New A-homo lactam D-homo lactone androstane derivative: Synthesis and evaluation of cytotoxic and anti-inflammatory activities in vitro
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389030%3A_____%2F20%3A00531060" target="_blank" >RIV/61389030:_____/20:00531060 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15310/20:73604861
Result on the web
<a href="http://doi.org/10.1016/j.steroids.2020.108596" target="_blank" >http://doi.org/10.1016/j.steroids.2020.108596</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.steroids.2020.108596" target="_blank" >10.1016/j.steroids.2020.108596</a>
Alternative languages
Result language
angličtina
Original language name
New A-homo lactam D-homo lactone androstane derivative: Synthesis and evaluation of cytotoxic and anti-inflammatory activities in vitro
Original language description
This paper describes the synthesis of a new A-homo lactam D-homo lactone androstane derivative from dehydroepiandrosterone. To evaluate the impact of the introduction of nitrogen in the parental scaffold on biological activity, a new androstane enamide-type lactam derivative was prepared and characterized. The new compound as well as starting compounds were screened for cytotoxic, anti-angiogenic and anti-inflammatory activities using several human cancer cell lines (MCF-7, MDA-MB-231, PC3, CEM, G-361, HeLa), endothelial (HUVEC) and non-tumour (MRC-5 and BJ) cell lines. Strong cytotoxic and anti-inflammatory activity with a broad therapeutical window was demonstrated by the A-homo lactam D-homo lactone androstane derivative. The induction of apoptosis in treated PC3 cultures was confirmed using apoptotic morphology screening and a fluorescent double-staining method. New A-homo lactam D-homo lactone androstane derivative induced apoptosis more than the tested reference compounds, Formestane and Doxorubicin. An in silico ADME analysis showed that the compounds possess drug-like properties.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2020
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Steroids
ISSN
0039-128X
e-ISSN
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Volume of the periodical
157
Issue of the periodical within the volume
MAY
Country of publishing house
US - UNITED STATES
Number of pages
8
Pages from-to
108596
UT code for WoS article
000527364000002
EID of the result in the Scopus database
2-s2.0-85079874274