Please use this identifier to cite or link to this item:
https://open.uns.ac.rs/handle/123456789/16306
DC Field | Value | Language |
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dc.contributor.author | Savić (Zaviš), Marina | en_US |
dc.contributor.author | Škorić, Dušan | en_US |
dc.contributor.author | Kuzminac, Ivana | en_US |
dc.contributor.author | Dimitar Jakimov | en_US |
dc.contributor.author | Kojić, Vesna | en_US |
dc.contributor.author | Lucie Rarova | en_US |
dc.contributor.author | Miroslav Strnad | en_US |
dc.contributor.author | Evgenija Đurendić | en_US |
dc.date.accessioned | 2020-06-10T16:31:36Z | - |
dc.date.available | 2020-06-10T16:31:36Z | - |
dc.date.issued | 2020 | - |
dc.identifier.citation | 10.1016/j.steroids.2020.108596 | en_US |
dc.identifier.issn | 0039-128X | en_US |
dc.identifier.uri | https://open.uns.ac.rs/handle/123456789/16306 | - |
dc.description.abstract | 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. | en_US |
dc.description.sponsorship | Ministry of Education, Science and Technological Development of the Republic of Serbia (Grant No. 172021) | en_US |
dc.description.sponsorship | Czech Science Foundation (Grant No. 19-01383S) | en_US |
dc.description.sponsorship | European Regional Development Fund - Project ENOCH (No. CZ.02.1.01/0.0/0.0/16_019/0000868) | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.relation | Synthesis, characterization and biological investigation of steroid derivatives and their molecular aggregates (Grant No. 172021) | en_US |
dc.relation.ispartof | Steroids | en_US |
dc.rights | Attribution-NonCommercial-NoDerivs 3.0 United States | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/3.0/us/ | * |
dc.subject | ADME analysis in silico Anti-angiogenic activity Anti-inflammatory activity Apoptotic morphology Cytotoxic activity Structural analysis | en_US |
dc.title | New A-homo lactam D-homo lactone androstane derivative: Synthesis and evaluation of cytotoxic and anti-inflammatory activities in vitro | en_US |
dc.type | Article | en_US |
dc.identifier.doi | 10.1016/j.steroids.2020.108596 | - |
dc.description.version | Published | en_US |
dc.relation.firstpage | 108596 | en_US |
dc.relation.volume | 157 | en_US |
item.fulltext | With Fulltext | - |
item.grantfulltext | open | - |
crisitem.author.dept | Departman za hemiju, biohemiju i zaštitu životne sredine | - |
crisitem.author.dept | Departman za hemiju, biohemiju i zaštitu životne sredine | - |
crisitem.author.dept | Departman za hemiju, biohemiju i zaštitu životne sredine | - |
crisitem.author.dept | Medicinski fakultet | - |
crisitem.author.orcid | 0000-0002-1019-3673 | - |
crisitem.author.orcid | 0000-0001-8045-3568 | - |
crisitem.author.parentorg | Prirodno-matematički fakultet | - |
crisitem.author.parentorg | Prirodno-matematički fakultet | - |
crisitem.author.parentorg | Prirodno-matematički fakultet | - |
crisitem.author.parentorg | Univerzitet u Novom Sadu | - |
Appears in Collections: | PMF Publikacije/Publications |
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File | Description | Size | Format | |
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STE_108596_edit_report.pdf | Author's Post-prints | 994.91 kB | Adobe PDF | View/Open |
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