Evidence map›Paper›PMID 36362320›Full record

ArticleInternational journal of molecular sciences2022

Synthesis and Biological Evaluation of New Isoxazolyl Steroids as Anti-Prostate Cancer Agents.

Anton S Rudovich, Miroslav Peřina, Anastasiya V Krech, Maria Y Novozhilova, Anastasia M Tumilovich, Tatyana V Shkel, Irina P Grabovec, Miroslav Kvasnica, Lukáš Mada, Maria G Zavialova and 4 more

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.1field-weighted citation impact, top 20% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed, 6 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

14 authors at 4 institutions in 3 countries.

Anton S RudovichInstitute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich Str., 5/2, 220141 Minsk, Belarus.ORCID 0000-0003-3521-727X
Miroslav PeřinaDepartment of Experimental Biology, Faculty of Science, Palacký University Olomouc, Šlechtitelů 27, 78371 Olomouc, Czech Republic.
Anastasiya V KrechInstitute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich Str., 5/2, 220141 Minsk, Belarus.
Maria Y NovozhilovaInstitute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich Str., 5/2, 220141 Minsk, Belarus.
Anastasia M TumilovichInstitute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich Str., 5/2, 220141 Minsk, Belarus.
Tatyana V ShkelInstitute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich Str., 5/2, 220141 Minsk, Belarus.
Irina P GrabovecInstitute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich Str., 5/2, 220141 Minsk, Belarus.
Miroslav KvasnicaDepartment of Experimental Biology, Faculty of Science, Palacký University Olomouc, Šlechtitelů 27, 78371 Olomouc, Czech Republic.ORCID 0000-0002-0597-3261
Lukáš MadaDepartment of Experimental Biology, Faculty of Science, Palacký University Olomouc, Šlechtitelů 27, 78371 Olomouc, Czech Republic.ORCID 0000-0002-2610-0515
Maria G ZavialovaInstitute of Biomedical Chemistry, 10 Building 8, Pogodinskaya Str., 119121 Moscow, Russia.ORCID 0000-0003-0761-2299
Arif R MekhtievInstitute of Biomedical Chemistry, 10 Building 8, Pogodinskaya Str., 119121 Moscow, Russia.
Radek JordaDepartment of Experimental Biology, Faculty of Science, Palacký University Olomouc, Šlechtitelů 27, 78371 Olomouc, Czech Republic.ORCID 0000-0002-4905-7126
Vladimir N ZhabinskiiInstitute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich Str., 5/2, 220141 Minsk, Belarus.ORCID 0000-0001-8591-2794
Vladimir A KhripachInstitute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich Str., 5/2, 220141 Minsk, Belarus.ORCID 0000-0002-3850-9860
National Academy of Sciences of Belarus · BYPalacký University Olomouc · CZInstitute of Biomedical Chemistry · RUInstitute of Molecular and Translational Medicine · CZ

Funding

Belarusian Foundation for Fundamental Research X22Mldg-001European Union LX22NPO5102Palacký University, Olomouc IGA_PrF_2022_007
6 · The paper itself

Abstract

Steroids with a nitrogen-containing heterocycle in the side chain are known as effective inhibitors of androgen signaling and/or testosterone biosynthesis, thus showing beneficial effects for the treatment of prostate cancer. In this work, a series of 3β-hydroxy-5-ene steroids, containing an isoxazole fragment in their side chain, was synthesized. The key steps included the preparation of Weinreb amide, its conversion to acetylenic ketones, and the 1,2- or 1,4-addition of hydroxylamine, depending on the solvent used. The biological activity of the obtained compounds was studied in a number of tests, including their effects on 17α-hydroxylase and 17,20-lyase activity of human CYP17A1 and the ability of selected compounds to affect the downstream androgen receptor signaling. Three derivatives diminished the transcriptional activity of androgen receptor and displayed reasonable antiproliferative activity. The candidate compound,

Indexed as

Antineoplastic AgentsProstatic NeoplasmsCell Line, TumorHumansMaleMolecular Docking SimulationReceptors, AndrogenSteroid 17-alpha-HydroxylaseSteroidsAntineoplastic AgentsReceptors, AndrogenSteroid 17-alpha-HydroxylaseSteroidsandrogen receptorandrogen signalingCYP17A1isoxazolesLAPC-4LNCaPmolecular dockingprostate cancerWeinreb amide

Identifiers

PMID36362320
PMCPMC9656436
OpenAlexW4308524292

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.