Novel Derivatives of Benfluron and Dimefluron: Synthesis and Anticancer activity
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11150%2F15%3A10312630" target="_blank" >RIV/00216208:11150/15:10312630 - isvavai.cz</a>
Alternative codes found
RIV/00216208:11160/15:10312630
Result on the web
<a href="http://benthamscience.com/journals/letters-in-drug-design-and-discovery/volume/12/issue/10/page/787/" target="_blank" >http://benthamscience.com/journals/letters-in-drug-design-and-discovery/volume/12/issue/10/page/787/</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.2174/1570180812666150529204508" target="_blank" >10.2174/1570180812666150529204508</a>
Alternative languages
Result language
angličtina
Original language name
Novel Derivatives of Benfluron and Dimefluron: Synthesis and Anticancer activity
Original language description
In this study, we tried to improve the anticancer properties of two potential cytostatic agents based on benzo[c]fluorene, benfluron and dimefluron, by the synthesis of their C-7 derivatives. In the new derivatives, we observed the effect in Ehrlich tumour-bearing mice as well as in human MCF-7, BT-549 and MDA-MB-231 cells. All of the compounds tested showed a strong inhibitory effect in vitro. When tested in vivo, their systemic toxicity in vivo was promisingly low. Benfluron and its O-methyloxime as well as dimefluron and its oxime, thiosemicarbazone and hydrazone inhibited tumour growth in vivo. Only benfluron and hydrazone of dimefluron prolonged the survival. Proliferating cell nuclear antigen (PCNA) protein was decreased in tumours treated with benfluron and O-methyloxime of dimefluron in cancer tissue. Benfluron thiosemicarbazone increased the infiltration of tumour with T-lymphocytes. Taken together, all derivatives were more cytotoxic then their parent compounds, but not neces
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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Result continuities
Project
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Continuities
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Letters in Drug Design and Discovery
ISSN
1570-1808
e-ISSN
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Volume of the periodical
12
Issue of the periodical within the volume
10
Country of publishing house
AE - UNITED ARAB EMIRATES
Number of pages
15
Pages from-to
787-801
UT code for WoS article
000364520600001
EID of the result in the Scopus database
2-s2.0-84946557554