl)benzylamine |
en |
| dc.subject.other |
4 (imidazo[2,1 b]benzothiazol 2' yl)benzylamine |
en |
| dc.subject.other |
antineoplastic agent |
en |
| dc.subject.other |
benzothiazole derivative |
en |
| dc.subject.other |
imidazolo[2,1 b]benzothiazole derivative |
en |
| dc.subject.other |
p53 inhibitor |
en |
| dc.subject.other |
paclitaxel |
en |
| dc.subject.other |
protein p53 |
en |
| dc.subject.other |
tumor suppressor protein |
en |
| dc.subject.other |
unclassified drug |
en |
| dc.subject.other |
animal experiment |
en |
| dc.subject.other |
animal model |
en |
| dc.subject.other |
antineoplastic activity |
en |
| dc.subject.other |
article |
en |
| dc.subject.other |
cancer cell culture |
en |
| dc.subject.other |
carbon nuclear magnetic resonance |
en |
| dc.subject.other |
controlled study |
en |
| dc.subject.other |
drug efficacy |
en |
| dc.subject.other |
drug structure |
en |
| dc.subject.other |
drug synthesis |
en |
| dc.subject.other |
drug targeting |
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 |
osteosarcoma |
en |
| dc.subject.other |
ovary carcinoma |
en |
| dc.subject.other |
proton nuclear magnetic resonance |
en |
| dc.subject.other |
xenograft |
en |
| dc.subject.other |
Animals |
en |
| dc.subject.other |
Antineoplastic Agents |
en |
| dc.subject.other |
Benzothiazoles |
en |
| dc.subject.other |
Cell Line, Tumor |
en |
| dc.subject.other |
Disease Models, Animal |
en |
| dc.subject.other |
Female |
en |
| dc.subject.other |
Gene Expression Regulation |
en |
| dc.subject.other |
Humans |
en |
| dc.subject.other |
Inhibitory Concentration 50 |
en |
| dc.subject.other |
Ovarian Neoplasms |
en |
| dc.subject.other |
Toluene |
en |
| dc.subject.other |
Transplantation, Heterologous |
en |
| dc.subject.other |
Tumor Suppressor Protein p53 |
en |
| dc.title |
Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors |
en |
| heal.type |
journalArticle |
en |
| heal.identifier.primary |
10.1016/j.bmc.2011.01.039 |
en |
| heal.publicationDate |
2011 |
en |
| heal.abstract |
Since activation of p53 in response to cytotoxic stress may have proapoptotic or protective effects depending on the nature of the injury, inhibitors of p53 may have therapeutic interest as modulators of chemotherapy toxicity or efficacy. In an attempt to identify novel p53 inhibitors, a quality collection of compounds structurally related to pifithrin-β were designed and synthesized as potential inhibitors of p53. The biochemical and biological evaluations supported that compounds of the tetrahydrobenzothiazole series were inhibitors of the p53 transcriptional activity and were effective in enhancing paclitaxel-induced apoptosis. In contrast, in spite of the increased cytotoxic potency, selected compounds of the benzothiazole series were not able to modulate the transcriptional activity of p53, as indicated by lack of change of p21 expression. The therapeutic interest of the compounds of the former series in combination with taxanes was confirmed in a human tumor xenograft model. © 2011 Elsevier Ltd. All rights reserved. |
en |
| heal.journalName |
Bioorganic and Medicinal Chemistry |
en |
| dc.identifier.issue |
5 |
en |
| dc.identifier.volume |
19 |
en |
| dc.identifier.doi |
10.1016/j.bmc.2011.01.039 |
en |
| dc.identifier.spage |
1649 |
en |
| dc.identifier.epage |
1657 |
en |