Novel Derivatives of Benfluron and Dimefluron: Synthesis and Anticancer activity

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/00216208:11160/15:10312630

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

Novel Derivatives of Benfluron and Dimefluron: Synthesis and Anticancer activity

Popis výsledku v původním jazyce

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

Název v anglickém jazyce

Novel Derivatives of Benfluron and Dimefluron: Synthesis and Anticancer activity

Popis výsledku anglicky

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

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

—

Projekt

—

Návaznosti

S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Letters in Drug Design and Discovery

ISSN

1570-1808

e-ISSN

—

Svazek periodika

12

Číslo periodika v rámci svazku

10

Stát vydavatele periodika

AE - Spojené arabské emiráty

Počet stran výsledku

15

Strana od-do

787-801

Kód UT WoS článku

000364520600001

EID výsledku v databázi Scopus

2-s2.0-84946557554