Please use this identifier to cite or link to this item:
https://open.uns.ac.rs/handle/123456789/16306
Title: | New A-homo lactam D-homo lactone androstane derivative: Synthesis and evaluation of cytotoxic and anti-inflammatory activities in vitro | Authors: | Savić (Zaviš), Marina Škorić, Dušan Kuzminac, Ivana Dimitar Jakimov Kojić, Vesna Lucie Rarova Miroslav Strnad Evgenija Đurendić |
Keywords: | ADME analysis in silico Anti-angiogenic activity Anti-inflammatory activity Apoptotic morphology Cytotoxic activity Structural analysis | Issue Date: | 2020 | Publisher: | Elsevier | Source: | 10.1016/j.steroids.2020.108596 | Project: | Synthesis, characterization and biological investigation of steroid derivatives and their molecular aggregates (Grant No. 172021) | Journal: | Steroids | 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. | URI: | https://open.uns.ac.rs/handle/123456789/16306 | ISSN: | 0039-128X | DOI: | 10.1016/j.steroids.2020.108596 | Rights: | Attribution-NonCommercial-NoDerivs 3.0 United States |
Appears in Collections: | PMF Publikacije/Publications |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
STE_108596_edit_report.pdf | Author's Post-prints | 994.91 kB | Adobe PDF | View/Open |
Page view(s)
41
Last Week
5
5
Last month
0
0
checked on May 10, 2024
Download(s)
66
checked on May 10, 2024
Google ScholarTM
Check
Altmetric
This item is licensed under a Creative Commons License