Молимо вас користите овај идентификатор за цитирање или овај линк до ове ставке:
https://open.uns.ac.rs/handle/123456789/16306
Назив: | New A-homo lactam D-homo lactone androstane derivative: Synthesis and evaluation of cytotoxic and anti-inflammatory activities in vitro | Аутори: | Savić (Zaviš), Marina Škorić, Dušan Kuzminac, Ivana Dimitar Jakimov Kojić, Vesna Lucie Rarova Miroslav Strnad Evgenija Đurendić |
Кључне речи: | ADME analysis in silico Anti-angiogenic activity Anti-inflammatory activity Apoptotic morphology Cytotoxic activity Structural analysis | Датум издавања: | 2020 | Издавач: | Elsevier | Извор: | 10.1016/j.steroids.2020.108596 | Пројекат: | Synthesis, characterization and biological investigation of steroid derivatives and their molecular aggregates (Grant No. 172021) | Часопис: | Steroids | Сажетак: | 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. | URI: | https://open.uns.ac.rs/handle/123456789/16306 | ISSN: | 0039-128X | DOI: | 10.1016/j.steroids.2020.108596 | Права: | Attribution-NonCommercial-NoDerivs 3.0 United States |
Налази се у колекцијама: | PMF Publikacije/Publications |
Датотеке у овој ставци:
Датотека | Опис | Величина | Формат | |
---|---|---|---|---|
STE_108596_edit_report.pdf | Author's Post-prints | 994.91 kB | Adobe PDF | Погледајте |
Преглед/и станица
38
Протекла недеља
5
5
Протекли месец
0
0
проверено 03.05.2024.
Преузимање/а
63
проверено 03.05.2024.
Google ScholarTM
Проверите
Алт метрика
Ова ставка је лиценцирана под Креативна дозвола грађана